CHIR-99021 (CT99021) HCl

Catalog No.S2924

CHIR-99021 (CT99021) HCl Chemical Structure

Molecular Weight(MW): 501.8

CHIR-99021 HCl (CT99021) 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.

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Cited by 101 Publications

Purity & Quality Control

Choose Selective GSK-3 Inhibitors

Biological Activity

Description CHIR-99021 HCl (CT99021) 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.
Targets
GSK-3β [1]
(Cell-free assay)
GSK-3α [1]
(Cell-free assay)
6.7 nM 10 nM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
3T3-L1 MVrGeY5kfGmxbjDBd5NigQ>? MlPSN{DPxE1? MV20JIg> MkexSG1UVw>? MXXJcohq[mm2czDwdoVi\Gmyb3P5eIUh\GmoZnXy[Y51cWG2aX;u M2W3NVEzODV3MkCw
insulin receptor–expressing CHO-IR NGPQSolHfW6ldHnvckBCe3OjeR?= NXT4c4J2PTByIH7N MojQN|AhdWmw NWTQSZNzTE2VTx?= M3WzVWFkfGm4YYTld{BIdHmlb3flckBUgW62aHHz[UApT1Nr Mn3vNVI3ODZ2OUe=
H4IIE MVTGeY5kfGmxbjDBd5NigQ>? M37FOlExKM7:TR?= M1v2blI1KGh? NYW4VI1LTE2VTx?= MYfS[Yd2dGG2ZYOg{tIu[2G2ZX7pckBi[3Srdnn0fUBidmRiVFnSSUBkd262YXnubY5oKHC{b33veIVzKGGldHn2bZR6 MoG4NVU{PTBzOUW=
Oct4/Sox2/Klf4-infected MEFs NWPoWJc6TnWwY4Tpc44hSXO|YYm= NV\6WG5OOTBizszN M2T4e|I5KGR? MkPYSG1UVw>? MnLRVJJwdW:2ZYOgUWVHeyC{ZYDyc4dz[W2vaX7nJHRz[W6|ZIXj[YQh[nliT3P0OEwhW2:6MjygZY5lKEuuZkS= MmOwNVk5OzlyNUW=
Sca-1+ HPC M3jKe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\mbFkzKM7:TR?= NETqS2g3KGR? NH6wNIVFVVOR MVvTfY5memerc4TpZ4FtdHlicILvcY91\XNiU3PhMVEsyqCKUFOgdJJwdGmoZYLheIlwdiCjbnSgZ49td267IH\vdo1ifGmxbjD0c4dmfGincjD3bZRpKEWJRh?= M{HNR|IyPjJ2M{S4
HMC1.2 MmLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13xbFMxKM7:TR?= NGnO[Gk4OiCq NFTyWldFVVOR M2fpcHJm\HWlZYOgZ4VtdCC|dYL2bZZidA>? MXiyNlA{QTNyMR?=
Endothelial cell(EC) NWTaRWFpTnWwY4Tpc44hSXO|YYm= M1\zSFMh|ryP M1XVTGROW09? MYTQdo9ud3SnczDlcoRwfGinbHnhcEBk\WyuIDjFR{kh\GmoZnXy[Y51cWG2aX;u NYDhNWNPOjJyNUKwNFY>
PANC1 MVHBdI9xfG:|aYOgRZN{[Xl? Ml6yxsA2KM7:TR?= M3LF[|czKGh? M2m1SGROW09? M3zwRXRzcWepZYLzJIFvKGGyb4D0c5Rq[yC{ZYPwc45{\Q>? MVGyNlIxOTF6Nh?=
INS-1E Mm\vSpVv[3Srb36gRZN{[Xl? MkH2Nk42KM7:TR?= MUeyOEBp NUHuPHozTE2VTx?= M3;6Nmlv\HWlZYOgZUBz\WS3Y4Tpc44hd2ZiTmCxJI93\XKneIDy[ZN{cW:w MUOyNlQzPzdyNB?=
hiPSC-NPs M1;KTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHydVQ{6oDLzszN M2G4WFczKGh? MYrEUXNQ M2\qUWlv[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc47DqA>? M4\nW|IzPjR{Nki3
platelets M3:zcGZ2dmO2aX;uJGF{e2G7 M33rflExKM7:TR?= MUCxOUBucW5? NF;yUXJFVVOR MnPtTY5kemWjc3XzJJRpem:vYnnuMY1m\GmjdHXkJJBt[XSnbHX0JIFo\3KnZ3H0bY9vKGGwZDDBWHAhe2WlcnX0bY9v MmDiNlMzOzl6N{e=
DN3 MoD2SpVv[3Srb36gRZN{[Xl? NEj2T5MyOCEQvF2= NYfqb5p1QTZiaB?= MXzEUXNQ NV;qdFZbUW6lcnXhd4V{KGOnbHyg[IV3\WyxcH3lcpQh[W6mIIDyc4xq\mW{YYTpc44> NFjMNZkzOzV{Nkm4PS=>
embryonic stem cells (ESC) MljkSpVv[3Srb36gRZN{[Xl? NWDYbW51OyEEtV2= NEHQ[4wyOSCm MkDySG1UVw>? M{To[HBzd22xdHXzJJNmdGZvcnXu[ZdidCCxZjDuZeOwfmVvdInw[UBud3W|ZTDlcYJzgW:waXOgd5RmdSClZXzsd{ApTVOFKR?= M37OZ|I{QDR|M{Gy
H460 Mnn4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfz[|N3PSEEtV2= NWXZWGF2OjRiaB?= NHjRb3pFVVOR NUXkSoRFWHKxbX;0[ZMh[2WubDDwdo9tcW[ncnH0bY9v M{TKeVI1OzZ5Nki4
H157 MojMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHIT5ZQPSEEtV2= MXKyOEBp MortSG1UVw>? M361VHBzd22xdHXzJINmdGxicILvcIln\XKjdHnvci=> MWCyOFM3PzZ6OB?=
