CDK Degrader

Cyclin K degrader 1 is a molecular glue degrader derived from the pan-CDK inhibitor AT-7519 (HY-50940), with potent Cyclin K degrading activity and a DC₅₀ of 21 nM. Cyclin K degrader 1 binds to CDK12, mediates the formation of a CDK12-DDB1 ternary protein complex, recruits the E3 ubiquitin ligase complex, and induces ubiquitination and proteasomal degradation of Cyclin K. Cyclin K degrader 1 can be used in the research of various Cyclin K-related diseases such as cancer.

dCeMM2 (Compound 2) is a molecular glue-type degrader that targets cyclin K. dCeMM2 induces ubiquitination and degradation of cyclin K by prompting an interaction of CDK12-cyclin K with a CRL4B ligase complex.

HQ005 is a potent CCNK degrader with an DC₅₀ value of 0.041 µM. HQ005 is a molecular-glue degrader that mediates interactions between target proteins and components of the ubiquitin-proteasome system to cause selective protein degradation.

CDK2 degrader 2 (Compound I-10) is a PROTAC degrader for CDK2 that degrades CDK2 in MKN1 cell with a DC₅₀ <100 nM.

ZLY025 is a potent and orally active CCNK molecular glue degrader with an DC₅₀ of 42.7 nM. ZLY025 exhibits broad-spectrum antiproliferative activity against various tumor cells with IC₅₀ values ranging from 0.08 to 2.45 μM. ZLY025 can induce cells apoptosis and G1 phase arrest. ZLY025 can be used for the research of cancer, such as lung cancer.

(S)-CDK2 degrader 6 (Compound 8) is the S-enantiomer of CDK2 degrader 6 (HY-176444). (S)-CDK2 degrader 6 is a selective CDK2 molecular glue degrader with a DC₅₀ of 166.7 nM in 24 h. (S)-CDK2 degrader 6 can be used for breast cancer research.

PROTAC CDK2 Degrader-1 (Compound 41) is a PROTAC degrader for cyclin-dependent kinase 2 (CDK2). PROTAC CDK2 Degrader-1 inhibits the phosphorylation of RB protein in CDK2 dependent cell line OVCAR3 with an IC₅₀ of 100-500 nM.

DS17 is a molecular glue that acts as a potent degrader of cyclin K, with an EC₅₀ of 13 nM. DS17 plays an important role in cancer research.

Anticancer agent 302 (Example 1) is an anticancer agent. Anticancer agent 302 has a DC₅₀ value of 199 nM for Cyclin E1 and an IC₅₀ value of 133 nM for pRB. Anticancer agent 302 can be used for tumor research.

PROTAC FLT3/CDK9 degrader-1 is a potent FLT3 and CDK9 dual PROTAC degrader. PROTAC FLT3/CDK9 degrader-1 induces apoptosis and effective degradation of target proteins FLT3 and CDK9. PROTAC FLT3/CDK9 degrader-1 has the potential for the research of FLT3-ITD mutated AML.

Reziciclideg is a cyclin-dependent kinase (CDK) degrader and antitumor agent. Reziciclideg is applicable for cancer research.

CCNE1 degrader-1 (I-2) is a degrader targeting CCNE1. CCNE1 degrader-1 can be used in cancer-related research.

SST0116CL1 is a HSP90 inhibitor (IC₅₀: 0.21 μM). SST0116CL1 binds to the ATP binding pocket of Hsp90, and interferes with Hsp90 chaperone function thus resulting in client protein (EGFR, CDK4 and AKT) degradation. SST0116CL1 induces degradation of Her2 in BT-474 cell (IC₅₀: 0.2 μM). SST0116CL1 has antiproliferative activity and inhibits tumor growth. SST0116CL1 can be used for the study of leukemia, gastric and ovarian carcinoma.

Baleraciclideg is a Cyclin-dependent kinase degrader and antineoplastic.

(R)-PROTAC CDK9 ligand-1 (Compound 19.4) is a CDK9-targeting degrader that can be used to synthesize PROTAC with antitumor activity.