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 that binds the E3 ubiquitin ligase Cereblon (CRBN).

THAL-SNS-032 Chemical Structure

THAL-SNS-032 Chemical Structure

CAS No. 2139287-33-3

Purity & Quality Control

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

THAL-SNS-032 Related Products

Signaling Pathway

CDK Signaling Pathways

CDK Signaling Pathway

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 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 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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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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