Checkpoint Kinase (Chk) Inhibitor

XL-844 (EXEL-9844) is an inhibitor of Chk1 and Chk2. XL-844 exhibits antineoplastic activity. XL-844 can result in tumor cell apoptosis through inhibition of cell cycle arrest. XL-844 inhibits VEGFR1 and VEGFR3. XL-844 can be studied in anti-cancer research.

CHK1-IN-12 (Compound example 1-5) is an orally active and highly selective checkpoint kinase 1 (CHK1) inhibitor with in vitro enzyme IC₅₀≤10 nM and cellular IC₅₀≤50 nM. CHK1-IN-12 inhibits the phosphorylation activity of CHK1 kinase to block the DNA damage response pathway, inducing tumor cell cycle arrest and apoptosis. CHK1-IN-12 is promising for research of cancers.

CBP-93872 is a G2 checkpoint inhibitor and a chemosensitizer. CBP-93872 specifically inhibits DNA double-strand break (DSB)-dependent, Nbs1-mediated ATR activation, without directly inhibiting ATR kinase activity or affecting ATR activation induced by other types of DNA damage; meanwhile, it suppresses the pathway between ATM and ATR activation, thereby reducing the autophosphorylation of ATR and the subsequent phosphorylation of Chk1. CBP-93872 does not inhibit DNA end resection at DSB sites. CBP-93872 induces cell death and enhances the cytotoxic effects of platinum-containing compounds and pyrimidine antimetabolites on cancer cells. CBP-93872 can be used in related research on p53-mutant cancers, colorectal cancer, and pancreatic cancer.

M2I-1 (Standard) is the analytical standard of M2I-1 (HY-100341). This product is intended for research and analytical applications. M2I-1 is a Mad2 inhibitor targeting the binding of Mad2 to Cdc20, an essential protein-protein interaction (PPI) within the spindle assembly checkpoint (SAC).

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 (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 Ki of 0.49 nM, it is also a Chk2 inhibitor, with a Ki of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC50=8 (Ki), 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.

CHK1-IN-4 is a selective checkpoint kinase 1 (Chk1) inhibitor with an IC₅₀ ≤ 1 nM. The IC₅₀ value of CHK1-IN-4 against Chk2 ranges from 50 to 100 nM. CHK1-IN-4 inhibits cancer cell proliferation and exhibits antitumor activity in colon cancer xenograft models. CHK1-IN-4 can be used for the research of colon cancer and breast cancer.

AZD-7762 hydrochloride (Standard) is the analytical standard of AZD-7762 (hydrochloride) (HY-10992A). This product is intended for research and analytical applications. AZD-7762 hydrochloride is a potent ATP-competitive checkpoint K_inase (Chk) inhibitor in with an IC₅₀ of 5 nM for Chk1.

AZD-7762 (Standard) is the analytical standard of AZD-7762 (HY-10992). This product is intended for research and analytical applications. AZD-7762 is a potent ATP-competitive checkpoint K_inase (Chk) inhibitor in with an IC₅₀ of 5 nM for Chk1.

GDC-0425 hydrochloride (RG-7602 hydrochloride) is an orally active, highly selective ChK1 inhibitor. GDC-0425 hydrochloride abrogates cell cycle arrest and inhibits genomic repair. GDC-0425 hydrochloride potently suppresses Gemcitabine (HY-17026)-induced pCDK1/2 expression. GDC-0425 hydrochloride can be used in research related to osteosarcoma, ovarian cancer, basal (triple-negative) breast cancer, and colorectal cancer.

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.