CDK Inhibitor

NU6301 is a NU6102 (a CDK2 inhibitor) (HY-15569) prodrug. NU6301 can rapidly generate NU6102 in mouse plasma. NU6301 has anticancer activity against endometrial cancer.

Cdc7-IN-21 (compound 10c) is a potent and selective Cdc7 inhibitor with an IC₅₀ of 0.07 nM. Cdc7-IN-21 can be used to study cancer.

Ulecaciclib is an orally activitive inhibitor of cyclin-dependent kinase (CDK), with K_i values of 0.62 μM (CDK2/Cyclin A), 0.2 nM (CDK4/Cyclin D1), 3 nM (CDK6/Cyclin D3), and 0.63 μM (CDK7/Cyclin H), respectively. Ulecaciclib can cross blood brain barrier and has good pharmacokinetic characteristics.

CDK12-IN-9 is a potent and selective CDK12 inhibitor with an IC₅₀ of 2.2 nM. CDK12-IN-9 inhibits pSER2 (a downstream marker of CDK12/13 activity). CDK12-IN-9 can be used for the research of cancer.

CDK2-IN-28 (compound 22) is a CDK2 inhibitor with good selectivity and cellular effects against other CDKs. CDK2-IN-28 has anti-proliferative effects on MKN1 cells (EC50: 0.31 μM).

CDK9-IN-26 (compound 1is a CDK9 inhibitor (IC₅₀=0.18 μM). .

VEGFR-2-IN-92 is a potent VEGFR-2 inhibitor (IC₅₀ = 0.208 μM). VEGFR-2-IN-92 occupies the inactive conformation of VEGFR-2 to inhibit its kinase activity, thereby disrupting the Cyclin D1-CDK4/6-Rb signaling axis and the p-FAK-related survival pathway, ultimately leading to cell cycle arrest and apoptosis in cancer cells. VEGFR-2-IN-92 can be used for research on colorectal cancer.

Cdk9 Rat Pre-designed siRNA Set A contains three designed siRNAs for Cdk9 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

Cdk5 Rat Pre-designed siRNA Set A contains three designed siRNAs for Cdk5 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

WEE1/PKMYT1-IN-4 is a selective WEE1/PKMYT1 inhibitor, with IC₅₀ values of 0.185 μM and 2.2 nM for human WEE1 and PKMYT1, respectively. WEE1/PKMYT1-IN-4 inhibits phosphorylation of CDK1 at T14 and Y15, disrupting the G2/M cell cycle checkpoint. WEE1/PKMYT1-IN-4 can be used for the research of colorectal cancer and amplified breast cancer.

ALK/PI3K/AKT-IN-1 (Compound 45) inhibits the proliferation of cancer cell A549, H1975 and PC9 with an IC₅₀ of 0.44, 0.83 and 1.51 μM. ALK/PI3K/AKT-IN-1 increases the expression of p21 and p27, inhibits the activity of CDK2 and p-Rb, arrests the cell cycle at G1 phase. ALK/PI3K/AKT-IN-1 inhibits the ALK/PI3K/AKT signaling pathway, promotes the depolarization of mitochondrial membrane potential, and inducing apoptosis in A549 cell. ALK/PI3K/AKT-IN-1 inhibits the formation and growth of A549 cell spheroids.

Cdk8 Rat Pre-designed siRNA Set A contains three designed siRNAs for Cdk8 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

(E/Z)-SU9516 is the isomer of SU9516 (HY-18629). SU9516 is a potent CDK2 inhibitor，with an IC₅₀ of 22 nM，and also shows inhibitory effects on CDK1 and CDK4，with IC₅₀s of 40，200 nM，respectively.

NUAK1-IN-2 (Compound 24) is a NUAK1 (IC₅₀ of 3.162 nM) and CDK2/4/6 inhibitor. NUAK1-IN-2 can be used in cancer, neurodevelopmental disorders and Alzheimer's disease research.

CDK12-Cyclin K Ligand-Linker Conjugates 1 is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for CDK12-Cyclin K (HY-176790) and a PROTAC linker (HY-W244922), which recruits E3 ligases. CDK12-Cyclin K Ligand-Linker Conjugates 1 can be used for synthesis of PROTAC PP-C8 (HY-144691).

CDK9-IN-44 (Compound 7) is a selective CDK9 inhibitor (IC₅₀=7.6 μM). CDK9-IN-44 inhibits CDK9/cyclin T1 kinase activity, blocking transcriptional elongation, reducing the expression of pro-cancer proteins (such as MCL1, c-MYC), and inducing tumor cell apoptosis. CDK9-IN-44 is promising for research of glioblastoma (GBM) and central nervous system (CNS) disorders.

CDK2-IN-51 is a pyrazolopyridine derivative, a CDK2 inhibitor with an IC₅₀ of 23.47 nM. CDK2-IN-51 does not have a pro-apoptotic effect and had no significant effect on CDK2 protein expression. CDK2-IN-51 reduces expression of DNA replication factors (Polα, MCM7, ORC2, and ORC4) and pre-G1 cell cycle arrest. CDK2-IN-51 can be used for the research of colorectal cancer.

CLK1/2-IN-2 is CLK1 and CLK2 inhibitor with IC₅₀ values of 1.1 nM and 2.4 nM, respectively. CLK1/2-IN-2 exhibits potent anti-cancer activities^[1].

Cdk16 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Cdk16 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

Carbonic anhydrase-IN-35 is a selective carbonic anhydrase (CA) inhibitor. Carbonic anhydrase-IN-35 potently inhibits tumor-associated hCA IX (K_i = 0.6 nM) and hCA XII (K_i = 2.2 nM). Carbonic anhydrase-IN-35 induces apoptosis in MCF-7 cells by elevating Bax, reducing Bcl-2, and downregulating CDK4/6. Carbonic anhydrase-IN-35 exhibits potent cytotoxicity against MCF-7 (IC₅₀ = 0.3975 μM normoxic/0.6575 μM hypoxic), MCF-7-ADR (IC₅₀> = 0.3975 μM normoxic/4.488 μM hypoxic), MDA-MB-231, and 4T1 breast cancer cells. Carbonic anhydrase-IN-35 can be used for the study of breast cancer.