THAL SNS 032

Name: THAL SNS 032
Brand: Tocris Bioscience
SKU: 6532

Catalog # 6532 | Tocris Bioscience a Bio-Techne Brand

Citations (2)

COA / SDS

Potent and selective Cdk9 Degrader (PROTAC®)

Key Product Details

Description:	Potent and selective Cdk9 Degrader (PROTAC^®)
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
Purity:	≥98% (HPLC)
Molecular Weight:	869.02

View Full Technical Details for THAL SNS 032

Technical Data
Citations (2) / Reviews

Biological Activity for THAL SNS 032

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.

PROTAC^® is a registered trademark of Arvinas Operations, Inc., and is used under license.

Licensing Information

Sold under license from Dana-Farber Cancer Institute.

Scientific Data Examples 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.

Technical Data for THAL SNS 032

M. Wt	869.02
Formula	C₄₀H₅₂N₈O₁₀S₂
Storage	Store at -20°C
Purity	≥98% (HPLC)
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for THAL SNS 032

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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 will 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

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References for THAL SNS 032

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

Citations for THAL SNS 032 (2)

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Citations are publications that use Bio-Techne products. Selected citations for THAL SNS 032 include:

Kaji et al. (2020) Characterization of cereblon-dependent targeted protein degrader by visualizing the spatiotemporal ternary complex formation in cells Sci Rep. 10:3088
PMID: 32080280
Vladimir et al. (2020) CDK9 activity is critical for maintaining MDM4 overexpression in tumor cells. Cell Death Dis. 11:754
PMID: 32934219

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