Laduviglusib (CHIR-99021) HCl

Synonyms: CT99021 HCl

Laduviglusib (CHIR-99021; CT99021) HCl is hydrochloride of CHIR-99021, which is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs Cdc2 and ERK2. CHIR-99021 is a potent pharmacological activators of the Wnt/beta-catenin signaling pathway. CHIR-99021 significantly rescues light-induced autophagy and augments GR, RORα and autophagy-related proteins.

Laduviglusib (CHIR-99021) HCl Chemical Structure

Laduviglusib (CHIR-99021) HCl Chemical Structure

CAS: 1797989-42-4

Selleck's Laduviglusib (CHIR-99021) HCl has been cited by 626 publications

Purity & Quality Control

Batch: Purity: 99.99%
99.99

Products often used together with Laduviglusib (CHIR-99021) HCl

Olaparib (AZD2281)


Laduviglusib HCl mediated glycogen synthase kinase (GSK3) inhibition sensitizes colorectal cancers (CRC) cells, HCT-15 to Olaparib.


Zhang N, et al. Cell Death Dis. 2021 Feb 15;12(2):183.

Y-27632 2HCl


Laduviglusib HCl and Y-27632 2HCl, along with a combination of other small molecules, promote the neuronal induction of mesenchymal stem cells (MSCs) derived from both adult and neonatal sources.


Cortés-Medina LV, et al. Stem Cells Int. 2019 Apr 1;2019:7627148.

IWR-1-endo


Laduviglusib HCl treatment upregulates total and active β-catenin, while IWR1-endo reduces active β-catenin expression in cardiac atrial appendage stem cells (CASCs) and SW480 cells.


Willems L, et al. Int J Mol Sci. 2020 May 30;21(11):3931.

MG132


Laduviglusib HCl and MG132 play a crucial role in identifying regulators of short half-life proteins when used as part of a protein stability probe.


Hickman KA, et al. Cytometry A. 2020;97(4):363-377.

IWP-2


Laduviglusib HCl and IWP-2 play a crucial role in the differentiation of human induced pluripotent stem cells (hiPSC) into cardiomyocytes.


Debus JD, et al. J Mol Cell Cardiol. 2019;129:303-313.

