YJ9069

YJ9069 is a selective CDK12/CDK13 PROTAC degrader with an IC50 of 22.22 nM for in VCaP cells. CDK12/13 degradation rapidly triggers gene-length-dependent transcriptional elongation defects, leading to DNA damage and cell-cycle arrest. YJ9069 effectively inhibits proliferation in subsets of prostate cancer cells and significantly suppresses prostate tumor growth. (Pink: CDK12/CDK13 degradation agent (HY-168658) ; Black: Linker (HY-W015967) ; Blue: ligand for E3 ligase (HY-103596) ) [1].

Product Specifications

UNSPSC

12352005

Target

CDK; DNA/RNA Synthesis; PROTACs

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; PROTAC

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/yj9069.html

Purity

97.63

Solubility

DMSO : ≥ 50 mg/mL

Smiles

O=C(NCC1=CC=CC=C1)N(C2=CN=C(N3CCN(C(COC4=C5C(C(N(C6CCC(NC6=O)=O)C5=O)=O)=CC=C4)=O)CC3)C=C2)[C@H](CC7)CC[C@@H]7NC8=NC=C9C(C=CC=C9)=N8

Molecular Formula

C46H46N10O7

Molecular Weight

850.92

References & Citations

[1]Yu Chang, et al. Development of an orally bioavailable CDK12/13 degrader and induction of synthetic lethality with AKT pathway inhibition. Cell Rep Med. 2024 Oct 15;5 (10) :101752.