CDK Inhibitor

p38α-IN-9 (Compound 2015) is a p38α inhibitor and blocks p38α’s enzymatic activity with an IC₅₀ lower than 20 nM. p38α-IN-9 inhibits MK2^T334 phosphorylation. p38α-IN-9 activates Cdc25b and Cdc25c and simultaneously inactivates Wee1, leading to mitotic catastrophe, aneuploidy or polyploidy and DNA damage. p38α-IN-9 Inhibits colorectal cancer (CRC) metastasis.

SNX2-1-108 is a CDK8 kinase inhibitor.

KB-0742 hydrochloride is a potent, selective and orally active CDK9 inhibitor with an IC₅₀ of 6 nM for CDK9/cyclin T1. KB-0742 hydrochloride is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 hydrochloride has potent anti-tumor activity.

CDK4/6-IN-27 (Example 12) is a CDK4/6 inhibitor. CDK4/6-IN-27 can be used for researching diseases such as cancer.

EF-4-177 is an orally active and allosteric CDK2 inhibitor with the IC₅₀ of 87 nM. EF-4-177 can disrupt spermatogenesis.

SZ-015268 is a CDK7 inhibitor with an IC₅₀ of 23.56 nM. SZ-015268 has extremely significant anti-tumor advantages. SZ-015268 inhibits HCC70, OVCAR-3, HCT116 and HCC1806 cells proliferation with IC₅₀s of 33, 80.56, 12.53, and 61.55 nM, respectively.

MM129 is an anticancer agent. MM129 inhibits key oncogenic signaling molecules such as AKT, mTOR, and CDK2, and downregulates the expression of PD-L1. MM129 induces cell cycle arrest. MM129 induces Apoptosis. MM129 induces DNA damage. MM129 induces oxidative stress. MM129 exhibits chemosensitizing properties. MM129 restores the expression of E-cadherin. MM129 can be used in the research of colorectal cancer.

PROTAC CDK9 degrader-6 is a PROTAC targeting to CDK9 sepcifically. PROTAC CDK9 degrader-6 mediates CDK9 degradation via the proteasome. PROTAC CDK9 degrader-6 degrades CDK9 with DC₅₀s of 0.10 μM and 0.14 μM for the CDK9₄₂ and CDK9₅₅ isoforms, respectively.

Cdk13 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Cdk13 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

GTGKT is a CAGE inhibitor. GTGKT binds to CAGE and blocks the binding of CAGE to GSK3β. GTGKT alters the localization of CAGE and inhibits the binding of CAGE to the promoter sequence of Cyclin D1. GTGKT enhances the Apoptotic effect of anticancer agents. GTGKT reduces the expression of Cyclin D1. GTGKT decreases the tumorigenic potential of melanoma and hepatocellular carcinoma cells.

CDK2-IN-48 (Compound 109) is a CDK2 inhibitor with IC₅₀ values for CDK2 and CDK1 of respectively < 0.05 and > 1 μM. CDK2-IN-48 can be used for the study of CDK2-dependent cancers.

KI-ARv-03 is a potent and selective ATP-competitive CDK9 inhibitor with an IC₅₀ of 0.15 μM (at 45 μM ATP), exhibiting over 130-fold selectivity against other CDKs (including CDK1-7). KI-ARv-03 reduces androgen receptor (AR)-driven transcription and proliferation in prostate cancer cells. KI-ARv-03 can be used for leukemia, pancreatic cancer, alveolar rhabdomyosarcoma (ARMS) and castration-resistant prostate cancer (CRPC) research. KI-ARv-03 is a ligand for target protein for PROTAC. KI-ARv-03 can be used to synthesize PROTAC KI-CDK9d-32 (HY-173523)^[1][2].

CDK6 ligand-Linker Conjugate 1 is a target protein ligand-linker conjugate that incorporates a ligand for CDK6 (HY-180278) and a linker, which recruits E3 ligases. CDK6 ligand-Linker Conjugate 1 can be used for synthesis of PROTAC CDK6 Degrader 1 (HY-180277).

CDK2-IN-50 is a CDK2 inhibitor (IC₅₀ = 0.77 nM). CDK2-IN-50 can induce G1 phase arrest, indicating that it has an effective CDK2/cyclin E targeting mechanism. CDK2-IN-50 also has a significant pro-apoptotic effect. CDK2-IN-50 can be used for the study of breast cancer.

CLK2/3-IN-1 (Compound 7c) is an orally active CLK2/3 inhibitor (EC₅₀: 5.07 nM and 30.03 nM, respectively). CLK2/3-IN-1 binds to Lys193 and Lys186 of CLK2/3 via hydrogen bonds. CLK2/3-IN-1 can inhibit the proliferation of SW480 tumor cells (IC₅₀: 163 nM). CLK2/3-IN-1 can be used to study CLK-related tumor diseases.

CDK4/6-IN-22 (Compound 1-A) is a CDK4 and CDK6 dual inhibitor.

ARUK2010694 (Compound 20) is a potent and selective NUAK1 inhibitor with a pIC₅₀ of 8.7. ARUK2010694 also inhibits CDK2, CDK4 and CDK6 activity, with inhibitory rate of 13%, 63% and 32% at 1 μM. ARUK2010694 can be used for the research of neurological disease, such as Alzheimer’s disease (AD).

VCC972839:01 is an inhibitor for cyclin dependent kinase (CDK9), with IC₅₀ of 7 nM. VCC972839:01 inhibits the cell viability of SCLC cells in nanomolar levels. VCC972839:01 induces apoptosis through an intrinsic pathway. VCC972839:01 exhibits antitumor activity in mouse model.

Telapristone acetate (CDB-4124) is a potent progesterone receptor (PR) modulator. Telapristone acetate inhibits the proliferation of ovarian cancer cells by inducing cell cycle arrest and apoptosis. Telapristone effectively inhibits the occurrence and development of spontaneous and chemically induced mammary tumors in rats. Telapristone acetate can be used for breast and ovarian cancer research.

LK1/2-IN-3 (compound 3) is a potent and selective CLK1 and CLK2 inhibitor with IC₅₀ values of 1.1, 2.1, 130, 260, 260 nM for CLK1, CLK2, SRPK1, SRPK2, SRPK3, respectively. CLK1/2-IN-3 shows anti-proliferative activity. CLK1/2-IN-3 reduces the levels of endogenous phosphorylated SR proteins and increases the expression of S6K mRNAs.