Art. -Nr.: HY-123937

THAL-SNS-032

10 Cited Publications

Kundenbewertung

Based on 10 publication(s) in Google Scholar

THAL-SNS-032 is a selective CDK9 PROTAC degrader. THAL-SNS-032 recruits CRBN to form a ternary complex with CDK9, thereby triggering ubiquitination and proteasomal degradation of CDK9. THAL-SNS-032 also induces the degradation of CDK1, CDK2 and CDK7. THAL-SNS-032 elevates pH2AX levels, reduces MCL1s expression, and activates caspase-3. THAL-SNS-032 induces cancer cell apoptosis, regulates transcription, and inhibits the replication of human cytomegalovirus (CMV) and SARS-CoV-2. THAL-SNS-032 can be used in research related to breast cancer, leukemia, cytomegalovirus infection and SARS-CoV-2 infection.
(Pink: CDK9 ligand (HY-10008); Blue: Cereblon ligand (HY-14658); Black: linker (HY-W015088)).

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Reinheit: 97.11%
CAS. Nr.: 2139287-33-3
Formel: C₄₀H₅₂N₈O₁₀S₂
Molecular Weight:869.02

Speicherung:

-20°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

THAL-SNS-032 Chemical Structure

CAS. Nr.: 2139287-33-3

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (10)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

THAL-SNS-032 is a selective CDK9 PROTAC degrader. THAL-SNS-032 recruits CRBN to form a ternary complex with CDK9, thereby triggering ubiquitination and proteasomal degradation of CDK9. THAL-SNS-032 also induces the degradation of CDK1, CDK2 and CDK7. THAL-SNS-032 elevates pH2AX levels, reduces MCL1s expression, and activates caspase-3. THAL-SNS-032 induces cancer cell apoptosis, regulates transcription, and inhibits the replication of human cytomegalovirus (CMV) and SARS-CoV-2. THAL-SNS-032 can be used in research related to breast cancer, leukemia, cytomegalovirus infection and SARS-CoV-2 infection^[1]^[2]^[3]. (Pink: CDK9 ligand (HY-10008); Blue: Cereblon ligand (HY-14658); Black: linker (HY-W015088)).

IC₅₀ & Target^[1]

CDK9	CDK9/CycT1

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle CDK Isoform-spezifische Produkte anzeigen :

Alle Caspase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CWR22R	IC₅₀	0.049 μM Compound: THAL-SNS032	Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability measured after 5 days by CellTiter-Glo assay Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability measured after 5 days by CellTiter-Glo assay	[PMID: 35925880]
MOLT-4	IC₅₀	50 nM Compound: 80	Antiproliferative activity against human MOLT4 cells incubated for 72 hrs by cell titer glo assay Antiproliferative activity against human MOLT4 cells incubated for 72 hrs by cell titer glo assay	[PMID: 32866383]
MOLT-4	IC₅₀	50 nM Compound: 87; THAL-SNS-032	Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell proliferation Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell proliferation	[PMID: 32707525]
U2932	IC₅₀	306 nM Compound: THAL-SNS-032	Cytotoxicity against human U2932 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Cytotoxicity against human U2932 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 37671907]

