Checkpoint Kinase (Chk) Inhibitor

BPTQ is a potent inhibitor against VEGFR1 and CHK2 with IC₅₀ values of 0.54 and 1.70 µmol/L, respectively. BPTQ is also an intercalator of DNA with anticancer activities. BPTQ inhibits the proliferation of HL-60 cells by arresting cells at S and G2/M phase with an IC₅₀ value of 12 µmol/L. BPTQ also activates the mitochondria-mediated Apoptosis pathway by a decrease in mitochondrial membrane potential, increase in the Bax:Bcl-2 ratio and activation of caspases.

Graviquinone is a Chk1 inhibitor. Graviquinone exhibits potent cytotoxicity against various cancer cell lines. Graviquinone possesses the characteristics of bypassing ABCB1-mediated multidrug resistance, selectively damaging cancer cell DNA, and regulating the DNA damage response. Graviquinone can also enhance cytotoxicity by increasing ROS levels in cancer cells. Graviquinone can be used for cancer research.

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.

CBP501 Affinity Peptide is a Chk kinase inhibitor that can abrogate G2 arrest induced by DNA-damaging agents. CBP501 Affinity Peptide can be used in cancer research.

NSC 109555 ditosylate is a potent, selective, ATP-competitive checkpoint kinase 2 (Chk2) inhibitor with an IC₅₀ of 240 nM. NSC 109555 ditosylate can be used for the research of cancer.

Zn-DPA-maytansinoid conjugate 1 is a small molecule-based maytansinoid conjugate targeting immune checkpoint. Zn-DPA-maytansinoid conjugate 1 induces lasting regression of tumor growth and rejuvenates tumor microenvironment (TME) to an "inflamed hot tumor" .

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.

FLT3/CHK1-IN-2 (Compound 30) is a dual inhibitor of FLT3 and CHK1, with IC₅₀s of 25.63, 16.39, 22.80 nM for CHK1, FLT3-WT, and FLT-D835Y respectively. FLT3/CHK1-IN-2 has favorable oral PK properties and kinase selectivity. FLT3/CHK1-IN-2 can be used for research of acute myeloid leukemia (AML).

GDC0575 (ARRY-575) hydrochloride is a highly-selective and orally active Chk1 (IC₅₀=1.2 nM) inhibitor. GDC0575 (ARRY-575) hydrochloride can be used for colitis-associated cancer (CAC) and colitis research.

(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.

CHK1-IN-9 (compound 11) is an orally active CHK1 inhibitor with an IC₅₀ value of 0.55 nM. CHK1-IN-9 can enhance the effect of DNA-damaging drugs on tumor cells. CHK1-IN-9 has synergistic anticancer effects with Gemcitabine (HY-17026).

CHK1-IN-13 (Compound 38) is a checkpoint kinase 1 (Chk1) inhibitor with an IC₅₀ of 10-50  nM. CHK1-IN-13 has anticancer activity, and can be used for the research of cancers, such as breast, ovarian and prostate cancer.

Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC₅₀ values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect.

CHK1-IN-14 is a free base form of CHK1 inhibitor. CHK1-IN-14 can be used in research on resistance to chemotherapy and radiotherapy.

DB07006 (compound 18) is a potent, ATP-cpmpetitive dual inhibitor of Wee1 (IC₅₀ = 0.030 μM) and Chk1 checkpoint kinases (IC₅₀ = 0.018 μM). DB07006 demonstrates effective abrogation of the G2/M checkpoint in combination with DNA-damaging agents in cellular models. DB07006 can be used for cancer research.

(S)-CCT245737 ((S)-SRA737) is a potent and selective oral inhibitor of checkpoint kinase 1 (CHK1).

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