GSK269962A HCl

Synonyms: GSK269962B, GSK269962

GSK269962A HCl is a selective ROCK(Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively.

GSK269962A HCl Chemical Structure

GSK269962A HCl Chemical Structure

CAS: 2095432-71-4

Selleck's GSK269962A HCl has been cited by 6 publications

Purity & Quality Control

Batch: Purity: 99.59%
99.59

GSK269962A HCl Related Products

Signaling Pathway

Choose Selective ROCK Inhibitors

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-H1581 Growth inhibition assay Inhibition of human NCI-H1581 cell growth in a cell viability assay, IC50=18.8477 μM SANGER
NCI-H1694 Growth inhibition assay Inhibition of human NCI-H1694 cell growth in a cell viability assay, IC50=24.8749 μM SANGER
NCI-H1963 Growth inhibition assay Inhibition of human NCI-H1963 cell growth in a cell viability assay, IC50=1.27839 μM SANGER
NCI-H2081 Growth inhibition assay Inhibition of human NCI-H2081 cell growth in a cell viability assay, IC50=34.6044 μM SANGER
NCI-H209 Growth inhibition assay Inhibition of human NCI-H209 cell growth in a cell viability assay, IC50=22.6272 μM SANGER
NCI-H2107 Growth inhibition assay Inhibition of human NCI-H2107 cell growth in a cell viability assay, IC50=25.6561 μM SANGER
NCI-H2126 Growth inhibition assay Inhibition of human NCI-H2126 cell growth in a cell viability assay, IC50=6.50426 μM SANGER
NCI-H2171 Growth inhibition assay Inhibition of human NCI-H2171 cell growth in a cell viability assay, IC50=0.95937 μM SANGER
NCI-H2227 Growth inhibition assay Inhibition of human NCI-H2227 cell growth in a cell viability assay, IC50=7.88616 μM SANGER
NCI-H524 Growth inhibition assay Inhibition of human NCI-H524 cell growth in a cell viability assay, IC50=22.8763 μM SANGER
NCI-H526 Growth inhibition assay Inhibition of human NCI-H526 cell growth in a cell viability assay, IC50=18.5431 μM SANGER
NCI-H720 Growth inhibition assay Inhibition of human NCI-H720 cell growth in a cell viability assay, IC50=2.45161 μM SANGER
NMC-G1 Growth inhibition assay Inhibition of human NMC-G1 cell growth in a cell viability assay, IC50=15.0578 μM SANGER
NOS-1 cell Growth inhibition assay Inhibition of human NOS-1 cell growth in a cell viability assay, IC50=5.82294 μM SANGER
OCI-AML2 cell Growth inhibition assay Inhibition of human OCI-AML2 cell growth in a cell viability assay, IC50=10.9496 μM SANGER
OCUB-M cell Growth inhibition assay Inhibition of human OCUB-M cell growth in a cell viability assay, IC50=17.201 μM SANGER
ONS-76 cell Growth inhibition assay Inhibition of human ONS-76 cell growth in a cell viability assay, IC50=13.9191 μM SANGER
OS-RC-2 cell Growth inhibition assay Inhibition of human OS-RC-2 cell growth in a cell viability assay, IC50=46.195 μM SANGER
OVCAR-4 cell Growth inhibition assay Inhibition of human OVCAR-4 cell growth in a cell viability assay, IC50=8.71808 μM SANGER
P30-OHK cell Growth inhibition assay Inhibition of human P30-OHK cell growth in a cell viability assay, IC50=7.62877 μM SANGER
P30-OHK cell Growth inhibition assay Inhibition of human PF-382 cell growth in a cell viability assay, IC50=7.04954 μM SANGER
PSN1 cell Growth inhibition assay Inhibition of human PSN1 cell growth in a cell viability assay, IC50=6.22126 μM SANGER
QIMR-WIL cell Growth inhibition assay Inhibition of human QIMR-WIL cell growth in a cell viability assay, IC50=0.49004 μM SANGER
RCC10RGB cell Growth inhibition assay Inhibition of human RCC10RGB cell growth in a cell viability assay, IC50=18.9036 μM SANGER
RKO cell Growth inhibition assay Inhibition of human RKO cell growth in a cell viability assay, IC50=10.5662 μM SANGER
RL95-2 cell Growth inhibition assay Inhibition of human RL95-2 cell growth in a cell viability assay, IC50=10.67 μM SANGER
