CDK Inhibitor

KDM1/CDK1-IN-1 (compound 4) is a potent KDM1 and CDK1 inhibitor, with IC₅₀ values of 0.096 and 0.078 μM, respectively.KDM1/CDK1-IN-1 induces cell cycle arrest at G2/M phase and apoptosis in HOP-92 cells. KDM1/CDK1-IN-1 exhibits potent cytotoxic activity against the CCRF-CEM, HOP-92 and Hep-G2 cells, with IC₅₀ values of 16.34, 3.45 and 7.79 μM, respectively.

CDK7-IN-12 is a potent inhibitor of CDK7. CDK7-IN-12 plays a key role in transcriptional regulation and cell cycle regulation. CDK7-IN-12 effectively inhibit malignant tumor proliferation in vitro and in vivo. CDK7-IN-12 has the potential for the research of cancer disease (extracted from patent WO2021249417A1, compound 43).

CDK2-IN-43 (Compound 3a) is a CDK2-cyclin E2 inhibitor with an IC₅₀ value of 6.0 nM. CDK2-IN-43 can be used in the research of the anti-cancer field.

CDK2-IN-36 (compound1) is a CDK2 inhibitor with anticancer activity.

CDK12/13-IN-2 (Compound 24) is a covalent inhibitor of CDK12/13, with IC₅₀ values of 15.5 nM and 12.2 nM for CDK12 and CDK13, respectively. CDK12/13-IN-2 can inhibit the proliferation of breast cancer cells and can be used in the research of triple-negative breast cancer.

Aristolochic acid D (Standard) (Aristolochic acid-IVa (Standard)) is the analytical standard of Aristolochic acid D (HY-N1465). This product is intended for research and analytical applications. Aristolochic acid D (Aristolochic acid-IVa) is an orally active PDE2 (IC₅₀: 4.673 μM) and CDK2 (IC₅₀: 25 μM) inhibitor that can be isolated from Aristolochia indica L. Aristolochic acid D exhibits anti-inflammatory activity and is non-carcinogenic and non-nephrotoxic. Aristolochic acid D can be used in the research of inflammation and tumor-related diseases.

ARUK2010489 (Compound 23) is a potent, selective and brain-penetrant NUAK1 inhibitor with a pIC₅₀ of 8.7. ARUK2010489 also inhibits CDK2, CDK4 and CDK6 activity, with inhibitory rate of 7%, 39% and 26% at 1 μM. ARUK2010489 can be used for the research of neurological disease, such as Alzheimer’s disease (AD).

CDK2-IN-18 (compound 8q) is a potent inhibitor of CDK2/E and CDK4/D1, with IC₅₀s of 8 nM and 46 nM, respectively. CDK2-IN-18 inhibits the proliferation of tumor cells.

Cdk9 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Cdk9 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

CDK2/9-IN-1 (compound 20a) is an orally active dual inhibitor of CDK2 and CDK9 with IC₅₀ values are 0.004 μM and 0.009 μM respectively. CDK2/9-IN-1 induces apoptosis by regulating G2/M cell cycle arrest. CDK2/9-IN-1 has antitumor activity.

EGFR/CDK2-IN-5 is a potent dual EGFR and CDK2 inhibitor with IC₅₀s of 17.30 and 212.10 nM, respectively. EGFR/CDK2-IN-5 also inhibits EGFR^T790M with an IC₅₀ of 123.8 nM. EGFR/CDK2-IN-5 exhibits potent anticancer activity. EGFR/CDK2-IN-5 induces G1 and S cell cycle arrest and apoptosis, accompanied by increased levels of caspase-3/9 and Bax, as well as decreased Bcl-2 levels. EGFR/CDK2-IN-5 can be used for the research of cancers, such as lung cancer, breast cancer, and leukemia.

CDK-IN-15 (Compound 456) is a potent Cyclin A inhibitor, with an IC₅₀ of 0.14 μM.

Cdk2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Cdk2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

CDK7-IN-20 is a potent, selective and irreversible CDK7 (CDK) inhibitor with an IC₅₀ value of 4 nM. CDK7-IN-20 displays >206-fold selectivity for CDK7 over CDK1, CDK2, CDK3, CDK5, CDK6, CDK9 and CDK12 . CDK7-IN-20 has the potential for autosomal dominant polycystic kidney disease (ADPKD) research.

Tacaciclib is a CDK inhibitor, antineoplastic effect.

CDK8-IN-7 (compound 12) is a potent and selective cyclin-dependent kinase 8 (CDK8) inhibitor with an K_d of 3.5 nM. CDK8-IN-7 shows cytotoxicity for MOLM-13, OCI-AML3, MV4-11, NRK and H9c2 cells with IC₅₀s of 5.9, 4.8, 5.4, 16.2, 12.5-25 µM, respectively. CDK8-IN-7 has the potential for the research of AML-cancer.

ZNL-02-096 is a selective Wee1 PROTAC degrader. ZNL-02-096 binds to CRBN and Wee1 to form a ternary complex, inducing CRBN- and proteasome-dependent ubiquitination and proteasomal degradation of Wee1. ZNL-02-096 inhibits recombinant PLK1 with an IC₅₀ of 102 nM, but does not induce its degradation in cells. ZNL-02-096 induces G₂/M phase arrest, Apoptosis, transient integrated stress response, upregulation of ATF4, and phosphorylation of GCN2. ZNL-02-096 reduces Tyr15 phosphorylation of CDK1. ZNL-02-096 can be used in research related to ovarian cancer, acute lymphoblastic leukemia, triple-negative breast cancer, multiple myeloma, and pancreatic ductal adenocarcinoma.

Palbociclib-d₄ (hydrochloride) is the deuterium labeled Palbociclib hydrochloride. Palbociclib (PD 0332991) is a selective CDK4 and CDK6 inhibitor with IC₅₀s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research.

Carbonic anhydrase inhibitor 33 (11D) is a dual inhibitor of CA (Carbonic anhydrase) IX/XII and CDK6, with K_i values of 19.7 nM and 26.1 nM for hCA IX and hCA XII, respectively. Carbonic anhydrase inhibitor 33 (11D) induces G1 arrest and apoptosis. Carbonic anhydrase inhibitor 33 (11D) can be used in the research for NSCLC.

CDK2/4-IN-2 (compound 56) is a CDK2 and CDK4 dual inhibitor with IC₅₀s less than 100 nM. CDK2/4-IN-2 can be used in the study of cancer.