CDK Degrader

BSJ-5-63 is a potent CDK12, CDK7, CDK9 PROTAC degrader. BSJ-5-63 BSJ-5-63 decreases the protein expression of CDK12, CDK7, CDK9, RNAPII, Cyclin K. BSJ-5-63 decreases the mRNA expression of BRCA1, BRCA2. BSJ-5-63 shows anticancer activity and has the potential for the research of prostate cancer.

BSJ-02-162 (CDK4/6-IN-11) is a CDK4/CDK6 and IKZF1/IKZF3 degrader, with DC₅₀ values of 32 nM and 6.1 nM against CDK4 and CDK6, respectively; its IC₅₀ ranges from 1 to 50 nM. BSJ-02-162 induces G1-phase cell cycle arrest, reduces phosphorylated retinoblastoma protein levels, and exerts antiproliferative activity in mantle cell lymphoma cells. BSJ-02-162 is applicable to research related to mantle cell lymphoma.

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.

TMX-2172 is a selective bivalent cereblon-recruiting PROTAC-based dual CDK2 and CDK5 degrader with IC₅₀ values of 6.5 nM and 6.8 nM, respectively. TMX-2172 shows selectivity for CDK2 and CDK5 over other cell cycle CDKs (CDK1, CDK4, and CDK6) and transcriptional CDKs (CDK7 and CDK9). TMX-2172 inhibits CDK2/CDK5 enzymatic activity, induces their proteasomal degradation, reduces ASCL1 protein levels and half-life, induces cancer cell death, and exerts antiproliferative effects. TMX-2172 can be used for the research of ovarian cancer and small cell lung cancer.

CDK4 degrader 1 is a selective CDK4 molecular glue degrader. CDK4 degrader 1 induces intracellular CDK4 degradation, and its activity is dependent on DCAF16. CDK4 degrader 1 targets the cysteine residue on DCAF16 through its vinylsulfonylpiperazine domain, thereby mediating the degradation of CDK4. CDK4 degrader 1 can be used in research related to cervical cancer.

CDK2 degrader 5 is a CRBN-binding CDK2 molecular glue degrader. CDK2 degrader 5 induces ubiquitination and subsequent proteasomal degradation of CDK2. CDK2 degrader 5 can be used for the research of cancer.

ZLC491 is an orally active PROTAC degrader that selectively targets CDK12/CDK13 and exhibits certain oral bioavailability. ZLC491 induces cereblon- and proteasome-dependent selective degradation of CDK12 and CDK13. ZLC491 inhibits the transcription and expression of long genes, and mainly acts on a subset of DNA damage response genes. ZLC491 inhibits the proliferation of various triple-negative breast cancer cells. ZLC491 can be used in research related to triple-negative breast cancer.

CPD-10 is a potent CCND1 and CDK4 PROTAC degrader. CPD-10 exhibits anti-proliferative effects on tumor cells and can also induce apoptosis. CPD-10 can be used for the study of breast cancer and lung cancer.

CDK8 ligand 1 is the ligand of CDK8. CDK8 ligand 1 can be used to synthesize LL-K8-22 (HY-149209).

dCeMM4 is a Cyclin K Molecular glue degrader. dCeMM4 mediates the direct interaction between CDK12:cyclin K and the CRL4B ligase complex, thereby driving the ubiquitination and proteasomal degradation of Cyclin K. dCeMM4 induces Apoptosis without cell cycle phase-specific arrest. dCeMM4 exhibits synergistic activity with DNA damage inducers, and a correlation exists between Cyclin K degradation and cellular sensitivity. dCeMM4 can be used in studies related to T-cell malignancies.

PROTAC CDK12/13 Degrader-1 (7f) is a highly selective cell cycle protein-dependent kinase CDK12/CDK13 dual degrader with the DC₅₀ values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 has anti-proliferative activity and can be used in breast cancer research.

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.

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.

SB1-G-187 is a multi-target kinase PROTAC degrader with activity against various kinases including GCK, YES1, IRAK1 and LYN. SB1-G-187 induces degradation of target kinases via a p97-dependent pathway, and forms ternary complexes with CRBN and specific functional kinases. SB1-G-187 can be used in tumor-related research.

PROTAC CDK9 degrader-9 is an orally active, selective CDK9 PROTAC degrader with a DC₅₀ of 3.94 nM. PROTAC CDK9 degrader-9 downregulates downstream targets c-Myc and MCL-1. PROTAC CDK9 degrader-9 inhibits the proliferation of breast cancer cells. PROTAC CDK9 degrader-9 can be used for the research of triple-negative breast cancer.

CDK7 ligand 2 (Compound A6) is a CDK7 ligand. CDK7 ligand 2 can be used in the synthesis of PROTACs.

(S)-JWZ-5-13 (compound 17-Neg), a PROTAC CDK7 degrader, is a negative control compound of JWZ-5-13 (HY-161828). (S)-JWZ-5-13 displays similar in vitro CDK7 inhibition (IC₅₀ = 21.1 nM) to JWZ-5-13, but fails to induce CDK7 degradation in cells.

PROTAC CDK9 degrader-2 is a PROTAC degrader targeting CDK9, with an IC₅₀ of 523 nM. PROTAC CDK9 degrader-2 selectively degrades CDK9 via the cereblon-dependent ubiquitin-proteasome pathway and inhibits the proliferation of cancer cells overexpressing CDK9. PROTAC CDK9 degrader-2 can be used for cancer research.

PROTAC CDK9 degrader-4 is a selective PROTAC CDK9 degrader. PROTAC CDK9 degrader-4 exhibits antiproliferative, pro-apoptotic and in vivo tumor growth inhibitory activities. PROTAC CDK9 degrader-4 can be used for the research of triple-negative breast cancer.