chk2

Baricitinib (INCB028050) is a JAK1 and JAK2 inhibitor (IC50=5.9/5.7 nM) with selective and oral activity. Baricitinib has potential anti-inflammatory, immunomodulatory and anti-tumor activity.

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.

ANI-7 is an activator of the aryl hydrocarbon receptor (AhR) pathway, inhibiting the growth of various cancer cells and selectively inhibiting the growth of MCF-7 breast cancer cells (GI50: 0.56 μM).

CCT241533 is an effective and selective ATP competitive inhibitor of CHK2 (Ki: 1.16 nM; IC50: 3 nM).

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

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.

CCT241533 hydrochloride is an effective and selective ATP competitive inhibitor of CHK2 (Ki: 1.16 nM; IC50: 3 nM).

M443 is a potent small molecule inhibitor of MRK that inhibits radiation-induced activation of p38 and Chk2 and can be used in cancer research.

PF 477736 (PF-736,PF-00477736) is a specifc, effective and ATP-competitive Chk1 inhibitor (Ki: 0.49 nM ) and also inhibits FGFR3, Aurora-A, VEGFR2, Flt3, Fms (CSF1R), Ret and Yes.

4-Demethyldeoxypodophyllotoxin, an aryl tetrahydronaphthalenyl lignan analog from the roots of Podophyllum peltatum, has anticancer activity and modulates the Chk-2 signaling pathway in MCF-7 breast cancer cells.

Chk2-IN-2 (compound 2) serves as a selective CHK2 inhibitor, showing promise for anticancer applications [1].

BML-277 (C 3742) is a selective checkpoint kinase 2 (Chk2) inhibitor.

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.

VER-00158411 is a checkpoint kinase 1 and CHK2 inhibitor [IC50: 4.4 nM and 4.5 nM, respectively].

PV1162 is a Chk2-specific inhibitor characterized by a potency with an IC 50 value of 0.29 nM. It operates by specifically targeting the gatekeeper-dependent hydrophobic pocket behind the ATP-binding site (adenine-binding region) to inhibit ATP binding to Chk2, effectively suppressing the phosphorylation activity of Chk2. This compound has demonstrated potential for application in cancer therapy.

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.

LD2 is a protein arginine methyltransferase 9 (PRMT9; IC50 = 0.9 µM) inhibitor. It can reduce the proliferation ability of Rec-1 and Raji lymphoblast cells, UPN1 mantle cell lymphoma, BL-41 Burkitt lymphoma, and OCI-Ly3 diffuse large B-cell lymphoma (DLBCL) cells (IC50s = 2.5-5 µM). LD2 (2.5 µM) can induce G2/M phase cell cycle arrest in THP-1 acute myeloid leukemia (AML) cells and reduce the phosphorylation levels of checkpoint kinases 1 (Chk1) and Chk2 in their cells.

SAR-020106 is a potent, ATP-competitive, and selective CHK1 inhibitor with an IC50 of 13.3 nmol L on the isolated human enzyme.

Chk2 inhibitor,ATP-competitive

PV-1115 is an effective and highly selective inhibitor of the Chk2.

SC-203885 is a checkpoint kinase 2 inhibitor.

AT13148 is an oral-active and ATP-competitive, multi-AGC kinase inhibitor for Akt1 2 3, p70S6K, PKA, and ROCKI II.

VRX-0466617 is a novel selective Chk2 inhibitor.