RPMI-6666 cell Growth inhibition assay Inhibition of human RPMI-6666 cell growth in a cell viability assay, IC50=18.5236 μM SANGER
RPMI-8402 cell Growth inhibition assay Inhibition of human RPMI-8402 cell growth in a cell viability assay, IC50=4.5856 μM SANGER
RXF393 cell Growth inhibition assay Inhibition of human RXF393 cell growth in a cell viability assay, IC50=0.393 μM SANGER
Ramos-2G6-4C10 cell Growth inhibition assay Inhibition of human Ramos-2G6-4C10 cell growth in a cell viability assay, IC50=1.357 μM SANGER
SCLC-21H cell Growth inhibition assay Inhibition of human SCLC-21H cell growth in a cell viability assay, IC50=7.61149 μM SANGER
SF126 cell Growth inhibition assay Inhibition of human SF126 cell growth in a cell viability assay, IC50=11.8321μM SANGER
SF268 cell Growth inhibition assay Inhibition of human SF268 cell growth in a cell viability assay, IC50=6.23183 μM SANGER
SF539 cell Growth inhibition assay Inhibition of human SF539 cell growth in a cell viability assay, IC50=1.28661 μM SANGER
SH-4 cell Growth inhibition assay Inhibition of human SH-4 cell growth in a cell viability assay, IC50=5.75508 μM SANGER
SIG-M5 cell Growth inhibition assay Inhibition of human SIG-M5 cell growth in a cell viability assay, IC50=11.7259 μM SANGER
SJSA-1 cell Growth inhibition assay Inhibition of human SJSA-1 cell growth in a cell viability assay, IC50=1.04526 μM SANGER
SK-LMS-1 cell Growth inhibition assay Inhibition of human SK-LMS-1 cell growth in a cell viability assay, IC50=32.5965 μM SANGER
SK-MM-2 cell Growth inhibition assay Inhibition of human SK-MM-2 cell growth in a cell viability assay, IC50=42.3405 μM SANGER
SK-N-DZ cell Growth inhibition assay Inhibition of human SK-N-DZ cell growth in a cell viability assay, IC50=9.48314 μM SANGER
SK-NEP-1 cell Growth inhibition assay Inhibition of human SK-NEP-1 cell growth in a cell viability assay, IC50=17.5456 μM SANGER
SK-PN-DW cell Growth inhibition assay Inhibition of human SK-PN-DW cell growth in a cell viability assay, IC50=24.9736 μM SANGER
SNB75 cell Growth inhibition assay Inhibition of human SNB75 cell growth in a cell viability assay, IC50=8.07737 μM SANGER
SR cell Growth inhibition assay Inhibition of human SR cell growth in a cell viability assay, IC50=0.000137 μM SANGER
SU-DHL-1 cell Growth inhibition assay Inhibition of human SU-DHL-1 cell growth in a cell viability assay, IC50=12.7336 μM SANGER
SW684 cell Growth inhibition assay Inhibition of human SW684 cell growth in a cell viability assay, IC50=39.011 μM SANGER
SW872 cell Growth inhibition assay Inhibition of human SW872 cell growth in a cell viability assay, IC50=0.88656 μM SANGER
SW962 cell Growth inhibition assay Inhibition of human SW962 cell growth in a cell viability assay, IC50=12.7521 μM SANGER
697 cell Growth inhibition assay Inhibition of human 697 cell growth in a cell viability assay, IC50=0.2991 μM SANGER
8-MG-BA cell Growth inhibition assay Inhibition of human 8-MG-BA cell growth in a cell viability assay, IC50=23.0793 μM SANGER
A101D cell Growth inhibition assay Inhibition of human A101D cell growth in a cell viability assay, IC50=1.87034 μM SANGER
ACN cell Growth inhibition assay Inhibition of human ACN cell growth in a cell viability assay, IC50=21.4387 μM SANGER
AM-38 cell Growth inhibition assay Inhibition of human AM-38 cell growth in a cell viability assay, IC50=7.26327 μM SANGER
ATN-1 cell Growth inhibition assay Inhibition of human ATN-1 cell growth in a cell viability assay, IC50=24.7555 μM SANGER
BB30-HNC cell Growth inhibition assay Inhibition of human BB30-HNC cell growth in a cell viability assay, IC50=22.2532 μM SANGER
BB49-HNC cell Growth inhibition assay Inhibition of human BB49-HNC cell growth in a cell viability assay, IC50=0.00789 μM SANGER
human BC-1 cell Growth inhibition assay Inhibition of human BC-1 cell growth in a cell viability assay, IC50=3.97107 μM SANGER
