1. Apoptosis
    PROTAC
    Metabolic Enzyme/Protease
  2. MDM-2/p53
    PROTAC
    E1/E2/E3 Enzyme
  3. MD-222

MD-222 

Cat. No.: HY-134823 Purity: 99.28% ee.: 100.00%
Handling Instructions

MD-222 is the first-in-class highly potent PROTAC degrader of MDM2. MD-222 induces rapid degradation of the MDM2 protein and activation of wild-type p53 in cells. MD-222 has anticancer effects.

For research use only. We do not sell to patients.

MD-222 Chemical Structure

MD-222 Chemical Structure

CAS No. : 2136246-72-3

Size Price Stock Quantity
5 mg USD 950 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
25 mg USD 3450 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

MD-222 is the first-in-class highly potent PROTAC degrader of MDM2. MD-222 induces rapid degradation of the MDM2 protein and activation of wild-type p53 in cells. MD-222 has anticancer effects[1][2].

IC50 & Target[1][2]

MDM2

 

In Vitro

MD-222 (1-30 nM; 1-2 hours) treatment shows very effective in reducing the levels of MDM2 protein and increasing the levels of p53 in a time- and dose-dependent manner in RS4;11 and RS4;11/IRMI-2 cells[1].
MD-222 (30-100 nM; 6 hours) is effective in increasing the expression of several p53-targeted genes, such as MDM2, CDKN1A, and PUMA in RS4;11 cells, indicating strong activation of p53[2].
MD-222 (4 days) shows cell growth inhibitory activity in RS4;11 cells with an IC50 of 5.5 nM, and has no effect on RS4;11/IRMI-2, MDA-MB-231 and MDA-MB-468 cells[1].

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

Western Blot Analysis[1]

Cell Line: RS4;11 and RS4;11/IRMI-2 cells
Concentration: 1 nM, 3 nM, 10 nM, 30 nM
Incubation Time: 1 hour, 2 hours
Result: Reduced the level of MDM2 and increased the level of p53.

RT-PCR[2]

Cell Line: RS4;11 cells
Concentration: 30 nM, 100 nM
Incubation Time: 6 hours
Result: Increasd the expression of several p53-targeted genes, such as MDM2, CDKN1A, and PUMA.
Molecular Weight

893.83

Formula

C₄₈H₄₇Cl₂FN₆O₆

CAS No.
SMILES

O=C1[[email protected]]2(C3=CC=C(Cl)C=C3N1)C4(CCCCC4)N[[email protected]]([[email protected]]2([H])C5=C(C(Cl)=CC=C5)F)C(NC6=CC=C(C=C6)C(NCCCCCC7=C8C(C(N(C9C(NC(CC9)=O)=O)C8)=O)=CC=C7)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (223.76 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1188 mL 5.5939 mL 11.1878 mL
5 mM 0.2238 mL 1.1188 mL 2.2376 mL
10 mM 0.1119 mL 0.5594 mL 1.1188 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: 5 mg/mL (5.59 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 5 mg/mL (5.59 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

MD-222MD222MD 222MDM-2/p53PROTACE1/E2/E3 EnzymeProteolysis-targeting chimeraE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseLenalidomideMDM2p53anticancerInhibitorinhibitorinhibit

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MD-222
Cat. No.:
HY-134823
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