Laduviglusib (CHIR-99021) HCl Related Products

Signaling Pathway

Choose Selective GSK-3 Inhibitors

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-H1581 Growth Inhibition Assay IC50=900.231 μM SANGER
NCI-H1155 Growth Inhibition Assay IC50=818.059 μM SANGER
BC-3 Growth Inhibition Assay IC50=805.203 μM SANGER
KARPAS-422 Growth Inhibition Assay IC50=789.315 μM SANGER
DEL Growth Inhibition Assay IC50=700.838 μM SANGER
KM-H2 Growth Inhibition Assay IC50=699.059 μM SANGER
U-87-MG Growth Inhibition Assay IC50=694.585 μM SANGER
NCI-SNU-1 Growth Inhibition Assay IC50=690.172 μM SANGER
NCI-SNU-16 Growth Inhibition Assay IC50=680.462 μM SANGER
TUR Growth Inhibition Assay IC50=671.322 μM SANGER
IM-9 Growth Inhibition Assay IC50=651.541 μM SANGER
L-363 Growth Inhibition Assay IC50=648.064 μM SANGER
NCI-H226 Growth Inhibition Assay IC50=628.353 μM SANGER
HT Growth Inhibition Assay IC50=622.785 μM SANGER
KARPAS-45 Growth Inhibition Assay IC50=618.221 μM SANGER
ML-2 Growth Inhibition Assay IC50=606.579 μM SANGER
LP-1 Growth Inhibition Assay IC50=603.587 μM SANGER
L-428 Growth Inhibition Assay IC50=600.671 μM SANGER
K052 Growth Inhibition Assay IC50=579.213 μM SANGER
CAL-148 Growth Inhibition Assay IC50=565.089 μM SANGER
UACC-812 Growth Inhibition Assay IC50=559.391 μM SANGER
EW-11 Growth Inhibition Assay IC50=552.399 μM SANGER
COLO-320-HSR Growth Inhibition Assay IC50=551.35 μM SANGER
NCI-H889 Growth Inhibition Assay IC50=547.23 μM SANGER
EVSA-T Growth Inhibition Assay IC50=543.684 μM SANGER
RL Growth Inhibition Assay IC50=542.442 μM SANGER
HSC-4 Growth Inhibition Assay IC50=539.293 μM SANGER
NCI-H2227 Growth Inhibition Assay IC50=530.254 μM SANGER
NB5 Growth Inhibition Assay IC50=526.43 μM SANGER
NCI-H2081 Growth Inhibition Assay IC50=525.513 μM SANGER
NCI-H510A Growth Inhibition Assay IC50=524.696 μM SANGER
NCI-H1436 Growth Inhibition Assay IC50=523.064 μM SANGER
HL-60 Growth Inhibition Assay IC50=522.924 μM SANGER
Mo-T Growth Inhibition Assay IC50=515.116 μM SANGER
NCI-H2171 Growth Inhibition Assay IC50=512.705 μM SANGER
NCI-H1694 Growth Inhibition Assay IC50=512.439 μM SANGER
P12-ICHIKAWA Growth Inhibition Assay IC50=511.416 μM SANGER
DU-4475 Growth Inhibition Assay IC50=511.101 μM SANGER
RPMI-8402 Growth Inhibition Assay IC50=510.021 μM SANGER
EHEB Growth Inhibition Assay IC50=507.208 μM SANGER
CA46 Growth Inhibition Assay IC50=504.407 μM SANGER
EC-GI-10 Growth Inhibition Assay IC50=502.169 μM SANGER
CPC-N Growth Inhibition Assay IC50=502.063 μM SANGER
RPMI-6666 Growth Inhibition Assay IC50=491.398 μM SANGER
NCI-H1395 Growth Inhibition Assay IC50=489.004 μM SANGER
D-283MED Growth Inhibition Assay IC50=488.924 μM SANGER
HDLM-2 Growth Inhibition Assay IC50=480.869 μM SANGER
NCI-H446 Growth Inhibition Assay IC50=477.08 μM SANGER
JAR Growth Inhibition Assay IC50=474.788 μM SANGER
NCI-SNU-5 Growth Inhibition Assay IC50=472.28 μM SANGER
COR-L279 Growth Inhibition Assay IC50=464.847 μM SANGER
NCI-H1092 Growth Inhibition Assay IC50=463.943 μM SANGER
A3-KAW Growth Inhibition Assay IC50=460.841 μM SANGER
TE-441-T Growth Inhibition Assay IC50=457.186 μM SANGER
KMS-12-PE Growth Inhibition Assay IC50=456.822 μM SANGER
SCLC-21H Growth Inhibition Assay IC50=455.699 μM SANGER
TALL-1 Growth Inhibition Assay IC50=455.297 μM SANGER
A4-Fuk Growth Inhibition Assay IC50=454.507 μM SANGER
MS-1 Growth Inhibition Assay IC50=454.385 μM SANGER
EW-1 Growth Inhibition Assay IC50=452.888 μM SANGER
DMS-79 Growth Inhibition Assay IC50=449.68 μM SANGER
COLO-684 Growth Inhibition Assay IC50=448.888 μM SANGER
BL-70 Growth Inhibition Assay IC50=439.429 μM SANGER
AM-38 Growth Inhibition Assay IC50=438.54 μM SANGER
RH-1 Growth Inhibition Assay IC50=435.09 μM SANGER
MDA-MB-134-VI Growth Inhibition Assay IC50=431.033 μM SANGER
NCI-H2141 Growth Inhibition Assay IC50=424.388 μM SANGER
KY821 Growth Inhibition Assay IC50=414.086 μM SANGER
GR-ST Growth Inhibition Assay IC50=410.497 μM SANGER
NCI-H716 Growth Inhibition Assay IC50=410.075 μM SANGER
MES-SA Growth Inhibition Assay IC50=409.98 μM SANGER
ECC4 Growth Inhibition Assay IC50=408.458 μM SANGER
FADU Growth Inhibition Assay IC50=403.083 μM SANGER
SW962 Growth Inhibition Assay IC50=398.69 μM SANGER
TE-6 Growth Inhibition Assay IC50=397.254 μM SANGER
IST-SL1 Growth Inhibition Assay IC50=394.406 μM SANGER
MN-60 Growth Inhibition Assay IC50=393.948 μM SANGER
NCI-H719 Growth Inhibition Assay IC50=391.893 μM SANGER
GOTO Growth Inhibition Assay IC50=390.641 μM SANGER
NCI-H596 Growth Inhibition Assay IC50=385.34 μM SANGER
COR-L88 Growth Inhibition Assay IC50=383.677 μM SANGER
HCC2157 Growth Inhibition Assay IC50=378.161 μM SANGER
P31-FUJ Growth Inhibition Assay IC50=376.964 μM SANGER
U-266 Growth Inhibition Assay IC50=373.132 μM SANGER
IST-SL2 Growth Inhibition Assay IC50=372.926 μM SANGER
ChaGo-K-1 Growth Inhibition Assay IC50=363.924 μM SANGER
SJSA-1 Growth Inhibition Assay IC50=360.939 μM SANGER
NCI-H1838 Growth Inhibition Assay IC50=359.987 μM SANGER
DMS-53 Growth Inhibition Assay IC50=358.711 μM SANGER
NCI-H2126 Growth Inhibition Assay IC50=358.521 μM SANGER
COLO-678 Growth Inhibition Assay IC50=357.863 μM SANGER
CW-2 Growth Inhibition Assay IC50=356.529 μM SANGER
NCI-H358 Growth Inhibition Assay IC50=355.356 μM SANGER
P30-OHK Growth Inhibition Assay IC50=353.063 μM SANGER
NCI-H2196 Growth Inhibition Assay IC50=352.624 μM SANGER
SW1990 Growth Inhibition Assay IC50=351.28 μM SANGER
NCI-H720 Growth Inhibition Assay IC50=349.846 μM SANGER
SK-PN-DW Growth Inhibition Assay IC50=347.426 μM SANGER
DOHH-2 Growth Inhibition Assay IC50=346.65 μM SANGER
CAL-54 Growth Inhibition Assay IC50=345.879 μM SANGER
D-502MG Growth Inhibition Assay IC50=345.812 μM SANGER
NB13 Growth Inhibition Assay IC50=345.58 μM SANGER
PF-382 Growth Inhibition Assay IC50=344.422 μM SANGER
KP-4 Growth Inhibition Assay IC50=343.733 μM SANGER
VM-CUB-1 Growth Inhibition Assay IC50=342.636 μM SANGER
NCI-H2030 Growth Inhibition Assay IC50=341.609 μM SANGER
NCI-H441 Growth Inhibition Assay IC50=341.418 μM SANGER
GT3TKB Growth Inhibition Assay IC50=338.412 μM SANGER
Raji Growth Inhibition Assay IC50=338.38 μM SANGER
MLMA Growth Inhibition Assay IC50=338.155 μM SANGER
HuO9 Growth Inhibition Assay IC50=337.47 μM SANGER
ARH-77 Growth Inhibition Assay IC50=337.32 μM SANGER
LAN-6 Growth Inhibition Assay IC50=336.977 μM SANGER
LC-2-ad Growth Inhibition Assay IC50=336.591 μM SANGER
NCI-H1522 Growth Inhibition Assay IC50=334.339 μM SANGER
BT-474 Growth Inhibition Assay IC50=332.418 μM SANGER
