Queen's Award Received in 2021 ISO 9001 Certified Delivered over 1,000,000 bio-reagents to life science researchers Trusted by Life Science Communities
Cart summary

You have no items in your shopping cart.

MGH-CP1

SKU: orb1217519

Description

MGH-CP1 is a potent and selective inhibitor TEAD palmitoylation. It exhibits dose-dependent and potent inhibition of TEAD2/4 auto-palmitoylation in vitro with IC50 of 710 nM and 672 nM, respectively.

Images & Validation

Key Properties

CAS Number896657-58-2
MW368.5
Purity>98% (HPLC)
FormulaC20H24N4OS
SMILESC1C2CC3CC1CC(C2)(C3)C4=CC=C(C=C4)NC(=O)CSC5=NC=NN5
TargetTEAD|TEAD2|TEAD4
SolubilityDMSO:74 mg/mL (200.81 mM);Ethanol:74 mg/mL (200.81 mM)

Bioactivity

In Vivo
MGH-CP1 (75 mg/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. Animal model: Mice (induced high-dose Cre recombination by intraperitoneal injection of 120 mg/kg Tamoxifen for two consecutive days). 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.
In Vitro
MGH-CP1 (0-100 μM) inhibits auto-palmitoylation of recombinant TEAD2 and TEAD4 in a dose-dependent manner. MGH-CP1 (0-2 μM) inhibits TEAD-binding sites (TBS)-Luc reporter activity in a dose-dependent manner in YAP-expressing HEK293 cells. 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. MGH-CP1 can suppress Myc expression, inhibit epithelial over-proliferation, and induce apoptosis when together with Lats1/2 deletion.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Similar Products

  • MGH-CP1 [orb1298429]

    99.76% (May vary between batches)

    896657-58-2

    368.5

    C20H24N4OS

    2 mg, 50 mg, 1 ml x 10 mM (in DMSO), 200 mg, 5 mg, 10 mg, 25 mg, 100 mg
Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Documents Download

Datasheet
Product Information
Download

Request a Document

Protocol Information

MGH-CP1 (orb1217519)

  • Star
  • Star
  • Star
  • Star
  • Star
  • 0.0
Based on 0 reviews

Participating in our Biorbyt product reviews program enables you to support fellow scientists by sharing your firsthand experience with our products.

Login to Submit a Review

No reviews yet

Step 1: Enter information below

(Recommended: An additional animal making an allowance for loss during the experiment)

Step 2: Enter the in vivo formulation

(This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

2 mg
¥ 1,040.00
5 mg
¥ 1,300.00
10 mg
¥ 1,950.00
25 mg
¥ 3,640.00
50 mg
¥ 6,240.00
100 mg
¥ 9,750.00
500 mg
¥ 20,020.00