BE-13 cell Growth inhibition assay Inhibition of human BE-13 cell growth in a cell viability assay, IC50=0.14081μM SANGER
BL-70 cell Growth inhibition assay Inhibition of human BL-70 cell growth in a cell viability assay, IC50=3.40703 μM SANGER
BV-173 cell Growth inhibition assay Inhibition of human BV-173 cell growth in a cell viability assay, IC50=18.8859 μM SANGER
Becker cell Growth inhibition assay Inhibition of human Becker cell growth in a cell viability assay, IC50=13.9545 μM SANGER
CAL-148 cell Growth inhibition assay Inhibition of human CAL-148 cell growth in a cell viability assay, IC50=35.6557 μM SANGER
TE-10 cell Growth inhibition assay Inhibition of human TE-10 cell growth in a cell viability assay, IC50=22.8423 μM SANGER
TE-12 cell Growth inhibition assay Inhibition of human TE-12 cell growth in a cell viability assay, IC50=32.4114 μM SANGER
TE-8 cell Growth inhibition assay Inhibition of human TE-8 cell growth in a cell viability assay, IC50=11.6089 μM SANGER
TE-9 cell Growth inhibition assay Inhibition of human TE-9 cell growth in a cell viability assay, IC50=36.6381 μM SANGER
TGW cell Growth inhibition assay Inhibition of human TGW cell growth in a cell viability assay, IC50=23.3577 μM SANGER
UACC-257 cell Growth inhibition assay Inhibition of human UACC-257 cell growth in a cell viability assay, IC50=8.70625 μM SANGER
WSU-NHL cell Growth inhibition assay Inhibition of human WSU-NHL cell growth in a cell viability assay, IC50=27.1907 μM SANGER
no-10 cell Growth inhibition assay Inhibition of human no-10 cell growth in a cell viability assay, IC50=0.66846 μM SANGER
no-11 cell Growth inhibition assay Inhibition of human no-11 cell growth in a cell viability assay, IC50=47.0263 μM SANGER
CAS-1 cell Growth inhibition assay Inhibition of human CAS-1 cell growth in a cell viability assay, IC50=0.847 μM SANGER
CCRF-CEM cell Growth inhibition assay Inhibition of human CCRF-CEM cell growth in a cell viability assay, IC50=8.65392 μM SANGER
CMK cell Growth inhibition assay Inhibition of human CMK cell growth in a cell viability assay, IC50=1.01323 μM SANGER
COLO-829 cell Growth inhibition assay Inhibition of human COLO-829 cell growth in a cell viability assay, IC50=3.24226 μM SANGER
COR-L279 cell Growth inhibition assay Inhibition of human COR-L279 cell growth in a cell viability assay, IC50=2.0738 μM SANGER
CP66-MEL cell Growth inhibition assay Inhibition of human CP66-MEL cell growth in a cell viability assay, IC50=36.5497 μM SANGER
CRO-AP2 cell Growth inhibition assay Inhibition of human CRO-AP2 cell growth in a cell viability assay, IC50=2.36088 μM SANGER
CTV-1 cell Growth inhibition assay Inhibition of human CTV-1 cell growth in a cell viability assay, IC50=23.9145 μM SANGER
Calu-6 cell Growth inhibition assay Inhibition of human Calu-6 cell growth in a cell viability assay, IC50=47.586 μM SANGER
D-247MG cell Growth inhibition assay Inhibition of human D-247MG cell growth in a cell viability assay, IC50=0.62814 μM SANGER
D-263MG cell Growth inhibition assay Inhibition of human D-263MG cell growth in a cell viability assay, IC50=0.08509 μM SANGER
D-336MG cell Growth inhibition assay Inhibition of human D-336MG cell growth in a cell viability assay, IC50=0.62854 μM SANGER
D-392MG cell Growth inhibition assay Inhibition of human D-392MG cell growth in a cell viability assay, IC50=1.43039 μM SANGER
D-502MG cell Growth inhibition assay Inhibition of human D-502MG cell growth in a cell viability assay, IC50=8.53492 μM SANGER
D-542MG cell Growth inhibition assay Inhibition of human D-542MG cell growth in a cell viability assay, IC50=12.3152 μM SANGER
DB cell Growth inhibition assay Inhibition of human DB cell growth in a cell viability assay, IC50=47.1417 μM SANGER
