CDC Inhibitor

Simurosertib (TAK-931) is an orally active, selective and ATP-competitive cell division cycle 7 (CDC7) kinase inhibitor, with an IC₅₀ of <0.3 nM. Simurosertib has anti-cancer activity.

MBQ-167 is a dual Rac/Cdc42 inhibitor, with IC₅₀s of 103 nM for Rac 1/2/3 and 78 nM for Cdc42 in MDA-MB-231 cells, respectively.

XL413 is a potent, selective and ATP competitive inhibitor of Cdc7, with an IC₅₀ of 3.4 nM, and also shows potent effect with IC₅₀s of 215, 42 nM on CK2, PIM1, respectively, and an EC₅₀ of 118 nM on pMCM.

XL413 (BMS-863233) hydrochloride is a potent, selective and ATP competitive inhibitor of Cdc7, with an IC₅₀ of 3.4 nM, and also shows potent effect with IC₅₀s of 215, 42 nM on CK2, PIM1, respectively, and an EC₅₀ of 118 nM on pMCM.

CKI-7 free base is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC₅₀ of 6 μM and a K_i of 8.5 μM. CKI-7 free base is a selective Cdc7 kinase inhibitor. CKI-7 free base also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 free base has a much weaker effect on casein kinase II and other protein kinases.

CDC25A/NF-κB-IN-1 is an effective dual-target inhibitor of CDC25A and NF-κB, and is a prodrug of Pt(IV). CDC25A/NF-κB-IN-1 has anticancer activity and low cytotoxicity to normal cells. CDC25A/NF-κB-IN-1 can trigger a variety of anticancer mechanisms, including S phase cell cycle arrest, mitochondrial endogenous apoptosis, endoplasmic reticulum stress, autophagy-dependent ferroptosis. CDC25A/NF-κB-IN-1 has good safety and can be used for ovarian cancer research.

LY3177833 (Example 4) is an orally active CDC7 and pMCM2 inhibitor with IC₅₀ values of 3.3 nM and 290 nM, respectively. LY3177833 is a senescence inducer.

CKI-7 is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC₅₀ of 6 μM and a K_i of 8.5 μM. CKI-7 is a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 has a much weaker effect on casein kinase II and other protein kinases.

DDO-6079 is a potent CDC37 inhibitor. DDO-6079 inhibits HSP90-CDC37 and CDC37-CDK4/6 chaperone complex by binding to an allosteric site on CDC37. DDO-6079 decreases the thermostability of CDK6.

(S)-LY3177833 ((S)-Example 2) hydrate is an orally active CDC7 kinase inhibitor. (S)-LY3177833 hydrate shows broad in vitro anticancer activity.

LY3177833 (Example 4) monhydrate is an orally active CDC7 and pMCM2 inhibitor with IC₅₀ values of 3.3 nM and 290 nM, respectively. LY3177833 monhydrate is a senescence inducer.

(S)-LY3177833 ((S)-Example 2) is an orally active CDC7 kinase inhibitor. (S)-LY3177833 shows broad in vitro anticancer activity.

Cdc7-IN-15 (Example 108) is a cdc7 kinase inhibitor. Cdc7-IN-15 can be used for cancer research.

XL413 (BMS-863233) hydrochloride is an orally active and selective CDC7 inhibitor (IC₅₀=3.4 nM). XL413 hydrochloride has favorable pharmacokinetic profiles and significantly inhibits tumor growth in rodent models. XL413 hydrochloride can be used in cancer research.

Cdc7-IN-14 (compound 82) is a potent CDC7 inhibitor with an IC₅₀ of <1 nM. Cdc7-IN-14 has the potential for the research of cancer.

Cdc7-IN-13 (compound 84) is a potent CDC7 inhibitor with an IC₅₀ of <1 nM. Cdc7-IN-13 has the potential for the research of cancer.

Cdc7-IN-18 (compound 1-2) is a potent CDC7 inhibitor with an IC₅₀ of 1.29 nM for Cdc7/DBF4 enzyme. Cdc7-IN-18 shows antiproliferative activities with IC₅₀ of 53.62 nM in COLO205 cells.

Cdc7-IN-12 (compound 1) is a potent CDC7 inhibitor with an IC₅₀ of <1 nM. Cdc7-IN-12 shows antiproliferative activities with IC₅₀ of 100-1000 nM in COLO205 cells. Cdc7-IN-12 has the potential for the research of cancer.

PSTAIR is a monoclonal antibody that recognizes the PSTAIR sequence in Cdc28, PSTAIR can be used as loading control.

Cdc7-IN-19 (compound 1-1) is a potent CDC7 inhibitor with an IC₅₀ of 1.49 nM.