In Vitro

THAL-SNS-032 (5-100 nM; 72 h) potently inhibits the viability of MCF7, T47D, BT474 and BT474 cells (EC₅₀ <100 nM), while exhibits weak activity in SKBR3, HCC1569, HCC1954, MDA-MB-231, HS578T, BT549, SUM149 and HCC3153 cells^[1].
THAL-SNS-032 (100 nM; 24-72 h) potently inhibits 3D spheroid formation and fibronectin adhesion in BT474, BT474-RH and BT474-TDM1R cells^[1].
THAL-SNS-032 (50 nM; 24-48 h) selectively degrades CDK9 protein in BT474, BT474-RH and BT474-TDM1R breast cancer cells^[1].
THAL-SNS-032 (50 nM; 72 h) significantly induces apoptosis, DNA damage (elevated pH2AX levels), and regulates apoptosis-related proteins (decreased MCL1s expression, activated caspase-3) in BT474, BT474-RH and BT474-TDM1R breast cancer cells^[1].
THAL-SNS-032 (0-100 nM; 72 h) reduces the viability of normal mammary epithelial MCF10A cells^[1].
THAL-SNS-032 exhibits nanomolar biochemical inhibitory activity against multiple CDK complexes, with the strongest inhibitory activity against CDK9/CycT1 (IC₅₀ = 4 nM)^[2].
THAL-SNS-032 (250 nM, up to 5 μM; 1-24 h) induces rapid, CRBN-dependent, and proteasome-mediated degradation of CDK9 in wild-type MOLT4 cells. Treatment with 250 nM causes substantial degradation of CDK9 within 1 hour, and this degradation effect persists for at least 24 hours^[2].
THAL-SNS-032 exhibits CRBN-dependent antiproliferative activity in MOLT4 cells (IC₅₀ = 50 nM) and induces CRBN-dependent inhibition of Pol II CTD Ser2 phosphorylation^[2].
THAL-SNS-032 (250 nM; 2-24 h, 6 h + washout) induces rapid and sustained apoptosis in MOLT4 cells^[2].
THAL-SNS-032 (1 nM-100 nM; 40 min-24 h, plus washout periods) induces concentration- and time-dependent degradation of CDK9, CDK2 and CDK7 (but not CDK1) in uninfected human foreskin fibroblasts (HFFs), and the reduction in CDK levels persists for 6 h after drug washout^[3].
THAL-SNS-032 (0.1 nM-10 nM; 3 h-3 days post-infection) induces more significant concentration- and time-dependent degradation of CDK9, CDK2, CDK7 and CDK1 in human cytomegalovirus strain AD169-infected HFFs, and maintains inhibitory effects on CDKs within 3 days of viral replication^[3].
THAL-SNS-032 (0.004 µM-1 µM; 7 days) potently inhibits the replication of HCMV AD169-GFP in HFFs, with an EC₅₀ of 0.025 µM^[3].
THAL-SNS-032 (for 4-10 days) inhibits the replication of HCMV Merlin in MRC-5 and TEV-1 cells, with EC₅₀ values ranging from 0.37 µM to 3.07 µM^[3].
THAL-SNS-032 (0.001 µM-1 µM; 5 days) inhibits the replication of MCMV Smith-GFP in MEF, with an EC₅₀ of 0.22 µM^[3].
THAL-SNS-032 (30 h) potently inhibits the replication of SARS-CoV-2 d6-YFP in Caco-2 cells, with an EC₅₀ of 0.11 µM^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

MCF7, T47D, BT474, BT474-RH, BT474-TDM1R, BT474-LAPA-R, SKBR3, HCC1569, HCC1954, MDA-MB-231, HS578T, BT549, SUM149, HCC3153
Concentration:

5, 20, 25, 50, 75, 100 nM
Incubation Time:

72 h
Result:

Displayed potent inhibitory activity in luminal A and luminal B/ER+/HER2+ cell lines with EC50 values ranging between 50-75 nM.
Showed significantly higher EC50 values in HER2+/ER- and triple-negative cell lines, with HER2+/ER- lines showing EC50 values three times higher than ER-positive/dual ER/HER2-positive lines.
Reduced cell viability in BT474, BT474-RH, BT474-TDM1R, and BT474-LAPA-R at tested concentrations.

Western Blot Analysis^[1]

Cell Line:

BT474, BT474-RH, BT474-TDM1R
Concentration:

50 nM
Incubation Time:

24, 48 h
Result:

Caused a significant decline in CDK9 protein levels at both 24 h and 48 h, but did not affect the levels of CDK7, CDK1, or CDK2.
In contrast, SNS-032 did not alter the levels of any analyzed kinases.

Apoptosis Analysis^[1]

Cell Line:

BT474, BT474-RH, BT474-TDM1R
Concentration:

50 nM
Incubation Time:

72 h
Result:

Caused a significant increase in apoptotic populations (early and late apoptosis), with BT474-derived resistant lines showing a greater increase in late apoptotic cells compared to parental BT474 cells.
SNS-032 had no appreciable effect on apoptosis.

Western Blot Analysis^[1]

Cell Line:

BT474, BT474-RH, BT474-TDM1R
Concentration:

50 nM
Incubation Time:

72 h
Result:

Increased levels of pH2AX (a marker of DNA damage), while SNS-032 had no effect on pH2AX levels.
Caused a slight reduction in caspase-3, most evident in BT474-TDM1R cells, and activated caspase-3 in these lines.
Reduced the short isoform of MCL1 in BT474-TDM1R cells.
Decreased total PARP levels, with minimal cleaved PARP detected.