DEL cell Growth inhibition assay Inhibition of human DEL cell growth in a cell viability assay, IC50=7.01898 μM SANGER
DMS-114 cell Growth inhibition assay Inhibition of human DMS-114 cell growth in a cell viability assay, IC50=49.8468 μM SANGER
DMS-153 cell Growth inhibition assay Inhibition of human DMS-153 cell growth in a cell viability assay, IC50=42.9923 μM SANGER
DOHH-2 cell Growth inhibition assay Inhibition of human DOHH-2 cell growth in a cell viability assay, IC50=4.22764 μM SANGER
DSH1 cell Growth inhibition assay Inhibition of human DSH1 cell growth in a cell viability assay, IC50=8.43623 μM SANGER
Daudi cell Growth inhibition assay Inhibition of human Daudi cell growth in a cell viability assay, IC50=2.09802 μM SANGER
EC-GI-10 cell Growth inhibition assay Inhibition of human EC-GI-10 cell growth in a cell viability assay, IC50=44.2589 μM SANGER
ECC4 cell Growth inhibition assay Inhibition of human ECC4 cell growth in a cell viability assay, IC50=32.1896 μM SANGER
EM-2 cell Growth inhibition assay Inhibition of human EM-2 cell growth in a cell viability assay, IC50=2.45594 μM SANGER
ES1 cell Growth inhibition assay Inhibition of human ES1 cell growth in a cell viability assay, IC50=5.54087 μM SANGER
ES3 cell Growth inhibition assay Inhibition of human ES3 cell growth in a cell viability assay, IC50=42.4729 μM SANGER
ES4 cell Growth inhibition assay Inhibition of human ES4 cell growth in a cell viability assay, IC50=35.195 μM SANGER
ES6 cell Growth inhibition assay Inhibition of human ES6 cell growth in a cell viability assay, IC50=0.24733 μM SANGER
ES7 cell Growth inhibition assay Inhibition of human ES7 cell growth in a cell viability assay, IC50=5.23124 μM SANGER
ES8 cell Growth inhibition assay Inhibition of human ES8 cell growth in a cell viability assay, IC50=0.81924 μM SANGER
EW-18 cell Growth inhibition assay Inhibition of human EW-18 cell growth in a cell viability assay, IC50=13.6759 μM SANGER
EW-22 cell Growth inhibition assay Inhibition of human EW-22 cell growth in a cell viability assay, IC50=47.7947 μM SANGER
GCIY cell Growth inhibition assay Inhibition of human GCIY cell growth in a cell viability assay, IC50=9.80389 μM SANGER
GDM-1 cell Growth inhibition assay Inhibition of human GDM-1 cell growth in a cell viability assay, IC50=8.39196 μM SANGER
GI-1 cell Growth inhibition assay Inhibition of human GI-1 cell growth in a cell viability assay, IC50=0.00523 μM SANGER
GI-ME-N cell Growth inhibition assay Inhibition of human GI-ME-N cell growth in a cell viability assay, IC50=0.04951 μM SANGER
GR-ST cell Growth inhibition assay Inhibition of human GR-ST cell growth in a cell viability assay, IC50=13.7902 μM SANGER
GT3TKB cell Growth inhibition assay Inhibition of human GT3TKB cell growth in a cell viability assay, IC50=1.60389 μM SANGER
HAL-01 cell Growth inhibition assay Inhibition of human HAL-01 cell growth in a cell viability assay, IC50=6.69712 μM SANGER
HCC1599 cell Growth inhibition assay Inhibition of human HCC1599 cell growth in a cell viability assay, IC50=37.6011 μM SANGER
HCC2218 cell Growth inhibition assay Inhibition of human HCC2218 cell growth in a cell viability assay, IC50=13.3834 μM SANGER
HD-MY-Z cell Growth inhibition assay Inhibition of human HD-MY-Z cell growth in a cell viability assay, IC50=25.2146 μM SANGER
HL-60 cell Growth inhibition assay Inhibition of human HL-60 cell growth in a cell viability assay, IC50=12.2114 μM SANGER
HOP-62 cell Growth inhibition assay Inhibition of human HOP-62 cell growth in a cell viability assay, IC50=23.9527 μM SANGER
HT cell Growth inhibition assay Inhibition of human HT cell growth in a cell viability assay, IC50=4.44321 μM SANGER
HT-144 cell Growth inhibition assay Inhibition of human HT-144 cell growth in a cell viability assay, IC50=4.90686 μM SANGER
