Home Cell Cycle CDK inhibitor - PROTAC inhibitor - E3 Ligase inhibitor THAL-SNS-032 For research use only.

THAL-SNS-032

THAL-SNS-032 is a selective Cyclin-dependent kinase 9 (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 Chemical Structure

THAL-SNS-032 Chemical Structure

CAS: 2139287-33-3

Selleck's THAL-SNS-032 has been cited by 1 publication

Purity & Quality Control

Batch: S897901 DMSO] 100 mg/mL] false] Ethanol] 30 mg/mL] false] Water] Insoluble] false Purity: 99.30%
99.30

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Biological Activity

Description THAL-SNS-032 is a selective Cyclin-dependent kinase 9 (CDK9) degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN).
Targets
CDK9 [1] CRBN [1]
In vitro
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.[1]
Cell Research Cell lines Wildtype MOLT4 cells, CRBN−/− MOLT4 cells
Concentrations 250nM
Incubation Time 6 h, 72 h
Method

Proliferation assays are performed by treating MOLT4 and CRBN−/− MOLT4 cells with THAL-SNS-032 at concentrations indicated for 72 hours. Anti-proliferative effects of compounds are assessed using Cell Titer Glo assay kit. IC50s are determined using Graphpad Prism non-linear regression curve fit. To determine the effect of washout, MOLT4 and CRBN−/− MOLT4 cells are treated with 250nM THAL-SNS-032. After 6 hours, compound is washed from cells by washing cells with media three times where indicated. Cells are allowed to grow for another 66 hours (72-hour total) and assayed for anti-proliferation using Cell Titer Glo assay kit.

Chemical Information & Solubility

Molecular Weight 869.02 Formula

C40H52N8O10S2
CAS No. 2139287-33-3 SDF --
Smiles CC(C)(C)C1=CN=C(O1)CSC2=CN=C(S2)NC(=O)C3CCN(CC3)CC(=O)NCCOCCOCCOCCNC4=CC=CC5=C4C(=O)N(C5=O)C6CCC(=O)NC6=O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (115.07 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 30 mg/mL

Water : Insoluble


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In vivo
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