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.

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.

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.

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

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

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

SCH900776 S-isomer (MK-8776 S-isomer) is an effective, specific and orally bioavailable inhibitor of checkpoint kinase Chk1 (IC50: 3 nM). It also inhibitors Chk2 (IC50: 1500 nM) and cyclin-dependent kinase CDK2 (IC50: 160 nM).

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.

Prexasertib dihydrochloride (LY2606368) is an ATP-competitive CHK1 inhibitor (Ki: 0.9 nmol/L). in the cell-free assay, its IC50 values are 8 nM and 9 nM for CHK2 and RSK, respectively.

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.

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.

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

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.

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.

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.

Potent Chk2 inhibitor (IC50 = 3 nM). Shows >63-fold selectivity for Chk1 over Chk2 and a panel of 84 other kinases. Inhibits Chk2 activation in response to etoposide-induced DNA damage in HT29 cells. Blocks ionizing radiation-induced apoptosis of mouse thymocytes. Caldwell et al (2011) Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2. J.Med.Chem. 54 580 PMID:21186793

Prexasertib dimesylate (LY2606368 dimesylate) is a highly selective, ATP-competitive, second-generation inhibitor of checkpoint kinase 1 (CHK1), with a K_i of 0.9 nM and an IC_50 of <1 nM, and also effectively inhibits CHK2 (IC_50 = 8 nM) and RSK1 (IC_50 = 9 nM). Its mechanism induces double-stranded DNA breakage and replication catastrophe, leading to apoptosis, and demonstrates potent anti-tumor activity.

Prexasertib is a potent and selective Chk1/Chk2 inhibitor. Prexasertib increases the effectiveness of conventional therapy in B-/T- cell progenitor acute lymphoblastic leukemia. LY2606368 causes replication catastrophe and antitumor effects through CHK1-d

Rabusertib (IC-83) is an inhibitor of the cell cycle checkpoint kinase 1 (chk1) with potential chemopotentiating activity. Rabusertib has been used in trials studying the treatment of Cancer, Solid Tumors, Advanced Cancer, Pancreatic Neoplasms, and Non-Small Cell Lung Cancer.

AZD7762 HCl is a checkpoint kinase inhibitor, driving checkpoint abrogation and enhancing DNA-targeted treatment.