Checkpoint Kinase (Chk) Inhibitor

Checkpoint Kinase (Chk) Inhibitors (87):

Cat. No.	Product Name	Effect	Purity

HY-18174

Prexasertib	Inhibitor	99.64%
Prexasertib (LY2606368) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a K_i of 0.9 nM and an IC₅₀ of <1 nM. Prexasertib inhibits CHK2 (IC₅₀=8 nM) and RSK1 (IC₅₀=9 nM). Prexasertib causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib shows potent anti-tumor activity.

HY-10992

AZD-7762	Inhibitor	99.94%
AZD-7762 is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC₅₀ of 5 nM for Chk1.

HY-14720

Rabusertib	Inhibitor	99.98%
Rabusertib (LY2603618) is a potent and selective inhibitor of Chk1 with an IC₅₀ of 7 nM.

HY-P99032

Monalizumab	Inhibitor	99.69%
Monalizumab (IPH2201) is an 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).

HY-13946

BML-277	Inhibitor	99.67%
BML-277 is a selective checkpoint kinase 2 (Chk2) inhibitor with an IC₅₀ of 15 nM.

HY-186085

BEN-28010	Inhibitor
BEN-28010 is a selective, orally active, blood-brain barrier permeable CHK1 inhibitor with an IC₅₀ of 4.0 nM. BEN-28010 functions as a radiosensitizer, exhibits antitumor efficacy in GBM models. BEN-28010 can be used for the research of glioblastoma.

HY-180357

Graviquinone	Inhibitor
Graviquinone is a Chk1 inhibitor. Graviquinone exhibits potent cytotoxicity against various cancer cell lines. Graviquinone possesses the characteristics of bypassing ABCB1-mediated multidrug resistance, selectively damaging cancer cell DNA, and regulating the DNA damage response. Graviquinone can also enhance cytotoxicity by increasing ROS levels in cancer cells. Graviquinone can be used for cancer research.

HY-18958

CCT245737	Inhibitor	99.48%
CCT245737 (SRA737) is an orally active and seletive Chk1 inhibitor, with an IC₅₀ of 1.3 nM.

HY-15532

SCH900776	Inhibitor	99.97%
SCH900776 (MK-8776) is a potent, selective and orally bioavailable inhibitor of checkpoint kinase1 (Chk1) with an IC₅₀ of 3 nM. SCH900776 shows 50- and 500-fold selectivity over CDK2 and Chk2, respectively.

HY-157941

ART0380	Inhibitor	99.90%
ART0380 is a potent, selective and orally active ATR kinase inhibitor. ART0380 potently inhibits human ATR-ATRIP complex with an IC₅₀ of 51.7 nM. ART0380 binds the ATP pocket of the ATR-ATRIP complex, blocks ATR-dependent Chk1 serine 345 phosphorylation, and induces cell cycle disorder and DNA damage. ART0380 demonstrates potent and selective antitumor activity in preclinical models with varying types of ataxia-telangiectasia mutated (ATM) gene aberrancy. ART0380 can be used for the research of cancer, such as colorectal cancer and prostate cancer.

HY-14715B

CCT241533 hydrochloride	Inhibitor	98.55%
CCT241533 hydrochloride is a potent and selective CHK2 inhibitor with an IC₅₀ of 3 nM and a K_i of 1.16 nM.

HY-13263

CHIR-124	Inhibitor	99.05%
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.

HY-10032

PF 477736	Inhibitor	99.04%
PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of Chk1, with a K_i of 0.49 nM, it is also a Chk2 inhibitor, with a K_i of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC₅₀=8 (K_i), 10, 14, 23, 23, 25, and 39 nM, respectively). PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo.

HY-18174A

Prexasertib dihydrochloride	Inhibitor	99.73%
Prexasertib dihydrochloride (LY2606368 dihydrochloride) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a K_i of 0.9 nM and an IC₅₀ of <1 nM. Prexasertib dihydrochloride inhibits CHK2 (IC₅₀=8 nM) and RSK1 (IC₅₀=9 nM). Prexasertib dihydrochloride causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dihydrochloride shows potent anti-tumor activity.

HY-18961

PD 407824	Inhibitor	99.00%
PD 407824 is a checkpoint kinase Chk1 and WEE1 inhibitor with IC₅₀s of 47 and 97 nM, respectively. PD 407824 is a chemical BMP sensitizer and increases the sensitivity of cells to sub-threshold amounts of BMP4.

HY-107407

SB-218078	Inhibitor	98.30%
SB-218078 is a potent, selective, ATP-competitive 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.

HY-18174E

Prexasertib dimesylate	Inhibitor	98.90%
Prexasertib dimesylate (LY2606368 dimesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a K_i 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.

HY-148962

LY2880070	Inhibitor	99.9%
LY2880070 is an orally active CHK1 inhibitor, IC₅₀ ＜ 1 nM. LY2880070 can be used as an anticancer agent for combination with DNA damaging agents.

HY-112167

GDC-0575	Inhibitor	99.68%
GDC-0575 (ARRY-575, RG7741) is a highly-selective oral small-molecule Chk1 inhibitor with an IC₅₀ of 1.2 nM.

HY-18175

CCT244747	Inhibitor	99.46%
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.

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