THAL-SNS-032

Research use only, not for human use.

THAL-SNS-032 is a novel CDK9 degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN).

THAL-SNS-032 is a novel CDK9 degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN); efficiently induces complete CDK9 degradation at 250 nM (6h treatment), inhibits proliferation of MOLT4 cells at lower concentrations (IC50 = 50 nM) than SNS-032 (IC50=173 nM), exhibits more potent inhibition of proliferation than SNS-032 across a panel of 11 different leukemia cancer cell lines; induces rapid degradation of CDK9 without affecting the levels of other SNS-032 targets, and has prolonged cytotoxic effects.

——

——

THAL SNS 032 | CDK9 PROTAC degrader

PROTACs

PROTAC

PROTAC

——

——

2139287-33-3

869.022

C40H52N8O10S2

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (115.07 mM)

O=C(C1CCN(CC(NCCOCCOCCOCCNC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)=O)CC1)NC5=NC=C(SCC6=NC=C(C(C)(C)C)O6)S5

N-(5-(((5-(tert-butyl)oxazol-2-yl)methyl)thio)thiazol-2-yl)-1-(14-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)-2-oxo-6,9,12-trioxa-3-azatetradecyl)piperidine-4-carboxamide

(-20℃)

With Ice Pack

≥ 2 years