cdk in 6

CDK-IN-6, a pyrazolo[1,5-a]pyrimidine compound, exhibits potent anticancer activities as a CDK inhibitor[1].

CDK4/6/1 Inhibitor (Crozbaciclib) is a type of CDK4/6 inhibitor (IC50s: 3 and 1 nM). CDK4/6 inhibitor is a class of compounds used for the treatment of some types of hormone receptor positive, HER2-negative breast cancer, which can block the process of breast cancer cell division and reproduction.

CDK4/6-IN-2 is a potent inhibitor of CDK4 and CDK6 [IC50s: 2.7 and 16 nM].

CDK4/6-IN-3, a brain-penetrant CDK4/CDK6 inhibitor (Kis: <0.3 nM and 2.2 nM), is used for the treatment of glioblastoma and inhibits CDK1 with a Ki of 110 nM.

CDK4/6/HDAC-IN-1 (Compound N14) is a dual-target inhibitor of CDK4/6 and HDAC, with IC50 values of 7.23 nM for CDK4, 13.20 nM for CDK6, 55.66 nM for HDAC1, and 48.38 nM for HDAC6. It induces apoptosis and G0/G1 phase arrest through the HDAC-p21-CDK signaling pathway and can inhibit hepatocellular carcinoma.

CDK7-IN-6 is a highly effective and specific inhibitor (IC50 ≤100 nM) of cyclin-dependent kinase 7 (CDK7). It showcases remarkable selectivity, with more than a 200-fold preference for CDK7 over CDK1, CDK2, and CDK5. This compound holds significant potential for cancer research purposes.

CDK4/6-IN-5 is a highly effective inhibitor of CDK4 and CDK6, with Ki values of 0.2 nM for CDK4/Cyclin D1 and 4.4 nM for CDK6/Cyclin D3 (WO2019207463A1, example A93).

CDK6/9-IN-1 (compound 66) is a potent, orally administered dual inhibitor of CDK6 and CDK9, with IC50 values of 40.5 nM and 39.5 nM, respectively.

CDK12-IN-6, a pyrazolotriazine compound, is a powerful inhibitor of CDK12. Its inhibitory activity is significant with an IC50 value of 1.19 μM when tested at high ATP concentration (2 mM). Notably, CDK12-IN-6 does not exhibit any inhibitory effect on CDK2/Cyclin E (IC50 >20 μM) and CDK9/Cyclin T1 (IC50 >20 μM) when tested under the same high ATP conditions (2 mM) (WO2021116178A1).

CDK4/6-IN-14 is a potent, highly selective inhibitor of Cyclin-Dependent Kinases 4 and 6 (CDK4/6), with inhibition concentrations (IC50s) of 10 nM and 16 nM, respectively. It shows over 60-fold selectivity for CDK4/6 compared to CDKs 1, 2, 7, and 9, and exhibits significant selectivity against 205 other kinases.

CDK6-IN-1 (compound 4i) is an inhibitor of CDK6 that suppresses cell growth and induces cell cycle arrest at the G1 phase.

CDK1-IN-6 (Ligand 3) is an effective inhibitor of CDK1 and shows potential for use in cancer research.

CDK4/6-IN-23 (Compound 42) is a potent and selective inhibitor of CDK4/6, displaying an IC50 of 11 nM for CDK6. This compound significantly activates immune cells and enhances IL-3 production. In mice undergoing 5-FU chemotherapy, CDK4/6-IN-23 demonstrates dual bone marrow protection and immunomodulatory effects.

CDK4/6-IN-24 (Compound A) is an inhibitor of CDK4/6 with broad-spectrum antitumor activity. It can effectively inhibit various cancer cells, exhibiting an IC50 in the submicromolar range.

CDK4/6/BRD4-IN-1 (B15) is an inhibitor targeting CDK4, CDK6, and BRD4, with IC50 values of 220 nM for BRD4-BD2, 146 nM for BRD4-BD1, 106 nM for CDK6, and 85 nM for CDK4. This compound is applicable for research in non-small cell lung cancer (NSCLC) and can induce cell cycle arrest and apoptosis.

CDK2 degrader6 (compound 6) is an orally active CDK2 degrader with a DC50 of 46.5 nM, and is applicable in breast cancer research.

CDK4/6-IN-15 hydrochloride is an orally active selective inhibitor of CDK4/6. It effectively restrains the growth of cancer cells by arresting the cell cycle at the G1 phase. Additionally, CDK4/6-IN-15 hydrochloride inhibits phosphorylation of the retinoblastoma tumor suppressor protein (Rb) at site S780 and suppresses E2 factor (E2F)-regulated gene expression.

CDK6/PIM1-IN-1 (Compound 51) hydrochloride is an orally active and potent dual inhibitor of CDK6 and PIM1, with IC50 values of 39 nM and 88 nM, respectively. It also inhibits CDK4 with an IC50 of 3.6 nM. This compound significantly suppresses the proliferation of acute myeloid leukemia (AML) cells, arrests the cell cycle at the G1 phase, and induces apoptosis. CDK6/PIM1-IN-1 hydrochloride demonstrates anti-AML activity.

CDK6/9-IN-2 is a highly potent dual inhibitor of CDK6 (IC50 = 15 nM) and CDK9 (IC50 = 22 nM) with selectivity over CDK2, CDK8, and CDK11. It suppresses proliferation in IFN-γ/TNF-α-induced HaCaT cells and inhibits the STAT3 pathway and expression of inflammatory factors. CDK6/9-IN-2 alleviates psoriasis dermatitis and is applicable in psoriasis research.

(R)-CDK2 degrader 6 (Compound 7) is the R enantiomer of CDK2 degrader 6. It functions as a selective molecular glue degrader for CDK2, with a DC50 of 27.0 nM within 24 hours. This compound can be utilized in breast cancer research.

(S)-CDK2 degrader 6 (Compound 8) is the S-enantiomer of CDK2 degrader 6. This selective CDK2 molecular glue degrader has a DC50 of 166.7 nM within 24 hours and is applicable in breast cancer research.

PROTACCDK6ligand 2 is a ligand specifically targeting the CDK6 protein, playing a crucial role in forming the PROTACCDK6 Degrader1.

PROTACCDK4/6/9 degrader 2 (Compound P4) is an orally active and low-toxicity PROTAC prodrug targeting CDK4/6/9. It significantly inhibits tumor growth and reduces lung metastasis of tumors. This compound is applicable in cancer research, including studies on breast cancer.

PROTACCDK4/6/9 degrader 1 is a PROTAC degrader targeting CDK4/6/9. It effectively degrades CDK4, CDK6, and CDK9 within triple-negative breast cancer (TNBC) cells, thereby inhibiting their proliferation. Additionally, PROTACCDK4/6/9 degrader 1 induces G1 phase arrest, promotes apoptosis, and suppresses cell migration and invasion in TNBC cells. This compound is useful for researching triple-negative breast cancer (TNBC).