3054009-82-1
Chemical Structure
KI-CDK9d-32
- CAS No.: 3054009-82-1
- Formula:C39H45N9O4
- Molecular Weight:703.83
InChIKey: DQQMOQXMKRXELC-XMOVUWPTSA-N
SMILES: O=C(N[C@H]1C[C@H](NC2=CC(CCC)=NC3=CC=NN23)CC1)C4=CC=C(CN5CCN(C6=CC7=C(C(N(C(CC8)C(NC8=O)=O)C7)=O)C=C6)CC5)C=C4
Biological Activity: KI-CDK9d-32 is a selective CDK9 PROTAC degrader (IC50 = 3 nM; DC50 = 0.89 nM). KI-CDK9d-32 induces CDK9 degradation via the ubiquitin-proteasome pathway to abrogates CDK9 enzymatic and scaffolding functions, downregulates MYC expression and MYC-dependent signaling, represses TNF-alpha signaling pathways activity and pre-rRNA levels. KI-CDK9d-32 disrupts nucleolar homeostasis, blocks cell cycle progression and cellular translation by reducing 4EBP1 phosphorylation, and elicits cancer cell cytotoxicity in a CRBN-dependent manner, while high ABCB1 activity attenuates the efficacy. KI-CDK9d-32 can be used for the research of acute lymphoblastic leukemia, rhabdomyosarcoma, pancreatic adenocarcinoma[1].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
KI-CDK9d-32 | 99.03% | KI-CDK9d-32 is a selective CDK9 PROTAC degrader (IC50 = 3 nM; DC50 = 0.89 nM). KI-CDK9d-32 induces CDK9 degradation via the ubiquitin-proteasome pathway to abrogates CDK9 enzymatic and scaffolding functions, downregulates MYC expression and MYC-dependent signaling, represses TNF-alpha signaling pathways activity and pre-rRNA levels. KI-CDK9d-32 disrupts nucleolar homeostasis, blocks cell cycle progression and cellular translation by reducing 4EBP1 phosphorylation, and elicits cancer cell cytotoxicity in a CRBN-dependent manner, while high ABCB1 activity attenuates the efficacy. KI-CDK9d-32 can be used for the research of acute lymphoblastic leukemia, rhabdomyosarcoma, pancreatic adenocarcinoma. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||