MD102
Based on 1 Customer Validation
MD102 is an orally active transglutaminase 2 (TG2) inhibitor with an IC50 of 0.35 μM. MD102 binds to the β-sandwich domain of TG2, disrupts the interaction between TG2 and p53, stabilizes p53, and reduces the activity of p-AKT and p-mTOR signaling pathways. MD102 induces cell apoptosis and inhibits tumor growth. MD102 can be used for the research of renal cell carcinoma.
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- Purity: 98.01%
- CAS No.: 2755794-94-4
- 화학식: C13H4BrCl2FN2O2
- 분자량:389.99
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
- 순도&문서
- References
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Help & FAQs
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Biological Activity
MD102 (48 h) potently inhibits the proliferation of ACHN and Caki-1 renal cell carcinoma cell lines, with GI50 values of 2.15 μM and 1.98 μM, respectively[1].
MD102 (1-10 μM; 24 h) stabilizes the p53 protein in ACHN and Caki-1 renal cancer cell lines, increasing p53 expression levels by 2.2-fold and 2.5-fold at the concentration of 10 μM, respectively[1].
MD102 (0.1-10 μM; 8 h) inhibits intracellular TG2 activity in ACHN renal cell carcinoma cells in a concentration-dependent manner in vitro[1].
MD102 (0.1-10 μM; 8 h) induces apoptosis in ACHN renal cell carcinoma cells in a concentration-dependent manner[1].
MD102 (48 h) regulates the p53/AKT/mTOR signaling pathway in ACHN renal cancer cells, enhances the activation level of p53, reduces the phosphorylation level of AKT/mTOR, and promotes the expression of apoptotic proteins[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:ACHN and Caki-1 renal cell carcinoma cell lines
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Concentration:1 μM, 10 μM
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Incubation Time:24 h
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Result:Increased p53 expression by 2.2-fold in ACHN cells at 10 μM relative to the control.
Increased p53 expression by 2.5-fold in Caki-1 cells at 10 μM relative to the control.
Increased p53 expression by 1.4-fold in ACHN cells at 1 μM relative to the control.
Increased p53 expression by 1.4-fold in Caki-1 cells at 1 μM relative to the control.
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Cell Line:ACHN renal cell carcinoma cell line
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Concentration:0.1, 1 and 10 μM
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Incubation Time:8 h
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Result:Induced significant apoptosis in ACHN cells in a concentration-dependent manner.
Increased the proportion of apoptotic cells relative to untreated controls.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (CAnN.Cg-Foxn1nu/CrljOri)[1]
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Dosage:10 mg/kg (p.o.); 50 mg/kg (p.o.); 10 mg/kg (i.p.); 15 mg/kg (i.p.)
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Administration:p.o.; once daily; 60 days; i.p.; twice weekly; 60 days
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Result:Achieved 66% tumor growth inhibition at 15 mg/kg i.p..
Achieved 71% tumor growth inhibition at 50 mg/kg p.o..
Increased p53 levels in treated tumor tissues.
Decreased Ki-67 levels in treated tumor tissues.
Did not induce body weight loss in mice.
Chemical Information
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CAS No. 2755794-94-4
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Appearance Solid
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분자량 389.99
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화학식 C13H4BrCl2FN2O2
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Color Brown to reddish brown
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SMILES
BrC1=CC=C(C2=NC(C(C(Cl)=C(Cl)C3=O)=O)=C3N2)C=C1F
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
용액&용해도
DMSO : 5 mg/mL (12.82 mM; ultrasonic and warming and heat to 60°C; 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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 (274 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 (sealed storage, away from moisture). 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 | 2.5642 mL | 12.8208 mL | 25.6417 mL | 64.1042 mL |
| 5 mM | 0.5128 mL | 2.5642 mL | 5.1283 mL | 12.8208 mL | |
| 10 mM | 0.2564 mL | 1.2821 mL | 2.5642 mL | 6.4104 mL |
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