2. Apoptosis
  3. Apoptosis
  4. MGH-CP1

MGH-CP1 

Cat. No.: HY-139330 Purity: 99.21%
COA Handling Instructions

MGH-CP1 is a potent and orally active TEAD2 and TEAD4 auto-palmitoylation inhibitor with IC50s of 710 nM and 672 nM, respectively. MGH-CP1 can decrease the palmitoylation levels of endogenous or ectopically expressed TEAD proteins in cells. MGH-CP1 can suppress Myc expression, inhibit epithelial over-proliferation, and induce apoptosis when together with Lats1/2 deletion.

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

MGH-CP1 Chemical Structure

MGH-CP1 Chemical Structure

CAS No. : 896657-58-2

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Based on 1 publication(s) in Google Scholar

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Description

MGH-CP1 is a potent and orally active TEAD2 and TEAD4 auto-palmitoylation inhibitor with IC50s of 710 nM and 672 nM, respectively. MGH-CP1 can decrease the palmitoylation levels of endogenous or ectopically expressed TEAD proteins in cells. MGH-CP1 can suppress Myc expression, inhibit epithelial over-proliferation, and induce apoptosis when together with Lats1/2 deletion[1].

IC50 & Target

IC50: 710 nM (TEAD2), 672 nM (TEAD4) [1]
In Vitro

MGH-CP1 (0-100 μM) inhibits auto-palmitoylation of recombinant TEAD2 and TEAD4 in a dose-dependent manner[1].
MGH-CP1 (0-2 μM) inhibits TEAD-binding sites (TBS)-Luc reporter activity in a dose-dependent manner in YAP-expressing HEK293 cells[1].
MGH-CP1 does not affect YAP nuclear localization or protein levels but potently inhibits TEAD-mediated transcription in a dose-dependent manner and effectively blocks cell over-proliferation[1].
MGH-CP1 can suppress Myc expression, inhibit epithelial over-proliferation, and induce apoptosis when together with Lats1/2 deletion[1].

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

MGH-CP1 (75mg/kg; PO; daily, for 2 weeks) inhibits the palmitoylation of TEAD proteins in the intestinal epithelium in wild-type mice, but inhibits upregulation of the TEAD target genes, CTGF and ANKRD1, in Lats1/2 KO mice intestine[1].

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

Animal Model: Mice (induced high-dose Cre recombination by intraperitoneal injection of 120mg/kg Tamoxifen for two consecutive days)[1]
Dosage: 75 mg/kg
Administration: PO; daily, for 2 weeks
Result: Effectively inhibited the palmitoylation of TEAD proteins in the intestinal epithelium in wild-type mice, but effectively inhibited upregulation of the TEAD target genes, CTGF and ANKRD1, in Lats1/2 KO mice intestine.
Molecular Weight

368.50

Appearance

Solid

Formula

C20H24N4OS
CAS No.
SMILES

O=C(CSC1=NN=CN1)NC2=CC=C(C=C2)C3(C[[email protected]](C4)C5)C[[email protected]]5C[[email protected]]4C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (271.37 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7137 mL 13.5685 mL 27.1370 mL
5 mM 0.5427 mL 2.7137 mL 5.4274 mL
10 mM 0.2714 mL 1.3569 mL 2.7137 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: ≥ 2.5 mg/mL (6.78 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.78 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (6.78 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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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.

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Keywords:

MGH-CP1896657-58-2ApoptosisTEAD auto-palmitoylationMycEpithelialLats1/2 deletionInhibitorinhibitorinhibit

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