H460 NYH6SohySXCxcITvd4l{KEG|c3H5 MoXaOUDDvU1? Mmn2NlQhcA>? M2m3bWROW09? MlL3RZR1\W63YYTld{Bk\WyuIHHwc5B1d3Orcx?= M2LiU|I1OzZ5Nki4
H157 M33GcmFxd3C2b4Ppd{BCe3OjeR?= Mn[zOUDDvU1? MV2yOEBp NXLEOGVTTE2VTx?= NHL2cVBFd2W|IH7veEB{cWewaX\pZ4FvfGy7IHHm[oVkfCCjcH;weI9{cXN? MV[yOFM3PzZ6OB?=
A549 Mnr4RZBweHSxc3nzJGF{e2G7 NFThVFU2KML3TR?= NI\h[VUzPCCq M3PpNWROW09? MYPJcoNz\WG|ZYOgZ4VtdCCjcH;weI9{cXN? NWLQb3FqOjR|Nke2PFg>
Neural progenitor cells MWXGeY5kfGmxbjDBd5NigQ>? NG\WW3M{KM7:TR?= MVKxNEBl MX3EUXNQ MWLJcoR2[2W|IHflcoVz[XSrb36gc4YhdmW3cnHsJJBzd2enbnn0c5Ih[2WubIO= NXX6V|Z5OjR4M{iwN|Q>
ES-D3 M1HjZmN6fG:2b4jpZ{BCe3OjeR?= NXr6OWJPOTEEoN88US=> NGS1PXo{KGR? Mn73SG1UVw>? M{TlW2lv\HWlZYOgcY9l\XKjdHWgZ5l1d3SxeHnjbZR6KHerdHigTWM2OCCxZjC0Mlkh|ryP MoLKNlQ4Pzl|NkW=
ES-CCE NHHkTGFEgXSxdH;4bYMhSXO|YYm= MkHDNVDDqM7:TR?= MUmzJIQ> MnLYSG1UVw>? NWXCeZdXUW6mdXPld{Bud2SncnH0[UBkgXSxdH;4bYNqfHl? M1ziPVI1Pzd7M{[1
ES-D3 MUDGeY5kfGmxbjDBd5NigQ>? MWO1xsDPxE1? MXqzJIQ> M2SxcmROW09? M2i5N3N1em:wZ3z5JIlv\HWlZYOgeIhmKGGldHn2bZR6KG:oIGfueE9j\XSjLXPheIVvcW5icHH0bJdigQ>? NHHXV44zPDd5OUO2OS=>
ES-CCE MmnnSpVv[3Srb36gRZN{[Xl? MYm1xsDPxE1? M{nm[VMh\A>? M3:yVGROW09? MWLTeJJwdmeueTDpcoR2[2W|IITo[UBi[3Srdnn0fUBw\iCZboSvZoV1[S2lYYTlcolvKHCjdHj3ZZk> M1vWOlI1Pzd7M{[1
SW982 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;VOmlEPTB;MD6yNVQyPiEQvF2= MVnTRW5ITVJ?
GCT M122NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nGXmlEPTB;MD6zNFY4OiEQvF2= NH7rRY1USU6JRWK=
769-P NWq3VYx{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEGzV4dKSzVyPUCuOVg1QTlizszN MXLTRW5ITVJ?
LOXIMVI MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXMTWM2OD1yLkW4PFMzKM7:TR?= MljGV2FPT0WU
D-336MG NUHsZ4hDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTBwOES2NkDPxE1? NVfWOHpXW0GQR1XS
S-117 NIjkXpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzKTWM2OD1yLkmyNVMyKM7:TR?= M2O4THNCVkeHUh?=
D-247MG NFjNU3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPXTWM2OD1yLkm0PFUzKM7:TR?= NVXYb4tMW0GQR1XS
TYK-nu M3rZfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYG5U5Y6UUN3ME2xMlA4QTF{IN88US=> NUSyR5ExW0GQR1XS
A498 Ml\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTFwM{C0Olkh|ryP NIXOVZFUSU6JRWK=
BCPAP NFW3TpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTFwNk[4PVgh|ryP Mn3OV2FPT0WU
KYSE-180 Ml;xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;xTWM2OD1zLkeyO|g5KM7:TR?= NHvTR41USU6JRWK=
MIA-PaCa-2 NHPVbmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2S5VWlEPTB;MT63OVk4PyEQvF2= MYnTRW5ITVJ?
HCC1395 NGDjVVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3MTWM2OD1zLke4Nlc{KM7:TR?= NFTUT49USU6JRWK=
RS4-11 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\pTWM2OD1zLkm1OFE2KM7:TR?= MVfTRW5ITVJ?
NCI-H2122 NE\XXlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vFUGlEPTB;Mj6yO|Y5PCEQvF2= NGDmV4dUSU6JRWK=
SNU-423 MmG0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXtTWM2OD1{LkS5O|g4KM7:TR?= M4jkT3NCVkeHUh?=
SK-LMS-1 NHf3bHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTR[XR4UUN3ME2yMlY1OTJ6IN88US=> NILSU5pUSU6JRWK=
RPMI-7951 NIjYWXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\IO3dKSzVyPUKuO|AyQTNizszN M4\zbnNCVkeHUh?=