Cell Viability Assay^[1]

Cell Line:

MCF10A
Concentration:

25, 50, 100 nM
Incubation Time:

72 h
Result:

Did not affect cell viability at 25 or 50 nM, but significantly reduced proliferation at 100 nM, with greater toxicity than SNS-032 at this concentration.

Western Blot Analysis^[2]

Cell Line:

Wildtype and CRBN−/− MOLT4 cells
Concentration:

250 nM; up to 5 μM
Incubation Time:

1 h, 8 h, 24 h (250 nM); 6 h (up to 5 μM)
Result:

Induced complete CRBN-dependent degradation of CDK9 at concentrations up to 5 μM after 6 hours, with a "hook effect" reducing degradation at 5 μM and above.
Caused substantial CDK9 degradation within 1 hour of 250 nM treatment that persisted for at least 24 hours.
Induced only modest protein level reductions of CDK1, CDK2, and CDK7 after 8 hours, attributed to downstream transcriptional changes rather than direct degradation.
Induced partial degradation of CDK10 only with longer exposure.
Blocked CDK9 degradation when pre-treated with MG132, excess thalidomide, or excess SNS-032.

Western Blot Analysis^[2]

Cell Line:

MOLT4 cells
Concentration:

250 nM
Incubation Time:

2 h, 4 h, 24 h; 6 h followed by washout and additional incubation
Result:

Induced complete CDK9 degradation within 2 hours.
Induced apoptosis (characterized by PARP and Caspase-3 cleavage) by 4 hours.
Caused loss of MCL-1, all of which persisted for 24 hours.
Increased levels of PARP cleavage, Caspase-3 cleavage, and ɣH2A.X activation after compound washout.

Apoptosis Analysis^[2]

Cell Line:

MOLT4 cells
Concentration:

250 nM
Incubation Time:

6 h followed by washout and 24 additional hours of incubation
Result:

Did not reduce apoptosis induced by THAL-SNS-032, while compound washout significantly reduced apoptosis induced by NVP-2 and SNS-032.

Western Blot Analysis^[3]

Cell Line:

HCMV-AD169-infected primary human foreskin fibroblasts (HFFs)
Concentration:

0.1, 1, 10 nM
Incubation Time:

3 h, 1 day, 3 days post-infection
Result:

Depleted CDK9 levels at 3 h post-infection at 10 nM.
Partially reduced CDK9 levels at 3 h post-infection at 1 nM.
Markedly reduced levels of CDK9, CDK2, CDK7, and CDK1 at 1 day post-infection.
Completely lost levels of CDK9, CDK2, CDK7, and CDK1 at 3 days post-infection.
Reduced CDK2 levels, which was unaffected in uninfected HFFs.

In Vivo

THAL-SNS-032 (2.5-10 mg/kg; i.p.; once to three times weekly) causes significant gastrointestinal toxicity and weight loss at all tested doses in BALB/c nu/nu mice bearing BT474 xenografts, with no observable tumor regression, demonstrating an inverse therapeutic index^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

BALB/c nu/nu (female, 4-5 weeks old)^[1]
Dosage:

2.5-10 mg/kg
Administration:

i.p.; once weekly (10 mg/kg); twice weekly (5 mg/kg); three times weekly (2.5 mg/kg)
Result:

Showed no signs of tumor regression at any dose tested.
Caused prominent weight loss in mice treated with 10 mg/kg and 5 mg/kg.
Induced gastrointestinal toxicity across all doses.
Partially reduced CDK9 levels in treated tumors.

