Checkpoint Kinase (Chk) Inhibitor

Zimistobart (BMS-986315) is a fully human IgG1 antibody that targets NKG2A. Zimistobart can be used for the study of non-small cell lung cancer (NSCLC). The isotype control for Zimistobart can refer to Human IgG1 kappa, Isotype Control (HY-P99001).

Prexasertib-d₄ (LY2606368-d₄) is the deuterium labeled Prexasertib (HY-18174). Prexasertib (LY2606368) 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 inhibits CHK2 (IC₅₀=8 nM) and RSK1 (IC₅₀=9 nM). Prexasertib causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib shows potent anti-tumor activity.

CBP-501, 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 is used for various types of cancer.

VRX0466617 is a selective and ATP-competitive Chk2 inhibitor with an IC₅₀ of 120 nM and a K_i of 11 nM. VRX0466617 does not inhibit the related Chk1 activity. VRX0466617 can be used in the study of cancer.

BBI-2779 is a highly selective, orally active CHK1 inhibitor with a CHK1 IC₅₀ of 0.3 nM. BBI-2779 leverages transcription-replication conflicts on extrachromosomal DNA (ecDNA) to induce synthetic lethality, replication stress, DNA damage and cell death in ecDNA-positive tumor cells. BBI-2779 blocks ecDNA-mediated acquired resistance to targeted therapies and inhibits tumor growth in mouse models of gastric cancer. BBI-2779 is applicable to ecDNA-positive cancer-related research.

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

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.

CHK1-IN-2 is a checkpoint kinase 1 (CHK1) inhibitor, with an IC₅₀ of 6 nM.

NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC₅₀=200 nM in a cell-free kinase assay). It is selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK with IC₅₀ values of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC₅₀=240 nM). It inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro.2 NSC 109555 (1,250 nM) potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of reactive oxygen species (ROS) in MIA PaCa-2 cells.

Chek1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Chek1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

Isogranulatimide is a selective checkpoint kinase 1 (Chk1) inhibitor with an IC₅₀ value of 0.1 μM. Isogranulatimide inhibits the G2/M checkpoint and inhibits the growth of p53-mutant tumor cells. Isogranulatimide is promising for research of tumors associated with DNA damage response.

PV1115 is a potent and highly selective Chk2 inhibitor with an IC₅₀ of 0.14 nM, 66000 nM, >100000 nM for Chk2, Chk1 and RSK2, respectively. PV1115 is situated within the ATP-binding pocket of Chk2.

PD-321852 is a Chk1 inhibitor, with IC₅₀ of 5 nM. PD-321852 can be used in anti-cancer research.

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

MCL1020 is a CHK1 inhibitor with an IC₅₀ of 1.61 μM. MCL1020 properly occupies the ATP pocket by interacting with a diverse range of the sites of CHK1 kinase. MCL1020 can be used for the study of hematologic malignancies.

CHEK2 Human Pre-designed siRNA Set A contains three designed siRNAs for CHEK2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

Chek2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Chek2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

Chek2 Rat Pre-designed siRNA Set A contains three designed siRNAs for Chek2 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

BEN-28010 is a selective, orally active, blood-brain barrier permeable CHK1 inhibitor with an IC₅₀ of 4.0 nM. BEN-28010 functions as a radiosensitizer, exhibits antitumor efficacy in GBM models. BEN-28010 can be used for the research of glioblastoma.