COLO-829 NIfUOYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\OWWlEPTB;Mj63OlU1KM7:TR?= NEHHcGNUSU6JRWK=
SCC-9 NYP2ZY9qT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37MfWlEPTB;Mj65OVQ5PSEQvF2= NEL1UVhUSU6JRWK=
A704 MnPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rW[2lEPTB;Mz6wPFEzKM7:TR?= NEe1PGRUSU6JRWK=
HOP-62 NXrtSoFwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTNwM{[wOVQh|ryP M1fmSnNCVkeHUh?=
HCC1569 NYLN[|Q{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HiWWlEPTB;Mz60PFMxPSEQvF2= NIDxTY1USU6JRWK=
A172 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NID1O5JKSzVyPUOuO|U1QThizszN NH\GTmdUSU6JRWK=
MOLT-16 Mn70S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;JTWM2OD1|Lki4OVU3KM7:TR?= NXnpXnM5W0GQR1XS
TE-15 MnzIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LQZmlEPTB;Mz65OVM1OyEQvF2= MkDrV2FPT0WU
OE19 NUjWTZoxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLsbYZHUUN3ME2zMlk3PDVzIN88US=> NFTTVJFUSU6JRWK=
MHH-ES-1 NFrNSGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPyPZdKSzVyPUSuNFQ2PDVizszN NFvHUmhUSU6JRWK=
NKM-1 NV7oXJFIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{CwZmlEPTB;ND6xN|k4OSEQvF2= MnW3V2FPT0WU
RCC10RGB MkLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTRwMkm0O|kh|ryP MmfWV2FPT0WU
BxPC-3 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTRwN{CzPVEh|ryP NFXLSpRUSU6JRWK=
ALL-PO M{LHO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTVTWM2OD12LkizPFU5KM7:TR?= MmTKV2FPT0WU
SK-OV-3 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XufGlEPTB;ND65PVM1KM7:TR?= M4PjNnNCVkeHUh?=
SW1710 M3TPdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjFPY9KSzVyPUWuOFI1PTZizszN Ml3jV2FPT0WU
NCI-H2452 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfkZ5hKSzVyPUWuOFU3OjhizszN NGjrb2JUSU6JRWK=
D-392MG MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjBdJhKSzVyPUWuOFkyPDVizszN NVXJSpRkW0GQR1XS
LB2518-MEL MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\JT2lEPTB;NT63NlYzPyEQvF2= Mnq2V2FPT0WU
BL-41 NGnFTVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXEUmxKSzVyPUWuPFEzPjZizszN M3TXR3NCVkeHUh?=
WM-115 NHfmTXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnHe|NKSzVyPUWuPFE2ODlizszN MVrTRW5ITVJ?
SK-MEL-2 M2r6Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjjeHZpUUN3ME22MlM5OzR2IN88US=> M3LJU3NCVkeHUh?=
CGTH-W-1 NH[4R5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\jV49KSzVyPU[uOFE4KM7:TR?= M1zUUHNCVkeHUh?=
BB65-RCC NE\2[JRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTZwNUOxPVUh|ryP M3;EUnNCVkeHUh?=
CAL-85-1 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnuwTWM2OD14Lk[wPVM3KM7:TR?= NETHeYNUSU6JRWK=
RT-112 NGm5OVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDMTWM2OD15LkG2OFU3KM7:TR?= M3q2OHNCVkeHUh?=
MC116 Mn3uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTXTWM2OD15LkK4OlkyKM7:TR?= NVSxc3RHW0GQR1XS
G-361 NETnUnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\r[5lyUUN3ME23MlQ3PTZzIN88US=> MYTTRW5ITVJ?
SW1417 M4HWbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWflbndKUUN3ME23MlY1PTh2IN88US=> MUfTRW5ITVJ?
MV-4-11 NVrFZXJQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVe2eIRCUUN3ME24MlU1OzB2IN88US=> M2\aeXNCVkeHUh?=
