| Cat. No. |
Product Name |
CAS No. |
Information |
| GY03968 |
SB218078
|
135897-06-2 |
A potent inhibitor of Chk1 that blocks phosphorylation of cdc25 with IC50 of 15 nM; less potently inhibits Cdc2 and PKC (IC50=250 and 1,000 nM, respectively) and causes 85% inhibition of PKD1 at 1 uM; enhances the cytotoxicity of DNA-damaging agents. |
| GY02620 |
CCT-245737
|
1489389-18-5 |
A highly potent, selective, ATP-competitive inhibitor of Chk1 with IC50 of 1.3 nM; weak inhibition on Chk2 (IC50=2440 nM); inhibits genotoxic-induced CHK1 activity (pS296 CHK1) and cell cycle arrest (pY15 CDK1) both in vitro and in human tumor xenografts; showes significant single-agent activity against a MYC-driven mouse model of B-cell lymphoma; orally active. |
| GY02560 |
CCT241533 hydrochloride
|
1431697-96-9 |
A potent and selective ATP-competitive inhibitor of CHK2 K5777:N5777with IC50 of 3 nM; shows good selectivity for CHK2 against CHK1 (IC50=180 nM) and a wider panel of kinases and with promising in vitro ADMET properties; inhibits CHK2 autophosphorylation at S516, band shift mobility changes, and HDMX degradation. |
| GY02503 |
CCT-244747
|
1404095-34-6 |
A novel, potent, highly selective, orally active, ATP competitive CHK1 inhibitor with biochemical IC50 of 8 nM; displays 75-fold selectivity against FLT3 and >1,000-fold selectivity against CHK2 and CDK1; inhibits cellular CHK1 activity (IC50=29-170nM), significantly enhances the cytotoxicity of several anticancer drugs and abrogates drug-induced S and G2 arrest in multiple tumor cell lines; enhances antitumor activity of gemcitabine and irinotecan in vivo. |
| GY07052 |
MU 380
|
2109805-78-7 |
MU 380 is a novel potent, selective CHK1 inhibitor 2 nM, >80-fold selectivity over CHK2; sensitizes a variety of tumor cell lines to hydroxyurea or gemcitabine up to 10 times; shows extended inhibitory effects in cells, and unlike SCH900776, does not undergo in vivo N-dealkylation to the significantly less selective metabolite; causes higher accumulation of DNA damage in tumor cells and subsequent enhanced cell death, and is more efficacious in the A2780 xenograft mouse model. |
| GY06980 |
Debromohymenialdisine
|
75593-17-8 |
Debromohymenialdisine is a marine sponge alkaloid that inhibits Chk1 and Chk2 with IC50 of 3 and 3.5 uM, respectively; also inhibits MAP kinase kinase 1 (IC50=881 nM), GSK3β (IC50=1.39 uM), and CDK5/p25 (IC50=9.12 uM), does not significantly affect ATM and ATR; blocks G2 arrest in cancer cells. |
| GY06979 |
PD-321852
|
622856-21-7 |
PD-321852 is a potent, reasonably selective Chk1 inhibitor with cell IC50 of 5 nM; potentiates gemcitabine-induced clonogenic death in a panel of pancreatic cancer cell lines; inhibits gemcitabine-induced Rad51 focus formation, and depletes RAD51 proteins in pancreatic cancer cells. |
| GY05347 |
GDC-0575
|
1196541-47-5 |
GDC-0575 (ARRY-575, RG-7741) is a potent, selective and orally bioavailable Chk1 inhibitor with IC50 of 1.2 nM; enhances the killing of primary AML cells ex vivo by inducing apoptosis combined with AraC, blocks the activation of CHK1 induced by AraC via decrease in the level of Tyr15-phosphorylated CDK2 at 100 nM in AML cells. |
| GY02328 |
CCT241533
|
1262849-73-9 |
A potent and selective ATP-competitive inhibitor of CHK2 K5777:N5777with IC50 of 3 nM; shows good selectivity for CHK2 against CHK1 (IC50=180 nM) and a wider panel of kinases and with promising in vitro ADMET properties; inhibits CHK2 autophosphorylation at S516, band shift mobility changes, and HDMX degradation. |
| GY02281 |
Prexasertib dihydrochloride
|
1234015-54-3 |
A potent, selective, ATP-competitive inhibitor of CHK1 with Ki of 0.9 nM; potently abrogates the G2-M checkpoint activated by doxorubicin in p53-deficient HeLa cells with EC50 of 9 nM; causes replication catastrophe in vitro and in vivo; shows significant tumor growth inhibition in xenograft tumor models. |
$ USD
Select Your Country or Region