SF268 Growth Inhibition Assay IC50=330.265 μM SANGER
LS-123 Growth Inhibition Assay IC50=328.164 μM SANGER
SK-MEL-30 Growth Inhibition Assay IC50=326.738 μM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=326.489 μM SANGER
SK-MEL-24 Growth Inhibition Assay IC50=324.111 μM SANGER
HCC1954 Growth Inhibition Assay IC50=323.582 μM SANGER
OCUB-M Growth Inhibition Assay IC50=323.434 μM SANGER
BHY Growth Inhibition Assay IC50=323.175 μM SANGER
SK-N-FI Growth Inhibition Assay IC50=322.452 μM SANGER
EW-13 Growth Inhibition Assay IC50=322.424 μM SANGER
HD-MY-Z Growth Inhibition Assay IC50=321.409 μM SANGER
CAL-51 Growth Inhibition Assay IC50=321.403 μM SANGER
EW-24 Growth Inhibition Assay IC50=320.07 μM SANGER
IMR-5 Growth Inhibition Assay IC50=315.38 μM SANGER
647-V Growth Inhibition Assay IC50=314.673 μM SANGER
SNU-475 Growth Inhibition Assay IC50=314.091 μM SANGER
J-RT3-T3-5 Growth Inhibition Assay IC50=313.521 μM SANGER
ES1 Growth Inhibition Assay IC50=312.189 μM SANGER
A388 Growth Inhibition Assay IC50=312.022 μM SANGER
ECC12 Growth Inhibition Assay IC50=310.254 μM SANGER
SCC-15 Growth Inhibition Assay IC50=306.017 μM SANGER
PLC-PRF-5 Growth Inhibition Assay IC50=304.907 μM SANGER
COLO-680N Growth Inhibition Assay IC50=302.893 μM SANGER
HLE Growth Inhibition Assay IC50=301.818 μM SANGER
C2BBe1 Growth Inhibition Assay IC50=300.691 μM SANGER
RL95-2 Growth Inhibition Assay IC50=300.247 μM SANGER
U251 Growth Inhibition Assay IC50=298.438 μM SANGER
NCI-H2347 Growth Inhibition Assay IC50=296.425 μM SANGER
SW626 Growth Inhibition Assay IC50=296.115 μM SANGER
NCI-H524 Growth Inhibition Assay IC50=295.769 μM SANGER
SHP-77 Growth Inhibition Assay IC50=295.597 μM SANGER
HT-1197 Growth Inhibition Assay IC50=292.879 μM SANGER
HuP-T3 Growth Inhibition Assay IC50=292.146 μM SANGER
ABC-1 Growth Inhibition Assay IC50=291.069 μM SANGER
HC-1 Growth Inhibition Assay IC50=290.602 μM SANGER
GMS-10 Growth Inhibition Assay IC50=287.183 μM SANGER
NCI-H1882 Growth Inhibition Assay IC50=286.035 μM SANGER
EW-7 Growth Inhibition Assay IC50=285.232 μM SANGER
T84 Growth Inhibition Assay IC50=284.665 μM SANGER
NCI-H2009 Growth Inhibition Assay IC50=283.953 μM SANGER
SH-4 Growth Inhibition Assay IC50=283.123 μM SANGER
TGW Growth Inhibition Assay IC50=283.058 μM SANGER
UACC-893 Growth Inhibition Assay IC50=280.54 μM SANGER
NCI-H1792 Growth Inhibition Assay IC50=279.187 μM SANGER
CAMA-1 Growth Inhibition Assay IC50=278.279 μM SANGER
NB69 Growth Inhibition Assay IC50=277.405 μM SANGER
BEN Growth Inhibition Assay IC50=276.461 μM SANGER
TE-10 Growth Inhibition Assay IC50=276.439 μM SANGER
SK-MEL-3 Growth Inhibition Assay IC50=275.457 μM SANGER
ES3 Growth Inhibition Assay IC50=270.358 μM SANGER
MHH-CALL-2 Growth Inhibition Assay IC50=269.92 μM SANGER
LN-405 Growth Inhibition Assay IC50=269.708 μM SANGER
MDA-MB-468 Growth Inhibition Assay IC50=269.333 μM SANGER
RD Growth Inhibition Assay IC50=269.119 μM SANGER
CAL-12T Growth Inhibition Assay IC50=268.366 μM SANGER
LU-165 Growth Inhibition Assay IC50=267.941 μM SANGER
A673 Growth Inhibition Assay IC50=267.025 μM SANGER
VA-ES-BJ Growth Inhibition Assay IC50=261.918 μM SANGER
MMAC-SF Growth Inhibition Assay IC50=261.192 μM SANGER
HuH-7 Growth Inhibition Assay IC50=260.996 μM SANGER
CAL-39 Growth Inhibition Assay IC50=260.272 μM SANGER
HSC-2 Growth Inhibition Assay IC50=258.584 μM SANGER
NCI-H187 Growth Inhibition Assay IC50=256.76 μM SANGER
CAL-27 Growth Inhibition Assay IC50=253.485 μM SANGER
NCI-H1304 Growth Inhibition Assay IC50=253.156 μM SANGER
TGBC1TKB Growth Inhibition Assay IC50=252.875 μM SANGER
NCI-H460 Growth Inhibition Assay IC50=251.417 μM SANGER
NCI-H2228 Growth Inhibition Assay IC50=250.864 μM SANGER
COR-L23 Growth Inhibition Assay IC50=250.412 μM SANGER
NCI-H1693 Growth Inhibition Assay IC50=249.495 μM SANGER
LC-1F Growth Inhibition Assay IC50=248.156 μM SANGER
KYSE-510 Growth Inhibition Assay IC50=247.517 μM SANGER
T47D Growth Inhibition Assay IC50=247.013 μM SANGER
SK-HEP-1 Growth Inhibition Assay IC50=246.043 μM SANGER
ES5 Growth Inhibition Assay IC50=245.038 μM SANGER
BFTC-909 Growth Inhibition Assay IC50=243.118 μM SANGER
HN Growth Inhibition Assay IC50=242.991 μM SANGER
GP5d Growth Inhibition Assay IC50=242.616 μM SANGER
IPC-298 Growth Inhibition Assay IC50=242.072 μM SANGER
EB2 Growth Inhibition Assay IC50=241.907 μM SANGER
MOLT-4 Growth Inhibition Assay IC50=241.209 μM SANGER
SW954 Growth Inhibition Assay IC50=237.868 μM SANGER
NCCIT Growth Inhibition Assay IC50=236.873 μM SANGER
NOMO-1 Growth Inhibition Assay IC50=236.02 μM SANGER
NCI-H520 Growth Inhibition Assay IC50=235.741 μM SANGER
GB-1 Growth Inhibition Assay IC50=235.177 μM SANGER
SW1783 Growth Inhibition Assay IC50=234.41 μM SANGER
YAPC Growth Inhibition Assay IC50=234.253 μM SANGER
MSTO-211H Growth Inhibition Assay IC50=233.276 μM SANGER
5637 Growth Inhibition Assay IC50=233.003 μM SANGER
NCI-H630 Growth Inhibition Assay IC50=232.897 μM SANGER
CHL-1 Growth Inhibition Assay IC50=228.13 μM SANGER
NCI-H322M Growth Inhibition Assay IC50=228.019 μM SANGER
NCI-H209 Growth Inhibition Assay IC50=226.53 μM SANGER
HCC1937 Growth Inhibition Assay IC50=224.389 μM SANGER
SAS Growth Inhibition Assay IC50=223.796 μM SANGER
AGS Growth Inhibition Assay IC50=222.523 μM SANGER
NCI-H1623 Growth Inhibition Assay IC50=222.389 μM SANGER
NCI-H1993 Growth Inhibition Assay IC50=222.239 μM SANGER
NCI-H1355 Growth Inhibition Assay IC50=221.377 μM SANGER
CaR-1 Growth Inhibition Assay IC50=221.251 μM SANGER
NCI-H1618 Growth Inhibition Assay IC50=221.018 μM SANGER
BC-1 Growth Inhibition Assay IC50=220.799 μM SANGER
SCC-3 Growth Inhibition Assay IC50=220.577 μM SANGER
SCC-4 Growth Inhibition Assay IC50=220.353 μM SANGER
THP-1 Growth Inhibition Assay IC50=219.606 μM SANGER
HOS Growth Inhibition Assay IC50=218.9 μM SANGER
LB771-HNC Growth Inhibition Assay IC50=217.893 μM SANGER
DMS-153 Growth Inhibition Assay IC50=217.836 μM SANGER
UACC-257 Growth Inhibition Assay IC50=217.43 μM SANGER
C3A Growth Inhibition Assay IC50=215.575 μM SANGER
ES7 Growth Inhibition Assay IC50=214.878 μM SANGER
NCI-H69 Growth Inhibition Assay IC50=214.185 μM SANGER
HO-1-N-1 Growth Inhibition Assay IC50=212.894 μM SANGER
TCCSUP Growth Inhibition Assay IC50=211.533 μM SANGER
A431 Growth Inhibition Assay IC50=211.299 μM SANGER
BT-20 Growth Inhibition Assay IC50=210.986 μM SANGER
EW-18 Growth Inhibition Assay IC50=210.763 μM SANGER
MHH-PREB-1 Growth Inhibition Assay IC50=210.381 μM SANGER
