THAL SNS 032

THAL-SNS-032 is a selective CDK9 degrader. THAL-SNS-032 consists of a CDK-binding SNS-032 ligand linked to a thalidomide.

Product information

CAS Number: 2139287-33-3

Molecular Weight: 869.02

Formula: C40H52N8O10S2

Chemical Name: 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

Smiles: CC(C)(C)C1=CN=C(CSC2=CN=C(NC(=O)C3CCN(CC(=O)NCCOCCOCCOCCNC4=CC=CC5=C4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)S2)O1

InChiKey: BXDZOYLPNAIDOC-UHFFFAOYSA-N

InChi: InChI=1S/C40H52N8O10S2/c1-40(2,3)29-21-43-32(58-29)24-59-33-22-44-39(60-33)46-35(51)25-9-13-47(14-10-25)23-31(50)42-12-16-56-18-20-57-19-17-55-15-11-41-27-6-4-5-26-34(27)38(54)48(37(26)53)28-7-8-30(49)45-36(28)52/h4-6,21-22,25,28,41H,7-20,23-24H2,1-3H3,(H,42,50)(H,44,46,51)(H,45,49,52)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: 100 mg/mL(115.07 mM). Water: Insoluble.

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

THAL-SNS-032 is a selective CDK9 degrader consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative which binds the E3 ubiquitin ligase Cereblon (CRBN). THAL-SNS-032 induces rapid degradation of CDK9 without affecting the levels of other SNS-032 targets. The transcriptional changes elicited by THAL-SNS-032 are more like those caused by NVP-2 than those induced by SNS-032. Strikingly, compound washout does not significantly reduce levels of THAL-SNS-032-induced apoptosis, suggesting that CDK9 degradation had prolonged cytotoxic effects compared to CDK9 inhibition.

References:

1. Calla M Olson, et al. Nat Chem Biol. 2018 Feb;14(2):163-170.

Products are for research use only. Not for human use.