HUTU-80 cell Growth inhibition assay Inhibition of human HUTU-80 cell growth in a cell viability assay, IC50=3.78986 μM SANGER
IST-MEL1 cell Growth inhibition assay Inhibition of human IST-MEL1 cell growth in a cell viability assay, IC50=32.9086 μM SANGER
IST-SL1 cell Growth inhibition assay Inhibition of human IST-SL1 cell growth in a cell viability assay, IC50=2.17079 μM SANGER
IST-SL2 cell Growth inhibition assay Inhibition of human IST-SL2 cell growth in a cell viability assay, IC50=3.26608 μM SANGER
K052 cell Growth inhibition assay Inhibition of human K052 cell growth in a cell viability assay, IC50=0.75301 μM SANGER
K5 cell Growth inhibition assay Inhibition of human K5 cell growth in a cell viability assay, IC50=33.5915 μM SANGER
KALS-1 cell Growth inhibition assay Inhibition of human KALS-1 cell growth in a cell viability assay, IC50=29.3969 μM SANGER
KARPAS-422 cell Growth inhibition assay Inhibition of human KARPAS-422 cell growth in a cell viability assay, IC50=42.9142 μM SANGER
KARPAS-45 cell Growth inhibition assay Inhibition of human KARPAS-45 cell growth in a cell viability assay, IC50=4.11247 μM SANGER
KE-37 cell Growth inhibition assay Inhibition of human KE-37 cell growth in a cell viability assay, IC50=9.835 μM SANGER
KG-1 cell Growth inhibition assay Inhibition of human KG-1 cell growth in a cell viability assay, IC50=23.9757 μM SANGER
KGN cell Growth inhibition assay Inhibition of human KGN cell growth in a cell viability assay, IC50=0.56742 μM SANGER
KM12 cell Growth inhibition assay Inhibition of human KM12 cell growth in a cell viability assay, IC50=3.52964 μM SANGER
KMOE-2 cell Growth inhibition assay Inhibition of human KMOE-2 cell growth in a cell viability assay, IC50=30.4549 μM SANGER
KNS-42 cell Growth inhibition assay Inhibition of human KNS-42 cell growth in a cell viability assay, IC50=8.81915 μM SANGER
KNS-81-FD cell Growth inhibition assay Inhibition of human KNS-81-FD cell growth in a cell viability assay, IC50=37.426 μM SANGER
KS-1 cell Growth inhibition assay Inhibition of human KS-1 cell growth in a cell viability assay, IC50=0.0046 μM SANGER
KU812 cell Growth inhibition assay Inhibition of human KU812 cell growth in a cell viability assay, IC50=23.484 μM SANGER
L-540 cell Growth inhibition assay Inhibition of human L-540 cell growth in a cell viability assay, IC50=20.7445 μM SANGER
LAMA-84 cell Growth inhibition assay Inhibition of human LAMA-84 cell growth in a cell viability assay, IC50=13.6742 μM SANGER
LB1047-RCC cell Growth inhibition assay Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50=28.3883 μM SANGER
LB2241-RCC cell Growth inhibition assay Inhibition of human LB2241-RCC cell growth in a cell viability assay, IC50=10.5536 μM SANGER
LB2518-MEL cell Growth inhibition assay Inhibition of human LB2518-MEL cell growth in a cell viability assay, IC50=1.71496μM SANGER
LB831-BLC cell Growth inhibition assay Inhibition of human LB831-BLC cell growth in a cell viability assay, IC50=11.1726 μM SANGER
LB996-RCC cell Growth inhibition assay Inhibition of human LB996-RCC cell growth in a cell viability assay, IC50=12.7431 μM SANGER
LC4-1 cell Growth inhibition assay Inhibition of human LC4-1 cell growth in a cell viability assay, IC50=32.8341 μM SANGER
LOUCY cell Growth inhibition assay Inhibition of human LOUCY cell growth in a cell viability assay, IC50=1.15276 μM SANGER
LOXIMVI cell Growth inhibition assay Inhibition of human LOXIMVI cell growth in a cell viability assay, IC50=30.2122 μM SANGER
LS-123 cell Growth inhibition assay Inhibition of human LS-123 cell growth in a cell viability assay, IC50=39.2258 μM SANGER
LU-134-A cell Growth inhibition assay Inhibition of human LU-134-A cell growth in a cell viability assay, IC50=7.14068 μM SANGER