CAL-72 NYHyWZR3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LW[2lEPTB;OD63OlEyOyEQvF2= MnvnV2FPT0WU
MKN28 NWrSXlRFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXqeHlKSzVyPUiuPFg2OTZizszN MofUV2FPT0WU
MEG-01 M2\KUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\IWHQyUUN3ME24Mlk6ODR|IN88US=> NVfrfIhKW0GQR1XS
ACHN MknNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjqRnZjUUN3ME25MlMxPTR4IN88US=> NIK0T|JUSU6JRWK=
NCI-H1755 MmHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHGfWgzUUN3ME25MlM6QTh4IN88US=> NXKyOHkxW0GQR1XS
NCI-H64 M2m0Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTlwNEKyOVUh|ryP MonQV2FPT0WU
COLO-205 M{\Lc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\KXJRpUUN3ME25MlQ{QDJzIN88US=> M1HTOHNCVkeHUh?=
CTV-1 M4i0VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3LPXd2UUN3ME25MlQ{QDl2IN88US=> MkS2V2FPT0WU
U-2-OS NIfzWWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXKTWM2OD17LkS1NFA3KM7:TR?= MYTTRW5ITVJ?
LB996-RCC M3rpTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjJOWU4UUN3ME25MlUzOzl5IN88US=> MUHTRW5ITVJ?
SK-N-DZ M164fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\mcIJKSzVyPUmuOlU4PDJizszN NH\m[nFUSU6JRWK=
EFM-19 M2rJNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTlwN{W1OlYh|ryP MXHTRW5ITVJ?
DBTRG-05MG NWOyWVBTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\3TWM2OD17Lke3O|ch|ryP NGPs[4lUSU6JRWK=
U-118-MG M1yzZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoG1TWM2OD17Lkm0OFQ1KM7:TR?= MorIV2FPT0WU
LB1047-RCC MmXMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4j4SGlEPTB;OT65PVc6QCEQvF2= NWH1[FJmW0GQR1XS
NCI-H28 M3T1eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmKzTWM2OD1zMD60OFE{KM7:TR?= MoLoV2FPT0WU
MZ2-MEL MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELPb|NKSzVyPUGwMlQ3PzdizszN M3\Lb3NCVkeHUh?=
M059J NXjvT3N7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTFyLk[xNFIh|ryP M4L3XHNCVkeHUh?=
HT-3 M1rzcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTFyLk[xO|kh|ryP NETONIFUSU6JRWK=
SNU-387 NX\pWnVRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXwTWM2OD1zMD63NlM2KM7:TR?= MkHlV2FPT0WU
NCI-H526 M2q5cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrLNGhKSzVyPUGxMlE{PjVizszN NWLQdGZHW0GQR1XS
HEL MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfGTo9IUUN3ME2xNU43PTd7IN88US=> NYXOWGZrW0GQR1XS
PA-1 NGfZOmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTFzLkmzJO69VQ>? MWTTRW5ITVJ?
PC-14 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTF{LkOyOEDPxE1? MnjMV2FPT0WU
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CAL-54 NIf4V|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTN2NT64O|kh|ryP MX;TRW5ITVJ?
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IST-SL2 NVS3b5NwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3VTWM2OD1|N{KuPVI3KM7:TR?= MmDrV2FPT0WU
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IST-SL1 NVfwRXhvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mkn1TWM2OD1|OUSuOFA3KM7:TR?= NGnyTHJUSU6JRWK=
TE-6 NFfKZZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fnS2lEPTB;M{m3MlI2PCEQvF2= NYLJNGEzW0GQR1XS
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MDA-MB-134-VI M2T4Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HmU2lEPTB;NEOxMlA{OyEQvF2= NVKyWmRZW0GQR1XS