DJM-1 Growth Inhibition Assay IC50=209.897 μM SANGER
NUGC-3 Growth Inhibition Assay IC50=209.678 μM SANGER
HPAF-II Growth Inhibition Assay IC50=209.671 μM SANGER
NCI-H1651 Growth Inhibition Assay IC50=206.73 μM SANGER
RPMI-2650 Growth Inhibition Assay IC50=205.467 μM SANGER
EGI-1 Growth Inhibition Assay IC50=204.833 μM SANGER
KYSE-70 Growth Inhibition Assay IC50=203.879 μM SANGER
NCI-H345 Growth Inhibition Assay IC50=203.027 μM SANGER
LS-1034 Growth Inhibition Assay IC50=202.553 μM SANGER
LAMA-84 Growth Inhibition Assay IC50=202.073 μM SANGER
MFE-280 Growth Inhibition Assay IC50=201.961 μM SANGER
MDA-MB-231 Growth Inhibition Assay IC50=200.902 μM SANGER
MFM-223 Growth Inhibition Assay IC50=201.587 μM SANGER
COLO-679 Growth Inhibition Assay IC50=200.859 μM SANGER
SJRH30 Growth Inhibition Assay IC50=200.515 μM SANGER
QIMR-WIL Growth Inhibition Assay IC50=200.116 μM SANGER
HT55 Growth Inhibition Assay IC50=199.192 μM SANGER
JVM-3 Growth Inhibition Assay IC50=198.419 μM SANGER
TE-5 Growth Inhibition Assay IC50=198.033 μM SANGER
IA-LM Growth Inhibition Assay IC50=197.822 μM SANGER
22RV1 Growth Inhibition Assay IC50=197.424 μM SANGER
TE-1 Growth Inhibition Assay IC50=196.26 μM SANGER
SW780 Growth Inhibition Assay IC50=196.734 μM SANGER
KOSC-2 Growth Inhibition Assay IC50=195.818 μM SANGER
SW1088 Growth Inhibition Assay IC50=195.677 μM SANGER
HGC-27 Growth Inhibition Assay IC50=195.538 μM SANGER
COLO-668 Growth Inhibition Assay IC50=193.157 μM SANGER
A2780 Growth Inhibition Assay IC50=192.891 μM SANGER
HCE-4 Growth Inhibition Assay IC50=190.992 μM SANGER
NCI-H838 Growth Inhibition Assay IC50=190.34 μM SANGER
ETK-1 Growth Inhibition Assay IC50=190.181 μM SANGER
KG-1 Growth Inhibition Assay IC50=189.798 μM SANGER
NCI-H1299 Growth Inhibition Assay IC50=188.719 μM SANGER
SK-LU-1 Growth Inhibition Assay IC50=188.428 μM SANGER
CAPAN-1 Growth Inhibition Assay IC50=187.453 μM SANGER
MONO-MAC-6 Growth Inhibition Assay IC50=187.392 μM SANGER
MDA-MB-453 Growth Inhibition Assay IC50=186.941 μM SANGER
NCI-H1563 Growth Inhibition Assay IC50=185.209 μM SANGER
LB2241-RCC Growth Inhibition Assay IC50=185.145 μM SANGER
MRK-nu-1 Growth Inhibition Assay IC50=184.972 μM SANGER
MDA-MB-415 Growth Inhibition Assay IC50=184.651 μM SANGER
DOK Growth Inhibition Assay IC50=184.643 μM SANGER
A427 Growth Inhibition Assay IC50=184.631 μM SANGER
SN12C Growth Inhibition Assay IC50=182.829 μM SANGER
LOUCY Growth Inhibition Assay IC50=182.688 μM SANGER
ONS-76 Growth Inhibition Assay IC50=182.387 μM SANGER
SBC-5 Growth Inhibition Assay IC50=181.934 μM SANGER
GI-ME-N Growth Inhibition Assay IC50=181.672 μM SANGER
PSN1 Growth Inhibition Assay IC50=181.66 μM SANGER
NCI-H522 Growth Inhibition Assay IC50=181.059 μM SANGER
SF126 Growth Inhibition Assay IC50=179.432 μM SANGER
NB10 Growth Inhibition Assay IC50=177.846 μM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=177.806 μM SANGER
COLO-741 Growth Inhibition Assay IC50=177.561 μM SANGER
EW-3 Growth Inhibition Assay IC50=176.555 μM SANGER
YT Growth Inhibition Assay IC50=176.399 μM SANGER
LNCaP-Clone-FGC Growth Inhibition Assay IC50=175.861 μM SANGER
SW756 Growth Inhibition Assay IC50=174.863 μM SANGER
ME-180 Growth Inhibition Assay IC50=174.016 μM SANGER
HH Growth Inhibition Assay IC50=173.848 μM SANGER
HuO-3N1 Growth Inhibition Assay IC50=172.273 μM SANGER
SW620 Growth Inhibition Assay IC50=171.535 μM SANGER
HUTU-80 Growth Inhibition Assay IC50=171.032 μM SANGER
Daoy Growth Inhibition Assay IC50=169.891 μM SANGER
KYSE-150 Growth Inhibition Assay IC50=169.636 μM SANGER
CP66-MEL Growth Inhibition Assay IC50=168.415 μM SANGER
Calu-3 Growth Inhibition Assay IC50=168.311 μM SANGER
JVM-2 Growth Inhibition Assay IC50=167.451 μM SANGER
OVCAR-5 Growth Inhibition Assay IC50=168.309 μM SANGER
KINGS-1 Growth Inhibition Assay IC50=167.354 μM SANGER
EFO-21 Growth Inhibition Assay IC50=165.45 μM SANGER
Ca9-22 Growth Inhibition Assay IC50=164.321 μM SANGER
AU565 Growth Inhibition Assay IC50=163.64 μM SANGER
CHP-212 Growth Inhibition Assay IC50=163.626 μM SANGER
CAL-62 Growth Inhibition Assay IC50=162.613 μM SANGER
EFO-27 Growth Inhibition Assay IC50=160.584 μM SANGER
NCI-H2052 Growth Inhibition Assay IC50=159.583 μM SANGER
ES4 Growth Inhibition Assay IC50=159.396 μM SANGER
HCC70 Growth Inhibition Assay IC50=159.242 μM SANGER
HCC38 Growth Inhibition Assay IC50=157.369 μM SANGER
DG-75 Growth Inhibition Assay IC50=156.694 μM SANGER
HCC1419 Growth Inhibition Assay IC50=156.077 μM SANGER
CAL-120 Growth Inhibition Assay IC50=155.821 μM SANGER
DK-MG Growth Inhibition Assay IC50=155.183 μM SANGER
RERF-LC-MS Growth Inhibition Assay IC50=154.772 μM SANGER
Calu-1 Growth Inhibition Assay IC50=154.003 μM SANGER
TT Growth Inhibition Assay IC50=153.49 μM SANGER
MDA-MB-361 Growth Inhibition Assay IC50=153.164 μM SANGER
AsPC-1 Growth Inhibition Assay IC50=152.764 μM SANGER
GAK Growth Inhibition Assay IC50=151.374 μM SANGER
GDM-1 Growth Inhibition Assay IC50=151.135 μM SANGER
NCI-H748 Growth Inhibition Assay IC50=150.209 μM SANGER
L-540 Growth Inhibition Assay IC50=149.75 μM SANGER
Caov-3 Growth Inhibition Assay IC50=149.714 μM SANGER
TE-9 Growth Inhibition Assay IC50=149.443 μM SANGER
639-V Growth Inhibition Assay IC50=148.705 μM SANGER
LB647-SCLC Growth Inhibition Assay IC50=148.562 μM SANGER
KYSE-520 Growth Inhibition Assay IC50=148.54 μM SANGER
GAMG Growth Inhibition Assay IC50=148.247 μM SANGER
GCIY Growth Inhibition Assay IC50=147.797 μM SANGER
DMS-114 Growth Inhibition Assay IC50=147.441 μM SANGER
BB49-HNC Growth Inhibition Assay IC50=147.404 μM SANGER
SW13 Growth Inhibition Assay IC50=147.253 μM SANGER
LK-2 Growth Inhibition Assay IC50=147.143 μM SANGER
OMC-1 Growth Inhibition Assay IC50=145.967 μM SANGER
G-401 Growth Inhibition Assay IC50=145.835 μM SANGER
HTC-C3 Growth Inhibition Assay IC50=145.075 μM SANGER
SCC-25 Growth Inhibition Assay IC50=144.005 μM SANGER
NCI-H810 Growth Inhibition Assay IC50=143.687 μM SANGER
CCF-STTG1 Growth Inhibition Assay IC50=143.334 μM SANGER
YKG-1 Growth Inhibition Assay IC50=142.889 μM SANGER
OE33 Growth Inhibition Assay IC50=141.798 μM SANGER
OCI-AML2 Growth Inhibition Assay IC50=141.507 μM SANGER
Detroit562 Growth Inhibition Assay IC50=141.466 μM SANGER
OVCAR-4 Growth Inhibition Assay IC50=140.749 μM SANGER
BHT-101 Growth Inhibition Assay IC50=140.208 μM SANGER
Ca-Ski Growth Inhibition Assay IC50=138.831 μM SANGER
OAW-42 Growth Inhibition Assay IC50=137.856 μM SANGER
G-402 Growth Inhibition Assay IC50=135.295 μM SANGER