LU-139 cell Growth inhibition assay Inhibition of human LU-139 cell growth in a cell viability assay, IC50=22.218 μM SANGER
LXF-289 cell Growth inhibition assay Inhibition of human LXF-289 cell growth in a cell viability assay, IC50=17.4351μM SANGER
MC116 cell Growth inhibition assay Inhibition of human MC116 cell growth in a cell viability assay, IC50=45.0841 μM SANGER
MDA-MB-134-VI cell Growth inhibition assay Inhibition of human MDA-MB-134-VI cell growth in a cell viability assay, IC50=39.2486 μM SANGER
MFH-ino cell Growth inhibition assay Inhibition of human MFH-ino cell growth in a cell viability assay, IC50=0.64383 μM SANGER
MHH-NB-11 cell Growth inhibition assay Inhibition of human MHH-NB-11 cell growth in a cell viability assay, IC50=0.0669 μM SANGER
ML-2 cell Growth inhibition assay Inhibition of human ML-2 cell growth in a cell viability assay, IC50=3.40304 μM SANGER
MOLT-13 cell Growth inhibition assay Inhibition of human MOLT-13 cell growth in a cell viability assay, IC50=4.43653 μM SANGER
MOLT-16 cell Growth inhibition assay Inhibition of human MOLT-16 cell growth in a cell viability assay, IC50=4.11163 μM SANGER
MOLT-4 cell Growth inhibition assay Inhibition of human MOLT-4 cell growth in a cell viability assay, IC50=14.4124 μM SANGER
MPP-89 cell Growth inhibition assay Inhibition of human MPP-89 cell growth in a cell viability assay, IC50=1.25922 μM SANGER
MRK-nu-1 cell Growth inhibition assay Inhibition of human MRK-nu-1 cell growth in a cell viability assay, IC50=0.57572 μM SANGER
MSTO-211H cell Growth inhibition assay Inhibition of human MSTO-211H cell growth in a cell viability assay, IC50=12.869 μM SANGER
MV-4-11 cell Growth inhibition assay Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50=0.13915 μM SANGER
NALM-6 cell Growth inhibition assay Inhibition of human NALM-6 cell growth in a cell viability assay, IC50=1.56109 μM SANGER
NB1 cell Growth inhibition assay Inhibition of human NB1 cell growth in a cell viability assay, IC50=3.84369 μM SANGER
NB10 cell Growth inhibition assay Inhibition of human NB10 cell growth in a cell viability assay, IC50=0.13915 μM SANGER
NB12 cell Growth inhibition assay Inhibition of human NB12 cell growth in a cell viability assay, IC50=16.5656 μM SANGER
NB13 cell Growth inhibition assay Inhibition of human NB13 cell growth in a cell viability assay, IC50=2.31278 μM SANGER
NB17 cell Growth inhibition assay Inhibition of human NB17 cell growth in a cell viability assay, IC50=3.58051 μM SANGER
NB6 cell Growth inhibition assay Inhibition of human NB6 cell growth in a cell viability assay, IC50=0.59114 μM SANGER
NCCIT cell Growth inhibition assay Inhibition of human NCCIT cell growth in a cell viability assay, IC50=41.8453 μM SANGER
NCI-H1155 cell Growth inhibition assay Inhibition of human NCI-H1155 cell growth in a cell viability assay, IC50=14.3408 μM SANGER
NCI-H1304 cell Growth inhibition assay Inhibition of human NCI-H1304 cell growth in a cell viability assay, IC50=11.8982 μM SANGER
NCI-H1355 cell Growth inhibition assay Inhibition of human NCI-H1355 cell growth in a cell viability assay, IC50=4.9411 μM SANGER
NCI-H1395 cell Growth inhibition assay Inhibition of human NCI-H1395 cell growth in a cell viability assay, IC50=22.8795 μM SANGER
NCI-H1417 cell Growth inhibition assay Inhibition of human NCI-H1417 cell growth in a cell viability assay, IC50=5.67522 μM SANGER
NCI-H1436 cell Growth inhibition assay Inhibition of human NCI-H1436 cell growth in a cell viability assay, IC50=3.84101 μM SANGER
NTERA-S-cl-D1 cell Growth inhibition assay Inhibition of human NTERA-S-cl-D1 cell growth in a cell viability assay, IC50=12.8935 μM SANGER
JiyoyeP-2003 cell Growth inhibition assay Inhibition of human JiyoyeP-2003 cell growth in a cell viability assay, IC50=36.6284 μM SANGER
Click to View More Cell Line Experimental Data