RH-1 M13YTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTZTWM2OD12M{WuNFkh|ryP NGrTfFNUSU6JRWK=
AM-38 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fpTmlEPTB;NEO4MlU1KM7:TR?= NIDSe2VUSU6JRWK=
BL-70 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULQ[5B5UUN3ME20N|kvPDJ7IN88US=> MV;TRW5ITVJ?
COLO-684 M1PVbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jDbWlEPTB;NES4Mlg5QCEQvF2= NEP4WI1USU6JRWK=
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SCLC-21H MmDKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTR3NT62PVkh|ryP MXzTRW5ITVJ?
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TE-441-T MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXwTWM2OD12NUeuNVg3KM7:TR?= NXXjbYFRW0GQR1XS
A3-KAW NITpNHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTR4MD64OFEh|ryP MVXTRW5ITVJ?
NCI-H1092 NX[xNXdzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvyTWM2OD12NkOuPVQ{KM7:TR?= MV3TRW5ITVJ?
COR-L279 NWfYVFN3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfSOpVKSzVyPUS2OE45PDdizszN M3jpR3NCVkeHUh?=
NCI-SNU-5 NFy1TXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXRcGJsUUN3ME20O|IvOjhizszN M{OxeHNCVkeHUh?=
JAR MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2GyWGlEPTB;NEe0Mlc5QCEQvF2= MVXTRW5ITVJ?
NCI-H446 NEPVPVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TVPWlEPTB;NEe3MlA5KM7:TR?= NWnnXYNSW0GQR1XS
HDLM-2 M17hdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTBR49KSzVyPUS4NE45PjlizszN MYTTRW5ITVJ?
D-283MED M{PQO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTR6OD65NlQh|ryP MkfpV2FPT0WU
NCI-H1395 MkSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fweGlEPTB;NEi5MlAxPCEQvF2= M{LTT3NCVkeHUh?=
RPMI-6666 MnOxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljpTWM2OD12OUGuN|k5KM7:TR?= MorIV2FPT0WU
CPC-N MmLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jMdGlEPTB;NUCyMlA3OyEQvF2= MmXIV2FPT0WU
EC-GI-10 NH3ueVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTVyMj6xOlkh|ryP NFGyWoxUSU6JRWK=
CA46 MnPaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXDOYY4UUN3ME21NFQvPDB5IN88US=> M{LqZXNCVkeHUh?=
EHEB MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrMR4dKSzVyPUWwO{4zODhizszN MorTV2FPT0WU
RPMI-8402 NIjIO4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTVzMD6wNlEh|ryP MnP2V2FPT0WU
DU-4475 NHfqNGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7SPFFKSzVyPUWxNU4yODFizszN M{[4ZnNCVkeHUh?=
P12-ICHIKAWA M4[2TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nubmlEPTB;NUGxMlQyPiEQvF2= NFrlb5RUSU6JRWK=
NCI-H1694 NXLQelQxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1X6cWlEPTB;NUGyMlQ{QSEQvF2= MlfKV2FPT0WU
NCI-H2171 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\nTWM2OD13MUKuO|A2KM7:TR?= MULTRW5ITVJ?
Mo-T NGPlNphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoT2TWM2OD13MUWuNVE3KM7:TR?= MnyxV2FPT0WU
HL-60 NI\uSIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDBSplKSzVyPUWyNk46OjRizszN M2XJ[XNCVkeHUh?=
NCI-H1436 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrYWFZKSzVyPUWyN{4xPjRizszN MWXTRW5ITVJ?
NCI-H510A MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLpTWM2OD13MkSuOlk3KM7:TR?= NVrPV|loW0GQR1XS