NOS-1 Growth Inhibition Assay IC50=134.765 μM SANGER
NCI-H1437 Growth Inhibition Assay IC50=134.59 μM SANGER
JEG-3 Growth Inhibition Assay IC50=134.359 μM SANGER
CP50-MEL-B Growth Inhibition Assay IC50=134.2 μM SANGER
BB30-HNC Growth Inhibition Assay IC50=134.116 μM SANGER
Capan-2 Growth Inhibition Assay IC50=133.975 μM SANGER
CTB-1 Growth Inhibition Assay IC50=132.897 μM SANGER
HT-1080 Growth Inhibition Assay IC50=132.204 μM SANGER
MFH-ino Growth Inhibition Assay IC50=131.114 μM SANGER
VMRC-RCZ Growth Inhibition Assay IC50=130.375 μM SANGER
LU-99A Growth Inhibition Assay IC50=129.931 μM SANGER
HEC-1 Growth Inhibition Assay IC50=129.198 μM SANGER
EB-3 Growth Inhibition Assay IC50=127.013 μM SANGER
UMC-11 Growth Inhibition Assay IC50=126.038 μM SANGER
NCI-H2087 Growth Inhibition Assay IC50=124.283 μM SANGER
SW1463 Growth Inhibition Assay IC50=124.077 μM SANGER
OPM-2 Growth Inhibition Assay IC50=123.176 μM SANGER
HT-29 Growth Inhibition Assay IC50=122.778 μM SANGER
HAL-01 Growth Inhibition Assay IC50=122.499 μM SANGER
KYSE-140 Growth Inhibition Assay IC50=122.141 μM SANGER
HuP-T4 Growth Inhibition Assay IC50=121.55 μM SANGER
NCI-N87 Growth Inhibition Assay IC50=121.044 μM SANGER
OVCAR-3 Growth Inhibition Assay IC50=119.915 μM SANGER
KNS-81-FD Growth Inhibition Assay IC50=119.417 μM SANGER
SUP-T1 Growth Inhibition Assay IC50=118.956 μM SANGER
SKG-IIIa Growth Inhibition Assay IC50=118.116 μM SANGER
RKO Growth Inhibition Assay IC50=117.898 μM SANGER
ATN-1 Growth Inhibition Assay IC50=117.828 μM SANGER
OVCAR-8 Growth Inhibition Assay IC50=117.668 μM SANGER
HCC1599 Growth Inhibition Assay IC50=117.156 μM SANGER
Calu-6 Growth Inhibition Assay IC50=116.798 μM SANGER
DMS-273 Growth Inhibition Assay IC50=115.617 μM SANGER
786-0 Growth Inhibition Assay IC50=113.453 μM SANGER
SIG-M5 Growth Inhibition Assay IC50=113.125 μM SANGER
NEC8 Growth Inhibition Assay IC50=112.624 μM SANGER
MDA-MB-157 Growth Inhibition Assay IC50=112.49 μM SANGER
U031 Growth Inhibition Assay IC50=112.065 μM SANGER
WSU-NHL Growth Inhibition Assay IC50=112.01 μM SANGER
HCT-15 Growth Inhibition Assay IC50=110.661 μM SANGER
A253 Growth Inhibition Assay IC50=110.479 μM SANGER
DU-145 Growth Inhibition Assay IC50=109.945 μM SANGER
D-263MG Growth Inhibition Assay IC50=108.961 μM SANGER
FTC-133 Growth Inhibition Assay IC50=108.488 μM SANGER
HOP-92 Growth Inhibition Assay IC50=108.475 μM SANGER
NCI-H23 Growth Inhibition Assay IC50=108.357 μM SANGER
PANC-08-13 Growth Inhibition Assay IC50=106.85 μM SANGER
RPMI-8226 Growth Inhibition Assay IC50=106.678 μM SANGER
SNU-C2B Growth Inhibition Assay IC50=105.023 μM SANGER
UM-UC-3 Growth Inhibition Assay IC50=103.842 μM SANGER
MKN45 Growth Inhibition Assay IC50=103.584 μM SANGER
KE-37 Growth Inhibition Assay IC50=102.95 μM SANGER
SK-MES-1 Growth Inhibition Assay IC50=101.762 μM SANGER
TE-11 Growth Inhibition Assay IC50=101.724 μM SANGER
Saos-2 Growth Inhibition Assay IC50=101.437 μM SANGER
LU-65 Growth Inhibition Assay IC50=101.081 μM SANGER
Mewo Growth Inhibition Assay IC50=99.5603 μM SANGER
IGR-1 Growth Inhibition Assay IC50=99.3119 μM SANGER
NCI-H292 Growth Inhibition Assay IC50=99.3004 μM SANGER
PC-3 Growth Inhibition Assay IC50=99.0564 μM SANGER
U-698-M Growth Inhibition Assay IC50=98.9489 μM SANGER
MKN7 Growth Inhibition Assay IC50=97.7439 μM SANGER
OS-RC-2 Growth Inhibition Assay IC50=97.461 μM SANGER
Caov-4 Growth Inhibition Assay IC50=95.685 μM SANGER
A2058 Growth Inhibition Assay IC50=95.4617 μM SANGER
RMG-I Growth Inhibition Assay IC50=95.1072 μM SANGER
MEL-JUSO Growth Inhibition Assay IC50=94.954 μM SANGER
MZ1-PC Growth Inhibition Assay IC50=94.5984 μM SANGER
J82 Growth Inhibition Assay IC50=93.7811 μM SANGER
23132-87 Growth Inhibition Assay IC50=93.168 μM SANGER
CAL-33 Growth Inhibition Assay IC50=93.0601 μM SANGER
BOKU Growth Inhibition Assay IC50=92.6957 μM SANGER
MZ7-mel Growth Inhibition Assay IC50=91.2676 μM SANGER
C-33-A Growth Inhibition Assay IC50=90.54 μM SANGER
NCI-H650 Growth Inhibition Assay IC50=89.8724 μM SANGER
TE-12 Growth Inhibition Assay IC50=89.3741 μM SANGER
MDA-MB-175-VII Growth Inhibition Assay IC50=85.7426 μM SANGER
SBC-1 Growth Inhibition Assay IC50=84.0208 μM SANGER
BFTC-905 Growth Inhibition Assay IC50=84.0172 μM SANGER
SW1573 Growth Inhibition Assay IC50=82.5893 μM SANGER
KMOE-2 Growth Inhibition Assay IC50=81.8531 μM SANGER
NCI-H1417 Growth Inhibition Assay IC50=81.4368 μM SANGER
NCI-H661 Growth Inhibition Assay IC50=81.344 μM SANGER
NB12 Growth Inhibition Assay IC50=80.9369 μM SANGER
KYSE-410 Growth Inhibition Assay IC50=80.2857 μM SANGER
HCE-T Growth Inhibition Assay IC50=80.1588 μM SANGER
SF295 Growth Inhibition Assay IC50=79.9553 μM SANGER
KP-N-YS Growth Inhibition Assay IC50=78.5878 μM SANGER
PANC-03-27 Growth Inhibition Assay IC50=78.435 μM SANGER
NB6 Growth Inhibition Assay IC50=78.1299 μM SANGER
HSC-3 Growth Inhibition Assay IC50=77.0282 μM SANGER
8-MG-BA Growth Inhibition Assay IC50=76.1096 μM SANGER
SK-MEL-1 Growth Inhibition Assay IC50=75.8019 μM SANGER
LS-411N Growth Inhibition Assay IC50=74.2528 μM SANGER
RT4 Growth Inhibition Assay IC50=73.5742 μM SANGER
KALS-1 Growth Inhibition Assay IC50=73.5475 μM SANGER
EW-16 Growth Inhibition Assay IC50=71.7415 μM SANGER
HCC1806 Growth Inhibition Assay IC50=71.4587 μM SANGER
Hs-578-T Growth Inhibition Assay IC50=70.3 μM SANGER
NCI-H2342 Growth Inhibition Assay IC50=69.3961 μM SANGER
C-4-II Growth Inhibition Assay IC50=69.3607 μM SANGER
NCI-H1703 Growth Inhibition Assay IC50=68.1171 μM SANGER
HuCCT1 Growth Inhibition Assay IC50=67.0374 μM SANGER
MFE-296 Growth Inhibition Assay IC50=64.4473 μM SANGER
AN3-CA Growth Inhibition Assay IC50=64.3035 μM SANGER
SCH Growth Inhibition Assay IC50=64.2351 μM SANGER
T-24 Growth Inhibition Assay IC50=62.7126 μM SANGER
K-562 Growth Inhibition Assay IC50=62.2452 μM SANGER
NCI-H1734 Growth Inhibition Assay IC50=61.9663 μM SANGER
NMC-G1 Growth Inhibition Assay IC50=61.9242 μM SANGER
EKVX Growth Inhibition Assay IC50=61.4958 μM SANGER
SiHa Growth Inhibition Assay IC50=59.6487 μM SANGER
LU-134-A Growth Inhibition Assay IC50=59.6016 μM SANGER
ACN Growth Inhibition Assay IC50=59.1587 μM SANGER
HT-1376 Growth Inhibition Assay IC50=59.0921 μM SANGER
LCLC-97TM1 Growth Inhibition Assay IC50=59.0553 μM SANGER
BV-173 Growth Inhibition Assay IC50=57.5142 μM SANGER
RPMI-8866 Growth Inhibition Assay IC50=57.2412 μM SANGER
DoTc2-4510 Growth Inhibition Assay IC50=56.6057 μM SANGER
NCI-H2405 Growth Inhibition Assay IC50=56.1693 μM SANGER
