CDK Inhibitor

Crozbaciclib fumarate is a CDK4/6 inhibitor with IC₅₀s of 3 and 1 nM, respectively.

Otviciclib (Compound 86) is a CDK inhibitor. Otviciclib has potent anti-proliferative activity against solid tumor cells (such as HCT116, NCIH82 and DU145 cells) with no significant toxicity to normal cells, and effectively induces the G2/M phase cells arrest and apoptosis. Otviciclib has a broad-spectrum anticancer activity, such as colon, pancreatic and lung cancer.

Lenoremycin (Ro 21-6150) is a microbial metabolite. Lenoremycin decreases β-catenin and cyclin D1 proteins levels. Lenoremycin decreases cancer stem cells (CSCs) populations via inducing reactive oxygen species production.

CDK4/6/BRD4-IN-2 (Compound PJ2) is a dual inhibitor of CDK4/6 and BRD4 with IC₅₀ values for CDK4, CDK6, BRD4 (BD1), and BRD4 (BD2) of 168.75, 292.45, 23.17, and 3.12 nM respectively. CDK4/6/BRD4-IN-2 has a strong inhibitory effect on non-small cell lung cancer (NSCLC) cell lines. CDK4/6/BRD4-IN-2 induces cell cycle arrest, senescence and apoptosis through ROS-mediated DNA damage. CDK4/6/BRD4-IN-2 can also effectively inhibit the migration and invasion of NCI-H358 cells. CDK4/6-IN-2 can be used for the study of KRAS-mutated NSCLC.

CDK9/10/GSK3β-IN-1 (compound 13c) is a kinase inhibitor (Flavopiridol (HY-10005) analogue) that effectively inhibits HsGSK3β (IC₅₀=59 nM), HsCDK9/CyclinT (IC₅₀=64 nM), HsCDK5/p25 (IC₅₀=1.093 μM) and HsCDK2/CyclinA (IC₅₀=1.725 μM). CDK9/10/GSK3β-IN-1 has anti-cancer cellular activity comparable to or higher than that of Flavopiridol. CDK9/10/GSK3β-IN-1 shows high anti-proliferative activity in vitro against up to seven cancer cell lines.

Zotiraciclib hydrochloride is a novel small molecule multi-target enzyme inhibitor with activity in inhibiting tumor growth. Zotiraciclib hydrochloride exerts its anti-tumor effect by reducing the level of Myc through inhibiting cyclin-dependent kinase 9 (CDK9). Zotiraciclib hydrochloride may be useful for inhibiting cancers that cross the blood-brain barrier. The high protein level of MCL-1 of Zotiraciclib hydrochloride is associated with survival, suggesting that it may serve as a prognostic factor and inhibitory target in further studies.

Cdk1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Cdk1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

Cdk14 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Cdk14 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

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..

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).

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

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.

Cdk4 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Cdk4 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

Maleimide-Val-Ala-PAB-SNS032 is a conjugate of ADC toxin and linker. SNS032 is an inhibitor for CDK, inhibiting the cell cycle at G1/S phase and cell viability of cancer cells. Maleimide-Val-Ala-PAB is a cleavable ADC linker. Maleimide-Val-Ala-PAB-SNS032 can be utilized for the synthesis of ADC molecules.

CLK1-IN-5 is a potent and selective CLK1 inhibitor with an IC₅₀ of 23 nM. CLK1-IN-5 can be used in the research of cancer and Alzheimer's disease.

Chikusetsusaponin IVa methyl ester (CME) is a natural triterpenoid saponin compound. Chikusetsusaponin IVa methyl ester induces G0/G1 cell cycle arrest and apoptosis in colon cancer cells by inhibiting the Wnt/β-catenin signaling pathway. By inhibiting the NF-κB and AP-1 signaling pathways, Chikusetsusaponin IVa methyl ester significantly reduces the production of NO, PGE₂ and pro-inflammatory cytokines (TNF-α, IL-6, IL-1β), and downregulates the levels of iNOS and COX-2. Chikusetsusaponin IVa methyl ester can be used in researches on colorectal cancer and inflammation.

P18IN005 hydrochloride is a novel inhibitor of p18, exhibiting potent activity in negatively regulating haematopoietic stem cell (HSC) self-renewal. P18IN005 hydrochloride has been shown to be more effective than p27 in inhibiting HSC self-renewal in mouse models. P18IN005 hydrochloride promotes the expansion of functional HSCs in short-term cultures. P18IN005 hydrochloride serves as a valuable tool for dissecting the signaling pathways involved in stem cell self-renewal.

Cdc7-IN-17 is a potent CDC7 inhibitor with an IC₅₀ of <10 μM, extracted from patent WO2018217439A1. Cdc7-IN-17 can be used for cancer research.

Multi-target kinase inhibitor 3 (compund 6i) is a multi-kinase target inhibitor with anticancer activity. Multi-target kinase inhibitor 3 inhibits EGFR, HER2, VEGFR-2, and CDK2 with IC50s of 0.063 μM, 0.054 μM, 0.119 μM, and 0.448 μM, respectively. Multi-target kinase inhibitor 3 has a good inhibitory effect on breast cancer cells MCF-7, with an IC50 of 6.10 μM.

GPX4/CDK-IN-1 (Compound B9) is a dual inhibitor of GPX4 and CDK, with IC₅₀ values of 542.5 nM, 191.2 nM and 68.1 nM for GPX4, CDK4 and CDK6, reapectively. GPX4/CDK-IN-1 shows strong cancer cell growth inhibition in vivo.