CDK Inhibitor

SLM6 is a sangivamycin-like molecule. SLM6 is a CDK9 inhibitor. SLM6 inhibits CDK9/cyclin K and CDK9/cyclin T1 kinase activity with IC₅₀s of 280 nM and 133 nM, respectively. SLM6 also inhibits CDK1/cyclin B and CDK2/ cyclin A with IC₅₀s of less than 300 nM. SLM6 induces apoptosis in multiple myeloma (MM) cells.

Xylocydine is an inhibitor of CDK1/2, inhibiting CDK function in various apoptotic processes. Xylocydine specifically blocks CDK1 and CDK2 activity with IC50 of 1.4 nM and 61 nM, respectively. In addition, Xylocydine downregulates phosphorylated nucleolin and retinoblastoma protein levels..

Crispene E is a STAT3 inhibitor with an IC₅₀ of 10.27 μM against STAT3 dimerization. Crispene E exerts specific cytotoxicity against STAT3-dependent MDA-MB-231 breast cancer cells. Crispene E is applicable to research related to breast cancer.

CDK7-IN-18 is a potent inhibitor of CDK7. CDK7-IN-18 is a pyrimidinyl derivative compound. CDK7-IN-18 has the potential for the research of various cancers, especially the cancer with transcriptional dysregulation (extracted from patent CN114249712A, compound 15).

RO8323 is an orally active, selective CDK8/CDK19 inhibitor, with an IC₅₀ of 2 nM against CDK8 and 3 nM against CDK19. RO8323 promotes regulatory T cell differentiation, inhibits effector T cell generation, reverses the Teff/Treg ratio, upregulates IL-10 production in myeloid cells, and suppresses the production of TNF-α, IL-6 and IL-12. RO8323 enhances immune reconstitution and prolongs cardiac allograft survival in a dose-dependent manner. RO8323 can be used in the research of chronic graft-versus-host disease, cardiac allograft rejection, acute graft-versus-host disease and experimental autoimmune encephalomyelitis.

CKD-712 is an orally active multi-target tetrahydroisoquinoline derivatived and a potent inhibitor of the NF-κB pathway. CKD-712 selectively inhibits MMP-9 with no effect on MMP-2, downregulates the expression of TNF-α, IL-6, cyclin A, cyclin B, CDK-1 and other proteins, and activates the PI3K/Akt signaling pathway. CKD-712 blocks the activation and nuclear translocation of NF-κB, downregulates inflammatory factors and pro-tumor metastatic proteins, and induces G2/M phase arrest in tumor cells and thereby inhibits the invasion of cancer cells. CKD-712 can be used for the research of sepsis, myocardial ischemia-reperfusion injury and non-small cell lung cancer.

CDK2-IN-8 is a potent CDK2 inhibitor with an IC₅₀ of 1.74 µM. CDK2-IN-8 shows antiproliferative activity. CDK2-IN-8 has the potential for the research of melanoma.

PARP1/CDK12-IN-2 is a selective dual PARP1/CDK12 inhibitor with an IC₅₀ of 42 nM for CDK12 and an IC₅₀ of 35 nM for PARP1. PARP1/CDK12-IN-2 inhibits CDK13. PARP1/CDK12-IN-2 induces Apoptosis and induces G2/M phase arrest. PARP1/CDK12-IN-2 exhibits anticancer activity against breast cancer and lung cancer. PARP1/CDK12-IN-2 can be used for research on triple-negative breast cancer.

CDK9-IN-34 (Compound 1b) is an inhibitor for CDK9 with an IC₅₀ of 0.25 μM. CDK9-IN-34 exhibits cytotoxicity to cancer cell HCT116, MCF7 and K652 with IC₅₀s of 1.43, 3.01 and 50.27 μM, respectively. CDK9-IN-34 exhibits antiviral activity against coronavirus 229E with an IC₅₀ of 145.92 μM.

CDK9-IN-33 (compound C35) is a potent, selective and orally active CDK9 inhibitor with IC₅₀ values of 17.44, 160, 316.30, 1771.00, >10000 nM for CDK9, CDK7, CDK2, CDK4, CDK6 respectively. CDK9-IN-33 induces apoptosis. CDK9-IN-33 decreases the protein expression of RPB1 CTD Ser2, RPB1, MCL1. CDK9-IN-33 shows anti-tumor activity.

RO5068760 is a potent, orally active and selective non-ATP-competitive MEK1/2 inhibitor with an IC₅₀ of 0.025 μM for MEK1. RO5068760 significantly inhibits MAPK pathway activity, thereby inducing G1 cell cycle arrest and apoptosis to inhibit cancer cell growth. RO5068760 exhibits significant efficacy in a broad spectrum of tumors with aberrant MAPK pathway activation. RO5068760 can be used for melanoma, colorectal cancer, non-small cell lung cancer (NSCLC), and pancreatic cancer research.

CDK9/HDAC1/HDAC3-IN-1 is dual-functional inhibitor of CDK9 and HDAC. CDK9/HDAC1/HDAC3-IN-1 inhibits the protein activity of CDK9/HDAC/HDAC3 with IC₅₀ s of 0.17  μM, 1.73  μM and 1.11 μM for CDK9, HDAC1, and HDAC3, respectively. CDK9/HDAC1/HDAC3-IN-1 inhibits cancer cells by inducing cell apoptosis and cell cycle arrest in the G2/M phase, as well as tumor growth in a murine TNBC MDA-MB-231 xenograft model. CDK9/HDAC1/HDAC3-IN-1 has a broad-spectrum anti-cancer activity, such as breast cancer, cervical cancer, and liver cancer.

CDK-IN-11 is a heterocyclic compound that has an action of promoting cardiomyocyte maturation.

CDK5-IN-2 (compound 15) is a highly selective CDK5 inhibitor with IC₅₀s of 0.2 and 23 for CDK5/p25 and CDK2/CycA, respectively.

GSK3-IN-10 (Compound 4) is a multi-target inhibitor, that mainly targets GSK3α and GSK3β with IC₅₀ of 1.0 nM and 2.0 nM. GSK3-IN-10 inhibits the activation of β-catenin, promotes the neuronal survival, and exhibits a protective effect against endoplasmic reticulum stress.

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.

CDK2-IN-9 is a potent CDK2 inhibitor with an IC₅₀ of 0.63 µM. CDK2-IN-9 shows antiproliferative activity. CDK2-IN-9 induces apoptosis and cell cycle arrest at S and G2/M phase. CDK2-IN-9 has the potential for the research of melanoma.

CDK9-IN-50 is a selective and orally active CDK9 inhibitor with an IC₅₀ of 2.2 nM. CDK9-IN-50 targets a distinct CDK9-specific subpocket to disrupt RNA polymerase II Ser2 phosphorylation and downregulate short-lived oncoproteins, including AR-V7 and Myc. CDK9-IN-50 exhibits antiproliferative activity against cancer cells, induces apoptosis and induces tumor growth inhibition in CRPC orthotopic mice models. CDK9-IN-50 can be used for the research of cancer, such as prostate 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.

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