RCM-1 Growth Inhibition Assay IC50=56.0078 μM SANGER
DV-90 Growth Inhibition Assay IC50=55.8917 μM SANGER
ES6 Growth Inhibition Assay IC50=55.8899 μM SANGER
LXF-289 Growth Inhibition Assay IC50=55.5066 μM SANGER
A375 Growth Inhibition Assay IC50=54.8059 μM SANGER
MC-IXC Growth Inhibition Assay IC50=54.4364 μM SANGER
697 Growth Inhibition Assay IC50=54.1555 μM SANGER
KGN Growth Inhibition Assay IC50=53.959 μM SANGER
MG-63 Growth Inhibition Assay IC50=53.9381 μM SANGER
COLO-824 Growth Inhibition Assay IC50=53.6976 μM SANGER
CHP-126 Growth Inhibition Assay IC50=53.5169 μM SANGER
CESS Growth Inhibition Assay IC50=52.145 μM SANGER
DB Growth Inhibition Assay IC50=51.9855 μM SANGER
SW837 Growth Inhibition Assay IC50=51.9785 μM SANGER
SK-N-AS Growth Inhibition Assay IC50=51.8281 μM SANGER
MCF7 Growth Inhibition Assay IC50=51.7554 μM SANGER
NCI-H1650 Growth Inhibition Assay IC50=51.5849 μM SANGER
NCI-H1793 Growth Inhibition Assay IC50=51.231 μM SANGER
KS-1 Growth Inhibition Assay IC50=50.2225 μM SANGER
LC4-1 Growth Inhibition Assay IC50=49.8912 μM SANGER
SNU-C1 Growth Inhibition Assay IC50=49.3207 μM SANGER
COR-L105 Growth Inhibition Assay IC50=48.973 μM SANGER
SNB75 Growth Inhibition Assay IC50=48.4118 μM SANGER
HCC2998 Growth Inhibition Assay IC50=48.2982 μM SANGER
NCI-H747 Growth Inhibition Assay IC50=47.7264 μM SANGER
D-542MG Growth Inhibition Assay IC50=47.4589 μM SANGER
UACC-62 Growth Inhibition Assay IC50=46.8608 μM SANGER
no-11 Growth Inhibition Assay IC50=46.2031 μM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=46.0755 μM SANGER
COLO-800 Growth Inhibition Assay IC50=45.5898 μM SANGER
H4 Growth Inhibition Assay IC50=45.3296 μM SANGER
KYSE-270 Growth Inhibition Assay IC50=45.0437 μM SANGER
ESS-1 Growth Inhibition Assay IC50=44.2062 μM SANGER
SR Growth Inhibition Assay IC50=43.8673 μM SANGER
TE-8 Growth Inhibition Assay IC50=43.7895 μM SANGER
LB831-BLC Growth Inhibition Assay IC50=43.697 μM SANGER
HCT-116 Growth Inhibition Assay IC50=43.2099 μM SANGER
IST-MEL1 Growth Inhibition Assay IC50=42.6938 μM SANGER
NY Growth Inhibition Assay IC50=42.1801 μM SANGER
MPP-89 Growth Inhibition Assay IC50=41.9211 μM SANGER
SK-CO-1 Growth Inhibition Assay IC50=41.7755 μM SANGER
BE-13 Growth Inhibition Assay IC50=41.4473 μM SANGER
HCC2218 Growth Inhibition Assay IC50=40.5849 μM SANGER
KM12 Growth Inhibition Assay IC50=38.5998 μM SANGER
CMK Growth Inhibition Assay IC50=38.4162 μM SANGER
HT-144 Growth Inhibition Assay IC50=38.2575 μM SANGER
no-10 Growth Inhibition Assay IC50=38.1294 μM SANGER
MKN1 Growth Inhibition Assay IC50=36.8444 μM SANGER
SK-UT-1 Growth Inhibition Assay IC50=36.3331 μM SANGER
8505C Growth Inhibition Assay IC50=35.9294 μM SANGER
EFE-184 Growth Inhibition Assay IC50=35.917 μM SANGER
IGROV-1 Growth Inhibition Assay IC50=35.3416 μM SANGER
TK10 Growth Inhibition Assay IC50=35.1322 μM SANGER
PFSK-1 Growth Inhibition Assay IC50=34.9241 μM SANGER
KU-19-19 Growth Inhibition Assay IC50=33.7534 μM SANGER
RVH-421 Growth Inhibition Assay IC50=33.168 μM SANGER
NCI-H1648 Growth Inhibition Assay IC50=32.8467 μM SANGER
HCC1143 Growth Inhibition Assay IC50=32.7979 μM SANGER
SW948 Growth Inhibition Assay IC50=32.7548 μM SANGER
KNS-42 Growth Inhibition Assay IC50=31.8662 μM SANGER
CAS-1 Growth Inhibition Assay IC50=31.7665 μM SANGER
LB373-MEL-D Growth Inhibition Assay IC50=31.0047 μM SANGER
SK-MM-2 Growth Inhibition Assay IC50=30.9792 μM SANGER
NALM-6 Growth Inhibition Assay IC50=30.4965 μM SANGER
CAKI-1 Growth Inhibition Assay IC50=30.2656 μM SANGER
LCLC-103H Growth Inhibition Assay IC50=30.2059 μM SANGER
IST-MES1 Growth Inhibition Assay IC50=29.7092 μM SANGER
A204 Growth Inhibition Assay IC50=29.6828 μM SANGER
JiyoyeP-2003 Growth Inhibition Assay IC50=29.6719 μM SANGER
SW872 Growth Inhibition Assay IC50=28.5326 μM SANGER
C32 Growth Inhibition Assay IC50=28.0826 μM SANGER
OAW-28 Growth Inhibition Assay IC50=28.0052 μM SANGER
SU-DHL-1 Growth Inhibition Assay IC50=27.9474 μM SANGER
MC-CAR Growth Inhibition Assay IC50=27.7907 μM SANGER
ES8 Growth Inhibition Assay IC50=27.7814 μM SANGER
COLO-792 Growth Inhibition Assay IC50=27.7728 μM SANGER
NCI-H2170 Growth Inhibition Assay IC50=27.5282 μM SANGER
KLE Growth Inhibition Assay IC50=27.2565 μM SANGER
SNG-M Growth Inhibition Assay IC50=27.2271 μM SANGER
NCI-H1770 Growth Inhibition Assay IC50=26.8986 μM SANGER
RO82-W-1 Growth Inhibition Assay IC50=26.7377 μM SANGER
KASUMI-1 Growth Inhibition Assay IC50=24.9328 μM SANGER
LU-139 Growth Inhibition Assay IC50=24.835 μM SANGER
NCI-H1963 Growth Inhibition Assay IC50=24.2839 μM SANGER
HMV-II Growth Inhibition Assay IC50=24.2163 μM SANGER
PANC-10-05 Growth Inhibition Assay IC50=24.0898 μM SANGER
K5 Growth Inhibition Assay IC50=23.5486 μM SANGER
REH Growth Inhibition Assay IC50=23.1699 μM SANGER
M14 Growth Inhibition Assay IC50=23.1132 μM SANGER
GI-1 Growth Inhibition Assay IC50=22.7841 μM SANGER
KURAMOCHI Growth Inhibition Assay IC50=22.7069 μM SANGER
LS-513 Growth Inhibition Assay IC50=22.6192 μM SANGER
RXF393 Growth Inhibition Assay IC50=22.6068 μM SANGER
SW684 Growth Inhibition Assay IC50=22.2858 μM SANGER
KARPAS-299 Growth Inhibition Assay IC50=22.1954 μM SANGER
TGBC24TKB Growth Inhibition Assay IC50=21.8957 μM SANGER
EoL-1- Growth Inhibition Assay IC50=21.8385 μM SANGER
BPH-1 Growth Inhibition Assay IC50=21.7035 μM SANGER
SK-MEL-28 Growth Inhibition Assay IC50=21.6863 μM SANGER
KYSE-450 Growth Inhibition Assay IC50=21.5354 μM SANGER
HCC1187 Growth Inhibition Assay IC50=20.3589 μM SANGER
NCI-H727 Growth Inhibition Assay IC50=20.2169 μM SANGER
Becker Growth Inhibition Assay IC50=20.1777 μM SANGER
MHH-NB-11 Growth Inhibition Assay IC50=19.5342 μM SANGER
A101D Growth Inhibition Assay IC50=19.243 μM SANGER
SNU-449 Growth Inhibition Assay IC50=18.715 μM SANGER
EM-2 Growth Inhibition Assay IC50=18.6248 μM SANGER
8305C Growth Inhibition Assay IC50=18.5305 μM SANGER
SIMA Growth Inhibition Assay IC50=17.9118 μM SANGER
Daudi Growth Inhibition Assay IC50=17.6149 μM SANGER
CCRF-CEM Growth Inhibition Assay IC50=16.6702 μM SANGER
NH-12 Growth Inhibition Assay IC50=16.0097 μM SANGER
LoVo Growth Inhibition Assay IC50=15.2659 μM SANGER
ST486 Growth Inhibition Assay IC50=14.2251 μM SANGER
NB1 Growth Inhibition Assay IC50=14.1935 μM SANGER
SF539 Growth Inhibition Assay IC50=14.0116 μM SANGER
SW48 Growth Inhibition Assay IC50=13.7265 μM SANGER
MEL-HO Growth Inhibition Assay IC50=13.8829 μM SANGER
KU812 Growth Inhibition Assay IC50=13.5175 μM SANGER
T98G Growth Inhibition Assay IC50=13.4717 μM SANGER
