THAL-SNS-032

Catalog No.S8979 Batch:S897901

Technical Data

Formula

C₄₀H₅₂N₈O₁₀S₂

Molecular Weight

869.02

CAS No.

2139287-33-3

Solubility (25°C)*

In vitro

DMSO

100 mg/mL (115.07 mM)

Ethanol

30 mg/mL (34.52 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil	0.625mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 12.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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]

Protocol (from reference)

Cell Assay:^{^[1]}	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.

Cell Assay:^{^[1]}

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.

References

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

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

Dual Inhibition of CDK4/6 and XPO1 Induces Senescence With Acquired Vulnerability to CRBN-Based PROTAC Drugs [ Gastroenterology, 2024, S0016-5085(24)00062-3]	PubMed: 38262581

Dual Inhibition of CDK4/6 and XPO1 Induces Senescence With Acquired Vulnerability to CRBN-Based PROTAC Drugs [ Gastroenterology, 2024, S0016-5085(24)00062-3]

PubMed: 38262581

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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