chk1 inhibitor

CHK1 inhibitor (GDC-0575 analog) functions as a CHK1 inhibitor.

Prexasertib (LY2606368) is a selective checkpoint kinase 1 (CHK1) inhibitor (Ki 0.9 nM, IC50<1 nM). Prexasertib causes double-stranded DNA breaks and replication mutations, leading to apoptosis. Prexasertib has antitumor activity.

Gartisertib (VX-803) is an orally active and selective Rad3-related protein (ATR) inhibitor with antitumor activity, inhibiting the antiproliferative effect induced in ccRCC cells, and inhibiting ATR-driven phosphorylation of checkpoint kinase 1 (Chk1), useful for studying solid tumors.

CCB02 is a selective CPAP-tubulin interaction inhibitor (IC50: 689 nM) with anti-tumor activity, showing no inhibition on cell cycle- and centrosome-related kinases, nor affecting the phosphorylation status of Aurora-A, CDK2, Plk1, Plk2, and CHK1.

CHK1-IN-3 is an inhibitor of checkpoint kinase 1 (CHK1; IC50: 0.4 nM).

CHK1-IN-4 hydrochloride is a potent inhibitor of checkpoint kinase 1 (chk1). CHK1-IN-4 hydrochloride potently inhibits chk1 phosphorylation in the tumor cells. CHK1-IN-4 hydrochloride has anti-tumor activity.

CHK-IN-1 is a dual inhibitor of CHK1 and CHK2 with antiproliferative activity.

GDC-0425 (RG-7602) is an orally administered, selective small molecule inhibitor of checkpoint kinase 1 (ChK1), used in research on various malignancies [1] [2].

SCH900776 (MK-8776) is an agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activities.

AZD-7762, an effective and specific inhibitor of Chk1(IC50=5 nM), is equally potent against Chk2 and less potent against CAM, Yes, Fyn, Lyn, Hck and Lck.

CCT245737 is an orally active, selective Chk1 inhibitor with an IC50 of 1.3 nM, and is >1,000-fold selective over CHK2 and CDK1.

Tuvusertib (M1774) is an orally available ataxia telangiectasia and Rad3-related (ATR) kinase inhibitor (Ki< 1 µΜ) with selective and potentially antitumor activity.Tuvusertib selectively inhibits ATR activity and blocks downstream phosphorylation of serine threonine protein kinase checkpoint kinase 1 (CHK1), thereby inhibits DNA damage checkpoint activation, disrupting DNA damage repair and inducing apoptosis in tumor cells.

CHK1-IN-2 is an inhibitor of checkpoint kinase 1 (CHK1; IC50: 6 nM).

CHK1-IN-4 is a potent inhibitor of checkpoint kinase 1 (chk1) and potently inhibits chk1 phosphorylation in the tumor cells with anti-tumor activity.

MBM-55 is an effective inhibitor of NIMA related kinase 2 (NEK2) with an IC50 of 1 nM. MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis.

A-443654, a pan-Akt inhibitor, exhibits equal potency against Akt1, Akt2, and Akt3 within cells (Ki=160 pM).

CCT244747 is a potent and highly selective CHK1 inhibitor that is orally active, ATP-competitive, and cytotoxic, abrogating drug-induced S and G2 blockade and inducing apoptosis in multiple tumor cell lines.

MRT00033659 is an effective broad-spectrum kinase inhibitor of CK1 (IC50=0.9 µM for CK1δ) and CHK1 (IC50=0.23 µM). MRT00033659 is a pyrazolo-pyridine analogue. It also induces p53 pathway activation and E2F-1 destabilization.

PD 407824 is a chemical BMP sensitiser that promotes increased cellular sensitivity to subthreshold amounts of BMP4.PD 407824 is a potent inhibitor of the checkpoint kinases Chk1 and WEE1 (IC50s: 47 and 97 nM, respectively).

SB-218078 is less potently inhibits Cdc2 (IC50: 250 nM) and PKC (IC50: 1000 nM). SB-218078 is a potent, ATP-competitive, and cell-permeable checkpoint kinase 1 inhibitor that inhibits Chk1 phosphorylation of cdc25C (IC50: 15 nM).

BX795 is an effective and selective PDK1 inhibitor (IC50: 6 nM), and its selectivity is 140- and 1600-fold for PDK1 over PKA and PKC in cell-free assays, respectively. Meanwhile, the selectivity for PDK1 is 100-fold than GSK3β.

BX-912 is a specific inhibitor of 3-Phosphoinositide-dependent Kinase-1 (PDK1, IC50: 12 nM). The selectivity of BX-912 is more 10 fold than C-Kit, EGFR, PKA, PKC etc.

WAY-230563 is a serine threonine kinase inhibitor that blocks CHK1 CHK2-mediated cell cycle checkpoints, leading to G2 M phase arrest in tumour cells following DNA damage.

PF-477736, also known as PF-00477736, is a potent CHK1 inhibitor with potential to enhance chemotherapy. This compound inhibits CHK1, an ATP-dependent serine threonine kinase that is a crucial component of the S G2 checkpoint system for DNA replication monitoring. By bypassing the final checkpoint defenses against DNA damage-induced lethal effects, PF-477736 may improve the antitumor efficacy of various chemotherapeutic agents in tumor cells with inherent checkpoint deficiencies.