DSH1 Growth Inhibition Assay IC50=13.3879 μM SANGER
NCI-H82 Growth Inhibition Assay IC50=13.2909 μM SANGER
C8166 Growth Inhibition Assay IC50=13.2318 μM SANGER
PC-14 Growth Inhibition Assay IC50=12.324 μM SANGER
PA-1 Growth Inhibition Assay IC50=11.93 μM SANGER
HEL Growth Inhibition Assay IC50=11.6579 μM SANGER
NCI-H526 Growth Inhibition Assay IC50=11.1365 μM SANGER
SNU-387 Growth Inhibition Assay IC50=10.7235 μM SANGER
HT-3 Growth Inhibition Assay IC50=10.6179 μM SANGER
M059J Growth Inhibition Assay IC50=10.6102 μM SANGER
MZ2-MEL Growth Inhibition Assay IC50=10.4677 μM SANGER
NCI-H28 Growth Inhibition Assay IC50=10.4413 μM SANGER
LB1047-RCC Growth Inhibition Assay IC50=9.99798 μM SANGER
U-118-MG Growth Inhibition Assay IC50=9.94444 μM SANGER
DBTRG-05MG Growth Inhibition Assay IC50=9.7777 μM SANGER
EFM-19 Growth Inhibition Assay IC50=9.75566 μM SANGER
SK-N-DZ Growth Inhibition Assay IC50=9.65742 μM SANGER
LB996-RCC Growth Inhibition Assay IC50=9.52397 μM SANGER
U-2-OS Growth Inhibition Assay IC50=9.45006 μM SANGER
CTV-1 Growth Inhibition Assay IC50=9.43894 μM SANGER
COLO-205 Growth Inhibition Assay IC50=9.43821 μM SANGER
NCI-H64 Growth Inhibition Assay IC50=9.42255 μM SANGER
NCI-H1755 Growth Inhibition Assay IC50=9.39986 μM SANGER
ACHN Growth Inhibition Assay IC50=9.30546 μM SANGER
MEG-01 Growth Inhibition Assay IC50=8.99043 μM SANGER
MKN28 Growth Inhibition Assay IC50=8.88516 μM SANGER
CAL-72 Growth Inhibition Assay IC50=8.76113 μM SANGER
MV-4-11 Growth Inhibition Assay IC50=8.54304 μM SANGER
SW1417 Growth Inhibition Assay IC50=7.64584 μM SANGER
G-361 Growth Inhibition Assay IC50=7.46561 μM SANGER
MC116 Growth Inhibition Assay IC50=7.28691 μM SANGER
RT-112 Growth Inhibition Assay IC50=7.16456 μM SANGER
CAL-85-1 Growth Inhibition Assay IC50=6.60936 μM SANGER
BB65-RCC Growth Inhibition Assay IC50=6.53195 μM SANGER
CGTH-W-1 Growth Inhibition Assay IC50=6.417 μM SANGER
WM-115 Growth Inhibition Assay IC50=5.81509 μM SANGER
SK-MEL-2 Growth Inhibition Assay IC50=6.38344 μM SANGER
BL-41 Growth Inhibition Assay IC50=5.81266 μM SANGER
LB2518-MEL Growth Inhibition Assay IC50=5.72627 μM SANGER
D-392MG Growth Inhibition Assay IC50=5.49145 μM SANGER
NCI-H2452 Growth Inhibition Assay IC50=5.45628 μM SANGER
SW1710 Growth Inhibition Assay IC50=5.42456 μM SANGER
SK-OV-3 Growth Inhibition Assay IC50=4.9934 μM SANGER
ALL-PO Growth Inhibition Assay IC50=4.83858 μM SANGER
BxPC-3 Growth Inhibition Assay IC50=4.70391 μM SANGER
RCC10RGB Growth Inhibition Assay IC50=4.29479 μM SANGER
NKM-1 Growth Inhibition Assay IC50=4.13971 μM SANGER
MHH-ES-1 Growth Inhibition Assay IC50=4.04545 μM SANGER
OE19 Growth Inhibition Assay IC50=3.96451 μM SANGER
TE-15 Growth Inhibition Assay IC50=3.95343 μM SANGER
MOLT-16 Growth Inhibition Assay IC50=3.88556 μM SANGER
A172 Growth Inhibition Assay IC50=3.75498 μM SANGER
HCC1569 Growth Inhibition Assay IC50=3.48305 μM SANGER
HOP-62 Growth Inhibition Assay IC50=3.36054 μM SANGER
A704 Growth Inhibition Assay IC50=3.0812 μM SANGER
SCC-9 Growth Inhibition Assay IC50=2.95485 μM SANGER
COLO-829 Growth Inhibition Assay IC50=2.7654 μM SANGER
RPMI-7951 Growth Inhibition Assay IC50=2.70193 μM SANGER
SK-LMS-1 Growth Inhibition Assay IC50=2.64128 μM SANGER
SNU-423 Growth Inhibition Assay IC50=2.49787 μM SANGER
NCI-H2122 Growth Inhibition Assay IC50=2.27684 μM SANGER
RS4-11 Growth Inhibition Assay IC50=1.95415 μM SANGER
HCC1395 Growth Inhibition Assay IC50=1.78273 μM SANGER
MIA-PaCa-2 Growth Inhibition Assay IC50=1.75977 μM SANGER
KYSE-180 Growth Inhibition Assay IC50=1.72788 μM SANGER
BCPAP Growth Inhibition Assay IC50=1.66898 μM SANGER
A498 Growth Inhibition Assay IC50=1.30469 μM SANGER
TYK-nu Growth Inhibition Assay IC50=1.07912 μM SANGER
D-247MG Growth Inhibition Assay IC50=0.94852 μM SANGER
S-117 Growth Inhibition Assay IC50=0.92131 μM SANGER
D-336MG Growth Inhibition Assay IC50=0.8462 μM SANGER
LOXIMVI Growth Inhibition Assay IC50=0.58832 μM SANGER
769-P Growth Inhibition Assay IC50=0.58499 μM SANGER
GCT Growth Inhibition Assay IC50=0.30672 μM SANGER
SW982 Growth Inhibition Assay IC50=0.21416 μM SANGER
ES-CCE Function Assay 5 μM 3 d DMSO Strongly induces the activity of Wnt/beta-catenin pathway 24779365
ES-D3 Function Assay 5 μM 3 d DMSO Strongly induces the activity of Wnt/beta-catenin pathway 24779365
ES-CCE Cytotoxic Assay 10 μM 3 d DMSO Induces moderate cytotoxicity 24779365
ES-D3 Cytotoxic Assay 10 μM 3 d DMSO Induces moderate cytotoxicity with IC50 of 4.9 μM 24779365
Neural progenitor cells Function Assay 3 μM 10 d DMSO Induces generation of neural progenitor cells 24638034
A549 Apoptosis Assay 5 µM 24 h DMSO Increases cell apoptosis 24367688
H157 Apoptosis Assay 5 µM 24 h DMSO Does not significantly affect apoptosis 24367688
H460 Apoptosis Assay 5 µM 24 h DMSO Attenuates cell apoptosis 24367688
H157 Growth Inhibition Assay 5 µM 24 h DMSO Promotes cell proliferation 24367688
H460 Growth Inhibition Assay 5 µM 24 h DMSO Promotes cell proliferation 24367688
embryonic stem cells (ESC) Function Assay 3 µM 11 d DMSO Promotes self-renewal of naïve-type mouse embryonic stem cells (ESC) 23843312
DN3 Function Assay 10 μM 96 h DMSO Increases cell development and proliferation 23526989
platelets Function Assay 10 μM 15 min DMSO Increases thrombin-mediated platelet aggregation and ATP secretion 23239877
hiPSC-NPs Growth Inhibition Assay 3 μM 72 h DMSO Increases cell proliferation  22642687
INS-1E Function Assay 2.5 μM 24 h DMSO Induces a reduction of NP1 overexpression 22427704
PANC1 Apoptosis Assay  5 μM 72 h DMSO Triggers an apoptotic response 22201186
Endothelial cell(EC) Function Assay 3 μM DMSO Promotes endothelial cell (EC) differentiation 22052006
HMC1.2 Growth Inhibition Assay 30 μM 72 h DMSO Reduces cell survival 22039301
Sca-1+ HPC Growth Inhibition Assay 2 μM 6 d DMSO Synergistically promotes Sca-1+ HPC proliferation and colony formation together with EGF 21624348
Oct4/Sox2/Klf4-infected MEFs Function Assay 10 μM 28 d DMSO Promotes MEFs reprogramming Transduced by Oct4, Sox2, and Klf4 19839055
H4IIE Function Assay 10 μM 24 h DMSO Regulates β-catenin activity and TIRE containing promoter activity 15350195
insulin receptor–expressing CHO-IR Function Assay 500 nM 30 min DMSO Activates Glycogen Synthase (GS) 12606497
3T3-L1 Function Assay 3 μM 4 h DMSO Inhibits preadipocyte differentiation 12055200
CHO-IR Function Assay 30 min EC50=0.77 μM 29016121
HepG2 Function Assay 3 h EC50=1.5 μM 22261023
Click to View More Cell Line Experimental Data