Biological Activity

Description GSK269962A HCl is a selective ROCK(Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively.
Targets
ROCK1 [1]
(Cell-free assay)
ROCK2 [1]
(Cell-free assay)
MSK1 [1]
(Cell-free assay)
RSK1 [1]
(Cell-free assay)
1.6 nM 4 nM 49 nM 132 nM
In vitro
In vitro GSK269962A completely abolished the actin stress fiber formation induced by angiotensin II in human smooth muscles. Such suppressive effect on actin fiber formation was observed beginning at around 1 μM GSK269962A. GSK269962A induced vasorelaxation in preconstricted rat aorta(tissue baths) with an IC50 of 35 nM. the relaxation induced by GSK269962A is reversible. GSK269962A suppressed IL-6 mRNA transcription and reduced LPS-induced IL-6 and TNF-α protein production in macrophages[1].
Cell Research Cell lines Human primary smooth muscle cells
Concentrations 3 μM
Incubation Time 150 min
Method Human primary smooth muscle cells were serum-starved(cells were grown on coverslips, and at approximately 50% confluence, they were serum-starved overnight) and stimulated with AngII (100 nM) for 2 h. ROCK inhibitors (3 μM for SB-772077-B or GSK269962A) were added 30 min before AngII stimulation, and cells were fixed and stained with rhodamine phalloidin. Confocal images of actin stain were obtained.
In Vivo
In vivo Oral administration of GSK269962A produced a profound dose-dependent reduction of systemic blood pressure in spontaneously hypertensive rats. The reduction of blood pressure was acute and substantial. The maximal effect on blood pressure was observed approximately 2 h after oral gavages. The reduction of blood pressure was accompanied by an acute, dose-dependent increase in heart rate, presumably due to the activation of baroreflex mechanism[1]. ROCK inhibition with the use of GSK 269962 in the 10 mg/kg dose, in turn, triggered an increase in VV(voided volume), PVR(post-void residual), VT(volume threshold), VE(voiding efficiency), ICI(intercontraction interval), BC(bladder compliance), and VTNVC(volume threshold to elicit NVC). The inhibition of the ROCK pathway through GSK 269962 appeared to have no effect on either HR(heart rate), SBP(systolic blood pressure), MBP(systolic blood pressure), or DBP(diastolic blood pressure)[2]. NVC:nonvoiding contractions.
Animal Research Animal Models female Wistar rats
Dosages 5 or 10 mg/kg
Administration intra-arterially

Chemical Information & Solubility

Molecular Weight 607.06 Formula

C29H30N8O5.HCl

CAS No. 2095432-71-4 SDF Download GSK269962A HCl SDF
Smiles CCN1C2=CC(=NC=C2N=C1C3=NON=C3N)OC4=CC=CC(=C4)NC(=O)C5=CC=C(C=C5)OCCN6CCOCC6.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (164.72 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 28 mg/mL

Water : Insoluble


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In vivo
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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. )

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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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