2. Stem Cell/Wnt
  3. YAP
  4. MSC-4106

MSC-4106 is an orally active and potent inhibitor of YAP/TAZ-TEAD. MSC-4106 inhibits TEAD1 or TEAD3 auto-palmitoylation and shows inhibitory effect on NCI-H226 tumor xenograft model.

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

MSC-4106 Chemical Structure

MSC-4106 Chemical Structure

CAS No. : 2738542-58-8

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5 mg USD 300 In-stock
10 mg USD 480 In-stock
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Based on 1 publication(s) in Google Scholar

MSC-4106 Related Antibodies

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  • Purity & Documentation

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Description

MSC-4106 is an orally active and potent inhibitor of YAP/TAZ-TEAD. MSC-4106 inhibits TEAD1 or TEAD3 auto-palmitoylation and shows inhibitory effect on NCI-H226 tumor xenograft model[1].

IC50 & Target

Target: YAP[1]
In Vitro

MSC-4106 (10 μM, 24 h) inhibited SK-HEP-1 reporter and NCI-266 cell viability with IC50 values of 4 nM and 14 nM, respectively[1].
MSC-4106 (10 μM, 6 h) crystallizes in the P-site of TEAD1, and against TEAD1 or TEAD3 palmitoylation in TEAD-Overexpressing HEK293 Cells by 97.3% and 75.9%, respectively[1].
MSC-4106 (10 μM, 4 d) targets TEAD indicated by a reduction in viability of NCI-H226 cells[1].

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

MSC-4106 Related Antibodies

Cell Viability Assay[1]

Cell Line: NCI-H226 (YAP dependent); SW620 YAP/TAZ KO (Yap-independent) cells
Concentration: 0, 3, 6, 9, 12, 15, 18, 21, 24, 26, 30 μM
Incubation Time: 96 hours
Result: Showed inhibitory effect to NCI-H226 and general cytotoxic to SW620 (IC50 >30 μM).

Immunofluorescence[1]

Cell Line: SK-HEP-1
Concentration: 0, 3, 6, 9, 12, 15, 18, 21, 24, 26, 30 μM
Incubation Time: 24 hours
Result: Inhibited YAP-TEAD interation.
In Vivo

MSC-4106 (100 mg/kg/d; p.o.; 7 d) displays anti-tumor effect with controlled tumor volume and good tolerability with stable body weight in mice[1].
MSC-4106 (1, 5, 100 mg/kg/d; p.o.; 0-72 h) down-regulates Cyr61 (cysteine-rich angiogenic inducer 61) expression, the TEAD-regulated target gene, in tumor lysates at all time points at 100 mg/kg and 24 h at 5 mg/kg[1].
Pharmacokinetics (PK) profile in different species[1]

Parameter Mouse Rat Dog
Cl (l/h/kg) 0.2 0.7 0.05
PO t1/2 (h) 45 40 3.6
PO AUC (μg•h/mL) 45 10 33
Vss (L/kg) 2 5 0.3
F (%) >90 80 18
Note: PO studies were performed at 10 mg/kg; MSC-4106 was formulated in 20% Kleptose in 50 mM PBS at pH 7.4.

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

Animal Model: NCI-H226 xenograft model in H2d Rag2 female mice (9-week-old)[1]
Dosage: 5, 100 mg/kg
Administration: Oral gavage; once daily; 32 days
Result: Resulted tumor growth controlled with 5 mg/kg while regressed with 100 mg/kg dosing after 32 treatment days.
Molecular Weight

359.30

Formula

C18H12F3N3O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC2=C(N(C3=CC=C(C(F)(F)F)C=C3)C4=NN(C)C=C42)C=C1)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 : 250 mg/mL (695.80 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 2.7832 mL 13.9159 mL 27.8319 mL
5 mM 0.5566 mL 2.7832 mL 5.5664 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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 (sealed storage, away from moisture). 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 2.7832 mL 13.9159 mL 27.8319 mL 69.5797 mL
5 mM 0.5566 mL 2.7832 mL 5.5664 mL 13.9159 mL
10 mM 0.2783 mL 1.3916 mL 2.7832 mL 6.9580 mL
15 mM 0.1855 mL 0.9277 mL 1.8555 mL 4.6386 mL
20 mM 0.1392 mL 0.6958 mL 1.3916 mL 3.4790 mL
25 mM 0.1113 mL 0.5566 mL 1.1133 mL 2.7832 mL
30 mM 0.0928 mL 0.4639 mL 0.9277 mL 2.3193 mL
40 mM 0.0696 mL 0.3479 mL 0.6958 mL 1.7395 mL
50 mM 0.0557 mL 0.2783 mL 0.5566 mL 1.3916 mL
60 mM 0.0464 mL 0.2319 mL 0.4639 mL 1.1597 mL
80 mM 0.0348 mL 0.1739 mL 0.3479 mL 0.8697 mL
100 mM 0.0278 mL 0.1392 mL 0.2783 mL 0.6958 mL
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MSC-4106 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:

MSC-41062738542-58-8MSC4106MSC 4106YAPYes-associated proteinorally activeHippo pathwayNCI-H226 cellsTEAD subtypepalmitoylationCyr61anti-tumorInhibitorinhibitorinhibit

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