Biological Activity

Description Laduviglusib (CHIR-99021; CT99021) HCl is hydrochloride of CHIR-99021, which is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs Cdc2 and ERK2. CHIR-99021 is a potent pharmacological activators of the Wnt/beta-catenin signaling pathway. CHIR-99021 significantly rescues light-induced autophagy and augments GR, RORα and autophagy-related proteins.
Targets
GSK-3β [1]
(Cell-free assay)
GSK-3α [1]
(Cell-free assay)
6.7 nM 10 nM
In vitro
In vitro

CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases. Furthermore, CHIR-99021 shows only weak binding to a panel of 22 pharmacologically relevant receptors and little inhibitory activity against a panel of 23 nonkinase enzymes. CHIR-99021 induces the activation of glycogen synthase (GS) in insulin receptor-expressing CHO-IR cells with EC50 of 0.763 μM. [1] In addition to simulating the actions of insulin, inhibition of GSK-3 by CHIR-99021 (3 μM) increases free cytosolic β-catenin by 1.9-fold, mimicking the canonical Wnt signaling pathway in 3T3-L1 preadipocytes. During any of the first 3 days of differentiation, CHIR-99021 treatment inhibits the preadipocyte differentiation with IC50 of 0.3 μM by blocking induction of CCAAT/enhancer-binding protein α (C/EBPα) and peroxisome proliferator-activated receptor γ (PPARγ). [2] Unlike lithium chloride and AR-A014418, CHIR-99021 treatment does not reduce the viability of INS-1E cells even at high concentrations. Instead, CHIR-99021 robustly increases the rate of proliferation of INS-1E cells in a dose-dependent manner, and significantly inhibits INS-E cell death induced by high glucose and high palmitate in a concentration-dependent manner. CHIR-99021 promotes primary beta cell replication in isolated rat islets at concentrations as low as 1 μM, with 2-3 fold increase of cell replication at 5 μM of CHIR-99021 treatment. [3]

Kinase Assay Cell-free kinase assays
Polypropylene 96-well plates are filled with 300 μL/well buffer (50 mM tris HCl, 10 mM MgCl2, 1 mM EGTA, 1 mM dithiothreitol, 25 mM β-glycerophosphate, 1 mM NaF, 0.01% BSA, pH 7.5) containing 27 nM GSK-3α or 29 nM GSK-3β, and 0.5 μM biotin-CREB peptide substrate. Various concentrations of CHIR-99021 are added in 3.5 μL of DMSO, followed by 50 μL of ATP stock to yield a final concentration of 1 μM ATP in all cell-free assays. After incubation, triplicate 100-μL aliquots are transferred to Combiplate eight plates containing 100 μL/well 50 μM ATP and 20 mM EDTA. After 1 hour, the wells are rinsed five times with PBS, filled with 200 μL of scintillation fluid, sealed, left 30 minutes, and counted in a scintillation counter. All steps are performed at room temperature.
Cell Research Cell lines INS-1E
Concentrations Dissolved in DMSO, final concentrations ~ 20 μM
Incubation Time 1, or 4 days
Method

Cells are maintained for 24 hours in starvation medium (culture medium with only 5 mM glucose, 1% fetal calf serum). Then cells are exposed to various concentrations of CHIR-99021 for 1, or 4 days. Cell number is measured by staining of cellular DNA with CyQuant dye, which becomes fluorescent when bound to DNA. Fluorescence is measured after 30 minutes of incubation using the FLUOstar Optima reader. Cell replication is determined by BrdUrd incorporation. BrdUrd labeling solution is added to the medium for the last 4 hours before the cells are fixed using FixDenat solution and incubated with monoclonal anti-BrdUrd-POD antibodies. After substrate solution is added to each well, the light emission is measured in a microplate luminometer using the Analyst HT detection system.

Experimental Result Images Methods Biomarkers Images PMID
Western blot Cleaved PARP / CD31 / VE-Cadherin / α-SMA / vimentin CTNNB1 β-catenin 30709379
Growth inhibition assay Cell viability 22039301
Immunofluorescence SOX10 / EdU Oct3/4 28174705
In Vivo
In vivo

Oral administration of CHIR-99021 at 30 mg/kg enhances glucose metabolism in a rodent model of type 2 diabetes, with a maximal plasma glucose reduction of nearly 150 mg/dl 3-4 hours after administration, while plasma insulin remains at or below control levels. Oral administration of CHIR-99021 at 16 or 48 mg/kg 1 hour before oral glucose challenges in ZDF rats significantly improves glucose tolerance with 14% and 33% reduction in plasma glucose at 16 mg/kg and 48 mg/kg, respectively, and the higher dose of CHIR-99021 also reduces hyperglycemia before the oral glucose challenge. [1]

Animal Research Animal Models Female db/db mice or male ZDF rats with type 2 diabetes
Dosages ~48 mg/kg
Administration Orally

Chemical Information & Solubility

Molecular Weight 501.8 Formula

C22H18Cl2N8.HCl

CAS No. 1797989-42-4 SDF Download Laduviglusib (CHIR-99021) HCl SDF
Smiles CC1=CN=C(N1)C2=CN=C(N=C2C3=C(C=C(C=C3)Cl)Cl)NCCNC4=NC=C(C=C4)C#N.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (199.28 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : 1.5 mg/mL


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
I recently purchased CHIR 99021 to inject mice intraperitoneally. The data sheet says using 10% captisol for in vivo use. Is it for IP injection? Or do you have other solutions to suggest to use for in vivo IP injection of CHIR 99021?

Answer:
The formulation of 15% Captisol is for oral gavage, and S2924 CHIR-99021 (CT99021) HCl in it is a suspension. S2924 CHIR-99021 (CT99021) HCl can be dissolved in 5% DMSO+30% PEG 300+ddH2O at 24mg/ml as a clear solution for IP injection.

Question 2:
How about the half-life of this compound? If it is necessary for daily treatment when the compound is used in long-term experiment?

Answer:
Please change the culture medium each day to add the new comound in it if the duration is more than 72h.

Question 3:
What is the difference between S2924 and S1263? Which one is better for differentiation?

Answer:
S1263 is the free base format of Chir-99021, while S2924 is the HCl salt format. They have the same biological activity but are slightly different in solubility.

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