2. PROTAC Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. PROTACs Cytochrome P450 Pregnane X Receptor (PXR)
  4. MI1013

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.

MI1013

MI1013 Chemical Structure

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
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Based on 1 publication(s) in Google Scholar

MI1013 Related Antibodies

Top Publications Citing Use of Products

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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)[1]. (Pink: Pregnane X Receptor (PXR) ligand (HY-175267); Blue: Cereblon ligand (HY-W410002); Black: linker).

IC50 & Target[1]

Cereblon

 

CYP3A4

 

In Vitro

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.

MI1013 Related Antibodies

Western Blot Analysis[1]

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.
Molecular Weight

914.94

Formula

C42H46N10O12S
Appearance

Solid

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
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0930 mL 5.4648 mL 10.9297 mL
5 mM 0.2186 mL 1.0930 mL 2.1859 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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
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MI1013 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MI1013MI 1013MI-1013PROTACsCytochrome P450Pregnane X Receptor (PXR)CYPsPregnane X ReceptorDegraderHepaRG cellsInhibitorinhibitorinhibit

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