CDK Inhibitor

CP-10 is a PROTAC connected by ligands for Cereblon and CDK, with highly selective, specific, and remarkable CDK6 degradation (DC₅₀=2.1 nM). It inhibits proliferation of several haematopoietic cancer cells with impressive potency including multiple myeloma, and can still degrades mutated and overexpressed CDK6.

Lerociclib (G1T38) is a potent and selective inhibitor of CDK4/6, with IC₅₀s of 1 nM, 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.

CDK5-IN-3 is a CDK5 inhibitor. CDK5-IN-3 exhibits an IC₅₀ of 0.6 μM against CDK5/p25, with a 30-fold selectivity over CDK2/CycA. CDK5-IN-3 can be used for research on CDK5-related diseases, such as autosomal dominant polycystic kidney disease.

CC-671 is a dual TTK protein kinase/CDC2-like kinase (CLK2) inhibitor with IC₅₀s of 0.005 and 0.006 μM for TTK and CLK2, respectively.

Tabersonine is a selective, orally active NLRP3 inhibitor. Tabersonine directly binds to the NACHT domain of NLRP3, inhibiting its ATPase activity and oligomerization, thereby blocking ASC spot formation and caspase-1 activation, and reducing the release of pro-inflammatory cytokines such as IL-1β. Tabersonine also inhibits K63-linked ubiquitination of TRAF6, blocking NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. Tabersonine can inhibit inflammatory responses, induce apoptosis of liver cancer cells through mitochondrial pathways and death receptor pathways, reduce mitochondrial membrane potential, promote cytochrome c release, and activate caspase proteins. Tabersonine is mainly used in the study of NLRP3-driven inflammatory diseases (such as acute lung injury, sepsis, peritonitis) and tumors such as liver cancer.

K00546 is a potent CDK1 and CDK2 inhibitor with IC₅₀s of 0.6 nM and 0.5 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. K00546 is also a potent CDC2-like kinase 1 (CLK1) and CLK3 inhibitor with IC₅₀s of 8.9 nM and 29.2 nM, respectively.

Leucettinib-92 (compound 92) is an inhibitor of DYRK/CLK kinase, The IC₅₀s are 147 nM (CLK1), 39 nM (CLK2), 5.2 nM (CLK4), 0.8 μM (CLK3), 124 nM (DYRK1A), 204 nM (DYRK1B), 0.16 μM (DYRK2), respectively. 1.0 μM (DYRK3), 0.52 μM (DYRK4), 2.78 μM (GSK3).

Tudociclib is a CDK2 inhibitor with an IC₅₀ value ≤20 nM. Tudociclib modulates CDK2 activity to influence cell cycle regulation. Tudociclib can be used for the research of cancer.

Abemaciclib metabolite M20 (LSN3106726), the active metabolite of Abemaciclib, is a selective CDK4/6 inhibitor for the treatment of cancer.

β-catenin-IN-3 (Compound C2) is a selective β-catenin inhibitor. β-catenin-IN-3 binds to allosteric site on the surface of β-catenin with K _D calculated at 54.96 nM. β-catenin-IN-3 selectively inhibits β-catenin via targeting a cryptic allosteric modulation site, lowers its cellular load. β-catenin-IN-3 significantly reduces viability of β-catenin driven cancer cells, and triggers β-catenin degradation via proteasome system in β-catenin-overexpressing cancer cells.

LDC4297 is a selective inhibitor of CDK7 with an IC₅₀ value of 0.13 nM. LDC4297 inhibits human cytomegalovirus (HCMV) replication with an EC₅₀ value of 24.5 nM. LDC4297 shows broad antiviral activities to Herpesviridae, Adenoviridae, Poxviridae, Retroviridae and Orthomyxoviridae with EC₅₀ value of 0.02-1.21 μM. LDC4297 can be used for the research of infection.

Abemaciclib (Standard) is the analytical standard of Abemaciclib. This product is intended for research and analytical applications. Abemaciclib (LY2835219) is a selective and BBB-permeable CDK4/6 inhibitor with IC₅₀ values of 2 nM and 10 nM for CDK4 and CDK6, respectively.

Briciclib (ON 014185) is a eukaryotic translation initiation factor 4E (eIF4E) inhibitor. Briciclib exhibits broad-spectrum anti-cancer activity, including in mantle cell leukemia, breast cancer, gastric cancer, and esophageal cancer cells. Briciclib reduces the expression of cyclin D1 and c-Myc, and enhances the expression of P53 and Cleaved Caspase 3 pro-apoptotic proteins. Briciclib can be used for the study of hematological system tumors and solid tumors.

AS2863619 free base is an orally active CDK8/19 inhibitor that also inhibits BMP2, MDA5 and RIG-I receptors. AS2863619 free base targets Stat5a-CDK8/19 to promote the differentiation of CD4⁺ T cells into regulatory T cells and induce FOXP3 expression, thereby restoring immune homeostasis and establishing transplant immune tolerance. AS2863619 free base also enhances the BMP2/SMAD signaling pathway to promote osteogenic differentiation and inhibit adipogenic differentiation. AS2863619 free base exerts osteoprotective effects by alleviating inflammation-induced impairment of osteogenic function and inducing neutrophil apoptosis (apoptosis). AS2863619 free base can be applied to research in related fields such as periodontitis-induced bone defects.

Vevorisertib trihydrochloride (ARQ 751 trihydrochloride) is an orally active allosteric AKT inhibitor that blocks AKT phosphorylation. Vevorisertib trihydrochloride inhibits tumor cell proliferation through Cyclin D1 and Ki67. Vevorisertib trihydrochloride inhibits liver fibrosis through collagen accumulation, alpha-SMA, COL1, and TGF-beta. Vevorisertib trihydrochloride reduces total bilirubin. Vevorisertib trihydrochloride significantly reduces tumor size in a cirrhotic rat HCC model. Vevorisertib trihydrochloride can be used for research on hepatocellular carcinoma.

FMF-06-098-1 is a multi-target kinase PROTAC degrader. FMF-06-098-1 can be used to target degradation kinases which degrades AAK1, AΒL2, AURKA, AURKB, BUBIB, CDC7, CDK1, CDK12, CDK13, CDK2, CDK4, CDk6, CDK7, CDK9, CHEK1, CSNKID, EPHA1, PER, FGFR1, GAK, IRAK4, ITK, LIMK2, MAP4K2, MAP4K3, MAPK6, MAPK7, MARK4, MELK, PKN3, PLK4, PRKAA1, PTK2, PTK6, RPS6KA4, S1K2, STK35, TNK2, UHMK1, ULK1, and WEE1.

PKCζ-IN-1 is a PKCζ-selective inhibitor with an IC₅₀ of 5.18 nM against human PKCζ. PKCζ-IN-1 also inhibits CDK2 with an IC₅₀ of 1.04 μM. PKCζ-IN-1 is applicable to research related to immune and inflammatory diseases.

SGC-CLK-1, a chemical probe, is a potent and selective inhibitor of Cdc2-like kinases CLK1, CLK2, and CLK4. SGC-CLK-1 can inhibit the growth of melanoma and glioblastoma cells.

JH-XI-10-02 is a PROTAC connected by ligands for Cereblon and CDK. JH-XI-10-02 is a highly potent and selective PROTAC CDK8 degrader, with an IC₅₀ of 159 nM. JH-XI-10-02 causes proteasomal degradation, does not affect CDK8 mRNA levels. JH-XI-10-02 shows no effect on CDK19.

PROTAC CDK9 Degrader-1 is a PROTAC connected by ligands for Cereblon and CDK as a selective CDK9 degrader.