NCI-H2081 NUDBb2VTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPTdmtKSzVyPUWyOU42OTNizszN MlP5V2FPT0WU
NB5 MkDJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HCTmlEPTB;NUK2MlQ{KM7:TR?= M{OyN3NCVkeHUh?=
NCI-H2227 NGLUe2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnVUZNKSzVyPUWzNE4zPTRizszN MnWxV2FPT0WU
HSC-4 Ml;YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoW1TWM2OD13M{muNlk{KM7:TR?= NH7mTWZUSU6JRWK=
RL M1HNdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTV2Mj60OFIh|ryP NEnQd5BUSU6JRWK=
EVSA-T MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfBTWM2OD13NEOuOlg1KM7:TR?= NYPxW495W0GQR1XS
NCI-H889 NXfrVlR1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknUTWM2OD13NEeuNlMh|ryP NWL3b49WW0GQR1XS
COLO-320-HSR NVTGOoJ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzUXZFKSzVyPUW1NU4{PSEQvF2= Mo\tV2FPT0WU
EW-11 M1vFV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE[4fnhKSzVyPUW1Nk4{QTlizszN MYrTRW5ITVJ?
UACC-812 NGDLWoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3n5W2lEPTB;NUW5MlM6OSEQvF2= MnzWV2FPT0WU
CAL-148 NWPNZotGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETEUndKSzVyPUW2OU4xQDlizszN MmW4V2FPT0WU
K052 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHOzVZlKSzVyPUW3PU4zOTNizszN MU\TRW5ITVJ?
L-428 NYi1O3RHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXWWHBKSzVyPU[wNE43PzFizszN NVfzeGZmW0GQR1XS
LP-1 M1:5VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;P[GZJUUN3ME22NFMvPTh5IN88US=> MXzTRW5ITVJ?
ML-2 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm[3TWM2OD14ME[uOVc6KM7:TR?= NHrudGlUSU6JRWK=
KARPAS-45 M3LBbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\nfoNxUUN3ME22NVgvOjJzIN88US=> NXjBW5FVW0GQR1XS
HT M3znZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2S5bGlEPTB;NkKyMlc5PSEQvF2= NYPIdItIW0GQR1XS
NCI-H226 NXLYOmdJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFj6ZYhKSzVyPU[yPE4{PTNizszN Ml24V2FPT0WU
L-363 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2Hx[mlEPTB;NkS4MlA3PCEQvF2= M2XKOXNCVkeHUh?=
IM-9 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3SZ4NoUUN3ME22OVEvPTRzIN88US=> M3naNXNCVkeHUh?=
TUR MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTZ5MT6zNlIh|ryP NX\KU2ZMW0GQR1XS
NCI-SNU-16 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzZSHpUUUN3ME22PFAvPDZ{IN88US=> NE\5OFlUSU6JRWK=
NCI-SNU-1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TyUWlEPTB;NkmwMlE4OiEQvF2= NW\LNVc5W0GQR1XS
U-87-MG MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTZ7ND61PFUh|ryP MkPSV2FPT0WU
KM-H2 NE\IdHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTZ7OT6wOVkh|ryP NWfxNWsxW0GQR1XS
DEL NXnQfXRHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWP3S3d4UUN3ME23NFAvQDN6IN88US=> NV;xdZp3W0GQR1XS
KARPAS-422 MnT2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nCWGlEPTB;N{i5MlMyPSEQvF2= MXrTRW5ITVJ?
BC-3 NIrvT5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHf5bGJKSzVyPUiwOU4zODNizszN NGLFdppUSU6JRWK=
NCI-H1155 NGTtZ2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknqTWM2OD16MUiuNFU6KM7:TR?= MYTTRW5ITVJ?
NCI-H1581 NHfQcnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTlyMD6yN|Eh|ryP MUfTRW5ITVJ?

