Chk2 Inhibitor

Prexasertib mesylate (LY2606368 mesylate) 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 mesylate inhibits CHK2 (IC₅₀=8 nM) and RSK1 (IC₅₀=9 nM). Prexasertib mesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib mesylate shows potent anti-tumor activity.

VER-00158411 is a checkpoint kinase 1 (CHK1) and CHK2 inhibitor with IC₅₀ values of 4.4 nM and 4.5 nM, respectively.

Chk2-IN-2 (compound 2) is a selective inhibitor of CHK2 with potential anticancer activity.

CBP-501 acetate, a cell-permeable calmodulin-binding peptide and a G2-abrogating drug candidate, inhibits the activity of multiple Ser²¹⁶-specific kinases, such as MAPKAP-K2, C-Tak1, CHK1 and CHK2, with IC₅₀ values of 0.9 μM, 1.4 μM 3.4 μM and 6.5 μM, respectively. CBP-501 acetate is used for various types of cancer.

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.

(E/Z)-Chk2-IN-1 ((E/Z)-Hymenialdisine analogue-1) (Compound 1) is a potent and selective cell cycle kinase Chk2 inhibitor with an IC₅₀ of 8 nM. (E/Z)-Chk2-IN-1 exhibits low inhibitory activity against other kinases (such as CK1δ, MEK1, and PKCα/βⅡ) with IC₅₀ values both >89 nM. (E/Z)-Chk2-IN-1 can be used for the research of cancer.

CCT241533 dihydrochloride is a potent and selective ATP competitive inhibitor of CHK2 with an IC₅₀ of 3 nM and K_i of 1.16 nM.

PV1162 is a selective Chk2 inhibitor with an IC₅₀ of 0.29 nM. PV1162 inhibits ATP binding to Chk2 by targeting the gatekeeper-dependent hydrophobic pocket, which is specific to Chk2 and located behind the ATP-binding site (adenine-binding region), thereby inhibiting the phosphorylation activity of Chk2. PV1162 holds potential application value in the field of cancer therapy.

PF 477736 (PF 00477736) (Standard) is the analytical standard of PF 477736 (HY-10032). This product is intended for research and analytical applications. 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.

(E/Z)-PV1162 is an inhibitor of Chk2 and RSK2. (E/Z)-PV1162 regulates the ATM-Chk2 pathway, apoptosis, cell cycle regulation and hypoxia-related processes. (E/Z)-PV1162 is applicable for cancer research.

Prexasertib lactate (LY2606368 lactate) is the lactate form of Prexasertib (HY-18174). Prexasertib lactate 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 lactate inhibits CHK2 (IC₅₀=8 nM) and RSK1 (IC₅₀=9 nM). Prexasertib lactate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib lactate shows potent anti-tumor activity.

Elrelesertib (Standard) (AZD1390 (Standard)) is the analytical standard of Elrelesertib (AZD1390) (HY-109566). This product is intended for research and analytical applications. Elrelesertib (AZD1390) is an orally active, brain-penetrant ATM kinase inhibitor with IC₅₀ values of 0.78 nM. Elrelesertib blocks ATM-dependent DNA damage response, inhibits ATM autophosphorylation and downstream Chk2, Rad50 phosphorylation, and accumulates at DNA breaks. Elrelesertib acts as a radiosensitizer, induces apoptosis, genomic instability, G2-M cell cycle arrest, ROS elevation, and mitochondrial membrane potential alteration. Elrelesertib has low efflux liability against P-gp and BCRP. Elrelesertib can be used for the research of central nervous system malignancies, glioblastoma multiforme, glioma, lung cancer brain metastases, and breast cancer.

CHK-IN-1 is an inhibitor of CHK1 and CHK2, with anti-proliferative activities.