2809353-52-2
Chemical Structure
LL-K9-3
- CAS No.: 2809353-52-2
- Formula:C31H49N5O6S3
- Molecular Weight:683.95
InChIKey: NPRIWHDFWDSJRZ-YFNKSVMNSA-N
SMILES: O=S(CCNC(CO[C@H]1[C@@H](CC[C@H](C1)C)C(C)C)=O)(N2CCC(CC2)C(NC3=NC=C(SCC4=NC=C(C(C)(C)C)O4)S3)=O)=O
Biological Activity: LL-K9-3 is a selective CDK9-cyclin T1 HyT degrader, with DC50 values of 0.662 μM and 0.589 μM for CDK9 and Cyclin T1, respectively. LL-K9-3 lacks an E3 ligand moiety and induces polyubiquitination and proteasome-mediated synchronous degradation of CDK9 and cyclin T1 via a hydrophobic tag-mediated mechanism. LL-K9-3 downregulates the protein levels of androgen receptor (AR) and c-Myc, and exhibits antiproliferative and pro-apoptotic (apoptosis) activity in prostate cancer cells. LL-K9-3 can be used in studies related to prostate cancer[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
LL-K9-3 | 98.90% | LL-K9-3 is a selective CDK9-cyclin T1 HyT degrader, with DC50 values of 0.662 μM and 0.589 μM for CDK9 and Cyclin T1, respectively. LL-K9-3 lacks an E3 ligand moiety and induces polyubiquitination and proteasome-mediated synchronous degradation of CDK9 and cyclin T1 via a hydrophobic tag-mediated mechanism. LL-K9-3 downregulates the protein levels of androgen receptor (AR) and c-Myc, and exhibits antiproliferative and pro-apoptotic (apoptosis) activity in prostate cancer cells. LL-K9-3 can be used in studies related to prostate cancer. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
References
- [1]. Li J, et al. Discovery of Small-Molecule Degraders of the CDK9-Cyclin T1 Complex for Targeting Transcriptional Addiction in Prostate Cancer. Journal of medicinal chemistry. 2022 Aug 25;65(16):11034-11057. [Content Brief]
- [2]. Lin R, et al. Discovery of HyT-Based Degraders of CDK9-Cyclin T1 Complex. Chemistry & biodiversity. 2023 Aug;20(8):e202300769. [Content Brief]
