Chk1 Inhibitor

AZD-7762 hydrochloride is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC₅₀ of 5 nM for Chk1.

CHK1-IN-3 is a potent and selective CHK1 inhibitor with an IC₅₀ of 0.4 nM. CHK1-IN-3 effectively inhibits the growth of malignant hematopathy cell lines and displays low affinity for hERG (IC₅₀ > 40 μM). CHK1-IN-3 significantly suppresses the tumor growth in vivo. CHK1-IN-3 can be used for the study of hematologic malignancies.

MRT00033659 is a potent broad-spectrum kinase inhibitor of CK1 (IC₅₀=0.9 μM for CK1δ) and CHK1 (IC₅₀=0.23 μM). MRT00033659, a pyrazolo-pyridine analogue, induces p53 pathway activation and E2F-1 destabilisation.

Chk1-IN-6 is a selective and orally active Chk1 inhibitor with an IC₅₀ of 16.1 nM. Chk1-IN-6 shows antiproliferative activity of MV-4-11 cells. Chk1-IN-6 exerts effective response in the MV-4-11 xenograft mouse model. Chk1-IN-6 exhibits synergistic anticancer effect with Gemcitabine (HY-17026). Chk1-IN-6 can be used in the research of cancers such as acute myeloid leukemia and colorectal adenocarcinoma.

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

Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) 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 Hydrate inhibits CHK2 (IC₅₀=8 nM) and RSK1 (IC₅₀=9 nM). Prexasertib Mesylate Hydrate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib Mesylate Hydrate 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.

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.

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

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.

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.

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.

(Rac)-SCH900776 ((Rac)-MK-8776) is the racemate of SCH900776 (HY-15532). SCH900776 (MK-8776) is a potent and selective Chk1 inhibitor with an IC₅₀ value of 3 nM.

BBI-355 (Compound 1) is an orally active, checkpoint kinase 1 (CHK1) inhibitor. BBI-355 is useful for the study of cancers with oncogene amplification.