TH-407a
Based on 1 Customer Validation
TH-407a is an orally active and selective USP15 inhibitor with an IC50 of 0.76 μM. As an allosteric modulator, TH-407a binds to a non-catalytic site to block deubiquitinating activity. TH-407a inhibits cell growth, proliferation, clonogenicity and migration, regulates the p53 signaling pathway, and reduces the stability of PARP1. TH-407a exhibits anti-tumor activity in breast cancer xenograft mouse models. TH-407a can be used for the research of breast cancer.
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- Purity : 98.37%
- CAS No.: 1903103-73-0
- 화학식: C22H18N4O
- 분자량:354.40
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
USP15 0.76 μM (IC50) |
PARP1 |
In Vitro
TH-407a potently inhibits the enzymatic activity of purified USP15 protein with an IC50 of 0.76 μM via Ub-AMC hydrolysis inhibition[1].
TH-407a (0.31-20 μM; 30 min) dose-dependently inhibits recombinant USP15-mediated hydrolysis of K48-linked diubiquitin[1].
TH-407a inhibits the interaction between USP15 protein and the covalent-binding ubiquitin analog Ub-PA in vitro[1].
TH-407a is selective for USP15, showing negligible inhibition of purified USP1, USP2, and USP7 proteins at 10 μM[1].
TH-407a (10× IC50; 30, 60, or 90 min) reversibly inhibits purified USP15 protein, with time-dependent recovery of enzymatic activity after dilution[1].
TH-407a (1.5625-12.5 μM) directly binds to immobilized USP15 protein with strong affinity, as demonstrated by a Kd of 4.26 μM via SPR[1].
TH-407a dose-dependently inhibits the proliferation of MCF-7, HCC70, MDA-MB-231, and MDA-MB-436 breast cancer cells, with IC50 values of 19.57 μM for MCF-7 and 38.66 μM for MDA-MB-436[1].
TH-407a (5-10 μM) inhibits clonal growth of MCF-7, HCC70, MDA-MB-231, and MDA-MB-436 breast cancer cells[1].
TH-407a (10 μM (HCC70, MDA-MB-231); 20 μM (MCF-7, MDA-MB-436); 12 or 24 h) impairs the migratory capacity of MCF-7, HCC70, MDA-MB-231, and MDA-MB-436 breast cancer cells[1].
TH-407a (5-40 μM (immunoblotting); 20 μM (MDM2 ubiquitination assessment)) modulates the p53 signaling pathway in MCF-7 breast cancer cells by downregulating MDM2, stabilizing p53, and increasing MDM2 ubiquitination[1].
TH-407a (5-40 μM (immunoblotting); 10 μM (CHX stability assay); 4 or 12 h (pre-treatment); 0-12 h (monitoring)) reduces PARP1 protein stability and expression in MCF-7, HCC70, MDA-MB-231, and MDA-MB-436 breast cancer cells by increasing PARP1 ubiquitination and accelerating its degradation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCC70, MDA-MB-231
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Concentration:10 μM
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Incubation Time:12 h
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Result:Impaired the migratory capacity of HCC70, MDA-MB-231.
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Cell Line:MCF-7, MDA-MB-436
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Concentration:20 μM
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Incubation Time:24 h
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Result:Impaired the migratory capacity of MCF-7, MDA-MB-436.
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Cell Line:MCF-7
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Concentration:5, 10, 20, 40 μM
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Incubation Time:12 h
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Result:Modulated the p53 signaling pathway in MCF-7 breast cancer cells by downregulating MDM2, stabilizing p53, and increasing MDM2 ubiquitination.
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Cell Line:MCF-7, HCC70, MDA-MB-231, and MDA-MB-436 breast cancer cells
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Concentration:5, 10, 20, 40 μM
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Incubation Time:0, 6, 12 h (monitoring)
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Result:Reduced PARP1 protein stability and expression by increasing PARP1 ubiquitination and accelerating its degradation.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
- Cell migration
- Somatic Cell Culture
- CCK-8/WST-8 Cell Proliferation Assay
- Cell Counting-Based Growth Curve Assay
- Breast Cancer Modeling
- Cell Viability Determination by MTT Colorimetric Assay
- Protocol for Cell Counting and Cell Density Analysis
- Patient-Derived Xenograft (PDX)
- Splenic/Portal-Vein Liver Metastasis Xenograft
- MTT Cell Proliferation Assay
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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CAS No. 1903103-73-0
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Appearance Solid
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분자량 354.40
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화학식 C22H18N4O
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Color White to off-white
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SMILES
[H]C1(CN(C(C2=CC=C3C(C=CC=C3)=C2)=O)C1)N4N=NC(C5=CC=CC=C5)=C4
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 12.5 mg/mL (35.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8217 mL | 14.1084 mL | 28.2167 mL | 70.5418 mL |
| 5 mM | 0.5643 mL | 2.8217 mL | 5.6433 mL | 14.1084 mL | |
| 10 mM | 0.2822 mL | 1.4108 mL | 2.8217 mL | 7.0542 mL | |
| 15 mM | 0.1881 mL | 0.9406 mL | 1.8811 mL | 4.7028 mL | |
| 20 mM | 0.1411 mL | 0.7054 mL | 1.4108 mL | 3.5271 mL | |
| 25 mM | 0.1129 mL | 0.5643 mL | 1.1287 mL | 2.8217 mL | |
| 30 mM | 0.0941 mL | 0.4703 mL | 0.9406 mL | 2.3514 mL |
TH-407a Related Classifications
HY-184273 Related Classifications
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