Chemical Information

CAS. Nr. 2139287-33-3
Appearance Solid
Molecular Weight 869.02
Formel C₄₀H₅₂N₈O₁₀S₂
Color Light yellow to yellow
SMILES

O=C(NCCOCCOCCOCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CN4CCC(C(NC5=NC=C(SCC6=NC=C(C(C)(C)C)O6)S5)=O)CC4
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Publications (10)

All In Vivo Efficacy StudyWB

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Journal Impact Factor

Nature

Inhibitors supercharge kinase turnover through native proteolytic circuits. [Abstract]

2026 Jan;649(8098):1032-1041. PMID: 41299171
Nature

Rapid unleashing of macrophage efferocytic capacity via transcriptional pause release. [Abstract]

2024 Apr;628(8007):408-415. PMID: 38480883
Nat Commun

CDK9 recruits HUWE1 to degrade RARα and offers therapeutic opportunities for cutaneous T-cell lymphoma. [Abstract]

2024 Dec 5;15(1):10594. PMID: 39632829

THAL-SNS-032 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Dec 5;15(1):10594. [Abstract]

MOLT-4 and HH cells were treated with THAL-SNS-032 ( and western blots were conducted.
Mol Cell

SPT5 stabilization of promoter-proximal RNA polymerase II. [Abstract]

2021 Nov 4;81(21):4413-4424.e5. PMID: 34480849
J Med Chem

Discovery of dCDK9-202 as a Highly Potent and Selective PROTAC CDK9 Degrader with Strong In Vivo Antitumor Activity. [Abstract]

2025 Oct 23;68(20):21172-21186. PMID: 41066447

THAL-SNS-032 purchased from MedChemExpress. Usage Cited in: J Med Chem. 2025 Oct 23;68(20):21172-21186. [Abstract]

Changes in tumor volume during dCDK9-202, (SNS032), or THAL-SNS032) treatments (10 mg/kg, i.v., qod).
Structure

PROTAC-mediated activation, rather than degradation, of a nuclear receptor reveals complex ligand-receptor interaction network. [Abstract]

2024 Dec 5;32(12):2352-2363.e8. PMID: 39389062
Res Sq

2026 Jan 6.
Biomed Pharmacother

Liposomal formulation of the CDK9 PROTAC THAL-SNS-032 enhances the antitumor activity in breast cancer cell lines. [Abstract]

2025 Aug:189:118352. PMID: 40652725
Patent

US20240425555A1.
Research Square Preprint

2024 May 2.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (115.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.1507 mL

5.7536 mL

11.5072 mL

5 mM

0.2301 mL

1.1507 mL

2.3014 mL

10 mM

0.1151 mL

0.5754 mL

1.1507 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (2.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (2.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (287 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Noblejas-López MDM, et al. Antitumoral Activity of a CDK9 PROTAC Compound in HER2-Positive Breast Cancer. International journal of molecular sciences. 2022 May 13;23(10):5476. [Content Brief]

[2]. Olson CM, et al. Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation. Nature chemical biology. 2018 Feb;14(2):163-170. [Content Brief]

[3]. Hahn F, et al. Development of a PROTAC-Based Targeting Strategy Provides a Mechanistically Unique Mode of Anti-Cytomegalovirus Activity. International journal of molecular sciences. 2021 Nov 27;22(23):12858. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.1507 mL	5.7536 mL	11.5072 mL	28.7680 mL
	5 mM	0.2301 mL	1.1507 mL	2.3014 mL	5.7536 mL
	10 mM	0.1151 mL	0.5754 mL	1.1507 mL	2.8768 mL
	15 mM	0.0767 mL	0.3836 mL	0.7671 mL	1.9179 mL
	20 mM	0.0575 mL	0.2877 mL	0.5754 mL	1.4384 mL
	25 mM	0.0460 mL	0.2301 mL	0.4603 mL	1.1507 mL
	30 mM	0.0384 mL	0.1918 mL	0.3836 mL	0.9589 mL
	40 mM	0.0288 mL	0.1438 mL	0.2877 mL	0.7192 mL
	50 mM	0.0230 mL	0.1151 mL	0.2301 mL	0.5754 mL
	60 mM	0.0192 mL	0.0959 mL	0.1918 mL	0.4795 mL
	80 mM	0.0144 mL	0.0719 mL	0.1438 mL	0.3596 mL
	100 mM	0.0115 mL	0.0575 mL	0.1151 mL	0.2877 mL

THAL-SNS-032

10 Cited Publications

100 mg Angebot einholen

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THAL-SNS-032

PROTAC Library

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) THAL-SNS-032

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle CDK Isoform-spezifische Produkte anzeigen

Alle Caspase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (10)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

THAL-SNS-032

PROTAC Library

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) THAL-SNS-032

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle CDK Isoform-spezifische Produkte anzeigen

Alle Caspase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (10)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

THAL-SNS-032 Related Classifications

HY-123937 Related Classifications