Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a potent, selective, ATP competitive CHK1 and CHK2 inhibitor, with a Ki of 0.9 nM for CHK1 and IC50s of <1 nM, 8 nM for CHK1 and CHK2, respectively. Prexasertib Mesylate Hydrate inhibits HT-29 CHK1 autophosphorylation (S296) and HT-29 CHK2 autophosphorylation (S516). Prexasertib Mesylate Hydrate shows potent anti-tumor activity, significantly abrogates the G2/M checkpoint in p53 deficient HeLa cells with an EC50 of 9 nM[1].
CBP501 Affinity Peptide is a Chk kinase inhibitor that can abrogate G2 arrest induced by DNA-damaging agents. CBP501 Affinity Peptide can be used in cancer research[1].
AZD-7762 hydrochloride is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC50 of 5 nM for Chk1.
CCT244747 is a potent, orally bioavailable and highly selective CHK1 inhibitor, with an IC50 of 7.7 nM; CCT244747 also abrogates G2 checkpoint with an IC50 of 29 nM.
A potent and selective (up to 263-fold) inhibitor of breast cancer cells with GI50 of 0.5 uM (MCF-7), via activation the aryl hydrocarbon receptor (AhR) pathway; inhibits other cell lines derived from other tumour types with GI50 of 3.2-46 uM (lung, colon, ovary, neuronal, glial, prostate, and pancreas); potently inhibits the growth of T47D, ZR-75-1, MCF-7, SKBR3, and MDA-MB-468 breast cancer cells with GI50 of 0.16-0.38 uM, induces cell cycle arrest checkpoint activation and DNA damage; binds to the AhR, induces translocation to the nucleus, activates the XRE, induces CYP1 activity, culminating in cell cycle arrest, checkpoint activation, DNA damage and cell death.
Prexasertib dihydrochloride (LY2606368 dihydrochloride) is a potent and selective ATP competitive inhibitor of the Chk1 protein kinase, with IC50s of <1 nM and 8 nM for CHK1 and CHK2, respectively, and a Ki of 0.9 nM against purified CHK1.
Monalizumab is a first-in-class immune checkpoint inhibitor targeting Natural Killer Group 2A (NKG2A). Monalizumab, a humanized anti-NKG2A blocking mAb, increases IFN-γ production, thereby promoting NK cell effector functions. Monalizumab can be used for the research of head and neck squamous cell carcinoma (HNSCC)[1][2].
PF 477736 is a potent, selective ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, 100-fold selectivity versus Chk2 (Ki, 47 nM).
CHK1-IN-7 (Compound 10c) is a potent human CHK1 inhibitor. CHK1-IN-7 shows no single agent effect, potentiates the antiproliferative effect of Gemcitabine HY-17026 in both prostate and breast cancer cell lines. CHK1-IN-7 can be used for the research of cancer[1].
AZD-7762 is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC50 of 5 nM for Chk1.
CCT241533 hydrochloride is a potent and selective CHK2 inhibitor with an IC50 of 3 nM and a Ki of 1.16 nM.
Prexasertib dimesylate (LY2606368 dimesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dimesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dimesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dimesylate shows potent anti-tumor activity[1][2].
CCT245737 is a orally active and seletive Chk1 inhibitor, with an IC50 of 1.3 nM。
CHK1-IN-3 is a Checkpoint Kinase 1 (CHK1) inhibitor with an IC50 of 0.4 nM[1].
BML-277 is a selective checkpoint kinase 2 (Chk2) inhibitor with an IC50 of 15 nM.
VRX0466617, a selective Chk2 inhibitor, inhibits the phosphorylation of Chk2 Ser 19 and Ser33-35. VRX0466617 can be used in the study of cancer[1].
GNE-900 is a an ATP-competitive, selective, and orally active ChK1 inhibitor with IC50s of 0.0011, 1.5 µM for ChKl, ChK2, respectively. GNE-900 abrogates the G2-M checkpoint, enhances DNA damage, and induces Apoptosis. gemcitabine (HY-17026) and GNE-900 administration shows anti-tumor activity[1].
CHIR-124 is a potent and selective Chk1 inhibitor with IC50 of 0.3 nM, and also potently targets PDGFR and FLT3 with IC50s of 6.6 nM and 5.8 nM.
LY2603618 is a potent and selective inhibitor of Chk1 with an IC50 of 7 nM.
GDC-0575 dihydrochloride is an orally bioavailable CHK1 inhibitor, with an IC50 of 1.2 nM, and has antitumor activity.
CHK1-IN-2 is a checkpoint kinase 1 (CHK1) inhibitor, with an IC50 of 6 nM.
SB-218078 is a potent, selective and cell-permeable checkpoint kinase 1 (Chk1) inhibitor that inhibits Chk1 phosphorylation of cdc25C with an IC50 of 15 nM. SB-218078 is less potently inhibits Cdc2 (IC50 of 250 nM) and PKC (IC50 of 1000 nM). SB-218078 causes apoptosis by DNA damage and cell cycle arrest[1][2][3].
Chk2-IN-1 (compound 1) is a potent and selective inhibitor of checkpoint kinase 2 (Chk2), with IC50s of 13.5 nM and 220.4 nM for Chk2 and Chk1, respectively. Chk2-IN-1 can elicit a strong ataxia telangiectasia mutated (ATM)-dependent Chk2-mediated radioprotection effect[1].
MRT00033659 is a potent broad-spectrum kinase inhibitor of CK1 (IC50=0.9 µM for CK1δ) and CHK1 (IC50=0.23 µM). MRT00033659, a pyrazolo-pyridine analogue, induces p53 pathway activation and E2F-1 destabilisation[1].
Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model[1].
CHK1 inhibitor is an inhibitor of CHK1.
A potent and highly selective Chk2 inhibitor with IC50 of 0.14 nM; displays greater than 100 uM for Chk1 in vitro.
SCH900776 is a potent, selective and oral inhibitor of checkpoint kinase1 (Chk1) with an IC50 of 3 nM. It shows 50- and 500-fold selectivity over CDK2 andChk2, respectively.
GDC-0425 (RG-7602) is an orally available, highly selective small molecule ChK1 inhibitor. GDC-0425 can be used for the research of various malignancies[1][2].
LY2880070 is an orally active CHK1 inhibitor. LY2880070 can be used as an anticancer agent for combination with DNA damaging agents[1].