CDK Inhibitor

Radicicol 6-oxime (KF25706) is an Hsp90 inhibitor with an EC₅₀ of 5.5 nM against human Hsp90. Radicicol 6-oxime binds to Hsp90 and disrupts its chaperone function, leading to destabilization and depletion of Hsp90-associated signaling molecules. Radicicol 6-oxime depletes Hsp90-associated signaling proteins such as Raf-1, v-src, p185erbB2, Cdk4, and mutant p53, thereby inhibiting K-ras and v-src signaling pathways. Radicicol 6-oxime exhibits antiproliferative activity against various tumor cells. Radicicol 6-oxime inhibits tumor growth in mouse tumor xenograft models. Radicicol 6-oxime can be used for research on breast cancer, colon cancer, and vulvar epidermoid carcinoma.

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.

CDK9-IN-24 (compound 21a) is a highly selective CDK9 inhibitor with significant inhibitory effect on tumor growth. CDK9-IN-24 effectively blocks cell proliferation and induces apoptosis by downregulating Mcl-1 and c-Myc, and can be used in acute myeloid leukemia research.

PB1-3 is an orally active CDK4/CDK6 inhibitor with selective antiproliferative activity against 4T1 and MCF-7 breast cancer cells. PB1-3 directly binds to CDK4 and CDK6, downregulates total protein expression, reduces Rb phosphorylation, and induces G0/G1 phase arrest. PB1-3 induces ROS accumulation, mitochondrial membrane potential collapse, initiation of mitochondria-mediated intrinsic apoptosis, upregulation of the Bax/Bcl-2 ratio, and activation of cleaved caspase-3. PB1-3 inhibits tumor growth in a 4T1 orthotopic syngeneic mouse model. PB1-3 can be used for research related to triple-negative breast cancer.

GSK3β/CDK5/CK1 IN-1 is a kinase inhibitor targeting GSK-3, CDK5, and CK1. GSK3β/CDK5/CK1 IN-1 is used in the research of cognitive, neurodegenerative, or neurological diseases or disorders.

BAY-1112054 (BAY-958) hydrochloride is a potent PTEFb/CDK9 inhibitor with high selectivity demonstrated, particularly within the CDK family. BAY-1112054 hydrochloride shows strong antiproliferative activity against cancer cell lines such as HeLa and MOLM-13. BAY-1112054 hydrochloride exhibits good metabolic stability. BAY-1112054 hydrochloride effectively inhibits tumor growth in mouse xenograft models without significant toxicity.

CDK8-IN-2 is an orally active CDK8 inhibitor of an IC₅₀ values of 0.010 μM. CDK8-IN-2 shows a CDK19 IC₅₀ value of 0.026 μM. CDK8-IN-2 inhibits phospho-STAT1, a pharmacodynamic biomarker of CDK8. CDK8-IN-2 inhibits WNT pathway activity. CDK8-IN-2 can be used for the research of colorectal carcinoma.

CDK4/6-IN-29 is an orally active and highly selective CDK4/6 inhibitor, with an IC₅₀ of 3.17 nM against CDK4 and an IC₅₀ of 4.91 nM against CDK6. CDK4/6-IN-29 induces apoptosis in non-small cell lung cancer cells, inhibits cancer cell migration, induces G1-phase cell cycle arrest, and exhibits anti-tumor efficacy in vivo. CDK4/6-IN-29 can be used for research related to non-small cell lung cancer.

CDK4-IN-5 is a potent, orally active and selective CDK4 inhibitor. CDK4-IN-5 suppresses CDK4 expression and downregulates the CDK4/CyclinD1 complex. CDK4-IN-5 induces G₀/G₁ phase cell cycle arrest in bladder cancer cells via CyclinD1 expression suppression. CDK4-IN-5 selectively exerts activity against bladder cancer cells. CDK4-IN-5 can be used for the research of bladder cancer.

CDK2/4/6-IN-3 (compound 32a) is a CDK2/4/6 inhibitor. CDK2/4/6-IN-3 can be used as a target protein ligand for the synthesis of PROTAC WWZ-11-098 (HY-181490).

JAK1/CDK7-IN-1 is a JAK1/CDK7 inhibitor. JAK1/CDK7-IN-1 forms a stable and tightly bound complex with JAK1. JAK1/CDK7-IN-1 disrupts the cell cycle, induces G₂/M phase arrest, and increases the proportion of pre-G₁ phase cells. JAK1/CDK7-IN-1 induces cellular apoptosis (apoptosis) and necrosis. JAK1/CDK7-IN-1 is applicable to research related to breast cancer and prostate cancer.

Indazole 1 is a potent CDC2-like kinase 2 (CLK2) inhibitor (IC₅₀=12.3 nM). Indazole 1 inhibits the phosphorylation of SR proteins (e.g., SRSF1, SRSF3) and modulates alternative splicing of Wnt signaling-related genes. Indazole 1 is promising for research of osteoarthritis.

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.

Rohitukine is an orally active CDK9/T1 inhibitor with an IC₅₀ of 0.3 μM. Rohitukine blocks ATP binding sites of CDK2/A and CDK9/T1, suppresses PPARγ, AKT, mTOR, C/EBPα, SREBP-2, and NF-κB signaling, and increases hepatic LXRα expression. Rohitukine induces S-phase cell cycle arrest, ROS generation, apoptosis, and exhibits anti-inflammatory activity. Rohitukine can be used for the research of leukemia, pancreatic cancer, prostate cancer, breast cancer, CNS cancer, ovarian cancer, lung cancer, dyslipidemia, inflammatory diseases, inflammatory bowel disease, and arthritis.

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.

XL413 hydrochloride (BMS-863233 hydrochloride) is an orally active, ATP-competitive, selective CDC7 kinase inhibitor. XL413 hydrochloride reduces MCM2 phosphorylation levels, decreases DNA replication origin activation, and inhibits CD69 upregulation in stimulated lymphocytes. XL-413 possesses cell-dependent antiproliferative and pro-apoptotic activities. XL413 hydrochloride attenuates ATR inhibitor-induced excessive origin activation, altered replication fork speed, and antiproliferative effects in sensitive cancer cells. XL413 hydrochloride inhibits SARS-CoV-2 infection. XL413 hydrochloride can be used for research related to cancer and SARS-CoV-2 infection.

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.