MI1013
Based on 1 Customer Validation
MI1013 is a PROTAC PXR degrader (DC50 = 89 nM, Dmax = 82%). MI1013 degrades PXR in human hepatocellular carcinoma RG cells (HepaRG). MI1013 specifically and safely regulates CYP3A4 promoter activity through PXR degradation. MI1013 affects several key genes involved in sulfate conjugation (e.g., SULT1E1), bile acid synthesis (CYP7A1), gluconeogenesis (PCK1), ketone synthesis (HMGCS20), and hepatocyte proliferation (MKI67). (Pink: PXR ligand 3: HY-175267, Blue: Pomalidomide-propargyl ligand: HY-W410002, Pink + Black: PXR ligand-Linker Conjugate 1: HY-175268).
(Pink: Pregnane X Receptor (PXR) ligand (HY-175267); Blue: Cereblon ligand (HY-W410002); Black: linker).
For research use only. We do not sell to patients.
- Purity: 99.10%
- Formula: C42H46N10O12S
- Molecular Weight:914.94
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
All PROTACs Isoforms
More
Biological Activity
|
Cereblon |
CYP3A4 |
MI1013 (0.01-10 μM, 0-96 h) induces degradation of PXR, but does not degrade RXRα and GSPT1 in HepaRG and MOLT4 cells[1].
MI1013 (1-10 μM, 24 h) inhibits PXR and PXR-HiBiT degradation, does not exhibit agonistic activity at concentrations up to 10 μM in HepaRG cells using the CYP3A4 gene promoter luciferase construct[1].
MI1013 is less competitive in binding to PXR LBD[1].
MI1013 (24 h) is nontoxic up to a concentration of 100 μM in HepaRG , HK-2, COS-1, and HepG2 cells[1].
MI1013 (2 μM, 24 h) effectively modulates PXR activity, allowing CAR to regain its function in HepaRG cells[1].
MI1013 (2 μM, 24 h) down-regulates the mRNA levels of CYP3A4, SULT1E1 and SULT1B1 encoding sulfotransferases, CYP7B1, NR0B2, and CYP7A1, and up-regulates the mRNA level of UGT1A1 in HepaRG Cells and Human Hepatocytes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:HepaRG cells
-
Concentration:0.01 μM, 0.1 μM, 0.5μM, 1 μM, 2 μM, 3 μM, 10 μM
-
Incubation Time:0 h, 4 h, 8 h, 12 h, 24 h, 48 h, 72 h, 96 h
-
Result:Induced degradation of PXR, but reversaled of PXR expression after 72 h.
Did not degrade RXRα and GSPT1.
Chemical Information
-
Appearance Solid
-
Molecular Weight 914.94
-
Formula C42H46N10O12S
-
Color Light yellow to yellow
-
SMILES
O=C(NC1=CC=C(S(=O)(C2=C(C)N(C3=CC(OC)=CC=C3OC)N=N2)=O)C=C1)CCOCCOCCOCCN4N=NC(CNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)=C4
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 50 mg/mL (54.65 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)
Purity & Documentation
-
Data Sheet (271 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
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 | 1.0930 mL | 5.4648 mL | 10.9297 mL | 27.3242 mL |
| 5 mM | 0.2186 mL | 1.0930 mL | 2.1859 mL | 5.4648 mL | |
| 10 mM | 0.1093 mL | 0.5465 mL | 1.0930 mL | 2.7324 mL | |
| 15 mM | 0.0729 mL | 0.3643 mL | 0.7286 mL | 1.8216 mL | |
| 20 mM | 0.0546 mL | 0.2732 mL | 0.5465 mL | 1.3662 mL | |
| 25 mM | 0.0437 mL | 0.2186 mL | 0.4372 mL | 1.0930 mL | |
| 30 mM | 0.0364 mL | 0.1822 mL | 0.3643 mL | 0.9108 mL | |
| 40 mM | 0.0273 mL | 0.1366 mL | 0.2732 mL | 0.6831 mL | |
| 50 mM | 0.0219 mL | 0.1093 mL | 0.2186 mL | 0.5465 mL |
Powered by Bioz