THAL SNS 032
Tocris Bioscience, part of Bio-Techne | Catalog # 6532
Potent and selective Cdk9 Degrader (PROTAC®)
Key Product Details
Description
Potent and selective Cdk9 Degrader (PROTAC®)
Product Description
THAL SNS 032 is a degrader (PROTAC®) comprising the cyclin-dependent kinase inhibitor SNS 032 (Cat. No. 4075) conjugated to the cereblon E3 ligase ligand, thalidomide (Cat. No. 0652). Potent, selective and cereblon-dependent degrader of Cdk9 (EC50 = 4 nM). Displays >15-fold selectivity for Cdk9 over other CDKs (EC50 values are 62, 171 and 398 nM for Cdk2, Cdk1 and Cdk7, respectively). Induces complete degradation of Cdk9 at 250 nM in MOLT4 cells. Inhibits proliferation of leukemia cell lines.Cdk9 antibodies validated for Western Blot also available: Catalog # NBP2-15848 and NBP3-15345.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Scientific Data Images for THAL SNS 032
Application of THAL SNS 032 in MOLT-4 cells.
Western Blot data showing knockdown of both CDK9 isoforms after THAL SNS 032 treatment of MOLT-4 cells (4 h incubation). Protein quantification (relative to DMSO-only control) is shown beneath the corresponding lane. Cdk9 primary antibody is used at 1:1000 dilution. Secondary is Anti-Rabbit HAF008, 1:1000, R&D Systems. GAPDH primary antibody is R&D Systems AF5718 used at 5μg/mL. Secondary is Anti-Goat HAF017, 1:1000, R&D Systems.Data courtesy of Jeff Cooper, Bio-Techne.Licensing Information
Sold under license from Dana-Farber Cancer Institute.Product Specifications
Molecular Weight
869.02
Formula
C40H52N8O10S2
Storage
Store at -20°C
Purity
≥98% (HPLC)
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
CAS Number
2139287-33-3
PubChem ID
131801483
InChI Key
BXDZOYLPNAIDOC-UHFFFAOYSA-N
SMILES
CC(C)(C1=CN=C(O1)CSC2=CN=C(S2)NC(C3CCN(CC3)CC(NCCOCCOCCOCCNC4=C5C(N(C(C5=CC=C4)=O)C6CCC(NC6=O)=O)=O)=O)=O)C
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 86.9 | 100 |
Preparing Stock Solutions
for THAL SNS 032
The following data is based on the product molecular weight 869.02
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.75 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.30 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Olson Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation. Nat.Chem.Biol. 2018 PMID: 29251720
Product Specific Notices for THAL SNS 032
For research use only
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