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MGH-CP1

SKU: orb1298429

Description

MGH-CP1 is a potent, selective inhibitor of TEAD palmitoylation, effectively blocking TEAD2 and TEAD4 auto-palmitoylation in vitro with IC50 values of 710 nM and 672 nM, respectively. This compound is a valuable chemical probe for investigating Hippo signaling pathway biology in cancer research and cellular models.

Research Area

Cell Biology

Images & Validation

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MGH-CP1

Key Properties

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CAS Number896657-58-2
MW368.5
Purity99.76% (May vary between batches)
FormulaC20H24N4OS
SMILESO=C(CSc1ncn[nH]1)Nc1ccc(cc1)C12CC3CC(CC(C3)C1)C2
TargetOthers,Apoptosis
Solubility10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.43 mM);Ethanol:74 mg/mL (200.81 mM);DMSO:45 mg/mL (122.12 mM)

Bioactivity

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Target IC50
TEAD2:672 nM|TEAD4:710 nM
In Vivo
MGH-CP1 inhibits TEAD activity in Lats1/2 KO intestine in vivo. MGH-CP1 can effectively inhibit the palmitoylation of TEAD proteins in the intestinal epithelium. MGH-CP1 is well tolerated and has no apparent adverse effect on overall animal health or body weight after 2 weeks of treatment. In contrast to its lack of apparent effect in wild-type intestine, MGH-CP1 treatment effectively inhibits upregulation of the TEAD target genes, CTGF and ANKRD1, in Lats1/2 KO intestine
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In Vitro
MGH-CP1 exhibits dose-dependent and potent inhibition of TEAD2/4 auto-palmitoylation in vitro, with IC50 of 710 nM and 672 nM, respectively. Furthermore, MGH-CP1 treatment markedly decreased the palmitoylation levels of endogenous or ectopically expressed TEAD proteins in cells.
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Cell Research
HEK293T cells, Lats1/2 conditional MEFs and MDA-MB-231 cells were cultured in DMEM supplemented with 10% FBS and 1% penicillin/streptomycin. For Lats1/2 conditional MEFs carrying CMV-CreER, Lats1/2 was deleted by incubation with 4-OH Tamoxifen (2.5 mM) in DMEM for 4 days prior to further experiment. Transfection in HEK293T cells was performed using Lipofectamine 2000 (Invitrogen). For luciferase reporter assays, HEK293T cells were transfected with the luciferase reporter constructs TBS-Luc (8XGTIIC-Luc), Super TOP-FLASH (STF), Gli-BS-Luc, BRE-Luc, and NF-kB-Luc, as well as the expression vectors of pGIPZ-YAP5SA, pGIPZ-YAP6SA, pGIPZ-TAZ4SA, pLV-β-Catenin-ΔN90, pCIG-Wnt3a, pCMV-LRP5C, pCIG-BMP4, pCIG-Gli1, pGIPZ-IKBKE (Rajurkar et al., 2017) and pCMV-Renilla lucifease. Luciferase activities were conducted 24 hours after transfection using the dual-luciferase reporter kit (Promega) in the cells treated with or without Wnt3A, LiCl or MGH-CP1. Assays were conducted in triplicates and quantified using PerkinElmer EnVision plate reader.
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Storage & Handling

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Storagekeep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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MGH CP1, MGHCP1, MGH-CP1, MGH-CP-1, inhibit, Myc, Epithelial, Lats1/2 deletion, Inhibitor, Apoptosis, TEAD auto-palmitoylation, TEAD2, TEAD4, TEAD

Similar Products

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  • MGH-CP1

    MGH-CP1 [orb1217519]

    >98% (HPLC)

    896657-58-2

    368.5

    C20H24N4OS

    5 mg, 25 mg, 100 mg, 50 mg, 2 mg, 10 mg, 1 g, 500 mg
Quality Guarantee

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Compound Identifiers

PubChem CID
2993112 ↗

Key Properties

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No computed properties available.

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MGH-CP1 (orb1298429)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

2 mg
¥ 1,040.00
5 mg
¥ 1,300.00
1 ml x 10 mM (in DMSO)
¥ 1,430.00
10 mg
¥ 1,690.00
25 mg
¥ 3,120.00
50 mg
¥ 5,070.00
100 mg
¥ 7,930.00
200 mg
¥ 10,790.00
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