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Cleaved PARP / CD31 / VE-Cadherin / α-SMA / vimentin; 

PubMed: 30709379     


NCI-H460 cells were co-cultured with HUVECs in a 3D culture system, and then treated with 1 μM CHIR-99021, 10 μM or 20 μM Cisplatin, or a combination of both, for 24 h. Cells were harvested and immunoblotted with anti-cleaved PARP, anti-CD31, anti-VE-cadherin, anti-α-SMA, anti-vimentin, and anti-β-actin antibodies. 

CTNNB1; 

PubMed: 23993102     


Treatment with the GSK3β inhibitor CHIR-99021 led to increased levels of β-catenin in RKO and HT29 (non-mutant) cells.

β-catenin; 

PubMed: 24165128     


HeLa cells were treated with 5 μm CHIR-99021 for the indicated times. The samples were analyzed by Western blot.

30709379 23993102 24165128
Growth inhibition assay
Cell viability; 

PubMed: 22039301     


HMC-1.2 cells were cultured in the absence or presence of GSK3β inhibitor (CHIR 99021, 3–30 µM) and viability cell count was assessed by trypan blue dye exclusion after 24 h, 48 h or 72 h. All data are presented as the mean ± SEM of three independent experiments conducted in triplicate. p < 0.05*, p < 0.001** p < 0.0001*** vs vehicle treated control cells.

22039301
Immunofluorescence
SOX10 / EdU; 

PubMed: 28174705     


Incorporation of EdU (white arrowheads) into SOX10+ ENS (enteric nervous system) cells with and without CHIR-99021.

Oct3/4; 

PubMed: 24779365     


Fluorescence micrographs showing the protein expression of Brachyury/Oct3/4 after a three day differentiation of ES-D3 cells with BIO (0.5 μM), SB-216763 (5 μM), CHIR-99021 (5 μM), or CHIR-98014 (1 μM). Nuclei were counterstained with DAPI (blue). The merge is shown in yellow. Original magnification 400x. Scale bar = 50 μm.

28174705 24779365
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] Administration of CHIR-99021 significantly augments hematopoietic repopulation in recipient mice transplanted with mouse or human hematopoietic stem cells (HSCs), suggesting that GSK-3 is a specific modulator of HSC activity. [4]

Protocol

Kinase Assay:

[1]

+ Expand

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:

[3]

+ Expand
  • 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.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: Female db/db mice or male ZDF rats with type 2 diabetes
  • Formulation: Formulated as solutions in 20 mM citrate-buffered 15% Captisol or as fine suspensions in 0.5% carboxymethylcellulose.
  • Dosages: ~48 mg/kg
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 93 mg/mL (185.33 mM)
Ethanol 2 mg/mL (3.98 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.
24mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 501.8
Formula

C22H18Cl2N8.HCl

CAS No. 1797989-42-4
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID