2. Stem Cell/Wnt Apoptosis
  3. YAP Apoptosis
  4. IAG933

IAG933 (YAP-TEAD-IN-3) is an orally available YAP/TAZ-TEAD inhibitor that has anti-tumor effects and promotes apoptosis. IAG933 YAP-TEAD-IN-3 inhibits Avi-human TEAD4217-434, with an IC50 value of 9 nM.

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IAG933 Chemical Structure

IAG933 Chemical Structure

CAS No. : 2714434-21-4

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10 mM * 1 mL in DMSO
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IAG933 Related Antibodies

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Description

IAG933 (YAP-TEAD-IN-3) is an orally available YAP/TAZ-TEAD inhibitor that has anti-tumor effects and promotes apoptosis. IAG933 YAP-TEAD-IN-3 inhibits Avi-human TEAD4217-434, with an IC50 value of 9 nM[1][2].

IC50 & Target

IC50: 9 nM (YAP-TEAD)[1]
In Vitro

IAG933 also has an inhibitory effect on NCI-H2052, with GI50 (inhibition of cell proliferation) and IC50 (inhibition of YAP reporter gene expression) values of 0.041 μM and 0.048 μM, respectively[1].
IAG933 (0-1 μM, 4 h) directly inhibits the interaction between YAP/TAZ and all four TEAD isoforms, selectively suppressing TEAD-driven transcriptional activity[2].
IAG933 (0.0001-10 μM, 24 h) shows a dose-dependent inhibition of TEAD target gene expression in MSTO211H and NCI-H226 cells, with IC50 values ranging from 11-26 nM[2].
IAG933 (0.001-10 μM, 72 h) demonstrates effective anti-proliferative activity in Hippo-dependent cell lines, with a GI50 of 13-91 nM in mesothelioma cells[2].

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

IAG933 Related Antibodies

Western Blot Analysis[2]

Cell Line: NCI-H2052, MSTO-211H
Concentration: 0, 0.3, 1 μM
Incubation Time: 4 h
Result: Inhibited the binding of YAP and TAZ with TEAD subtypes.

Real Time qPCR[2]

Cell Line: NCI-H2052, MSTO-211H
Concentration: 0.0001, 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 24 h
Result: Decreased the expression of CYR61, ANKRD1, and CTGF.

Cell Viability Assay[2]

Cell Line: MSTO-211H,NCI-H2052,NCI-H226,IST-MES2,NCI-H28，SF-268,NUGC-3,LMSU,NCI-H292,NCI-H522, Ludlu1, MKN-45, NCI-H460, CCK81, LU-99, NCI-H1792, NCI-H1944, HCC-44, SW837, HCC-1171, MDST8, NCI-H1755, CAL-12T, Hs746T, KATO-Ⅲ, CALU-3, RERF-GC-1B
Concentration: 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 72 h
Result: Suppressed the proliferation of mesothelioma and Hippo mutation cell lines showed moderate sensitivity against non-mesothelioma cell lines with Hippo mutations (SF-268, LMSU, and NUGC-3).
In Vivo

IAG933 (30-240 mg/kg, i.g., once a day, 28 days) shows a dose-dependent anti-tumor effect in mouse xenograft models, promoting cell apoptosis[2].
IAG933 (3-30 mg/kg, i.g., once a day, 2 weeks) causes tumor regression in the MSTO-211H rat xenograft model[2].

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

Animal Model: Mouse MSTO-211H cell-derived xenograft (CDX) model; mouse NCI-H226 cell-derived xenograft (CDX) model[2]
Dosage: 30, 60, 120, 240 mg/kg, single dose; 70, 210 mg/kg, once daily, 28 days
Administration: i.g.
Result: Had a short half-life in mice, inhibiting the transcription of TEAD in the body, promoting apoptosis, and lowering the expression of BCL2L1 and MCL1.
Led to tumor regression and a decrease in Ki67 expression.
Animal Model: A rat MSTO-211H xenograft model[2]
Dosage: 3, 10, 30 mg/kg, once daily, 2 weeks
Administration: i.g.
Result: Showed the tumor stagnant at 10 mg/kg, and shrank at 30 mg/kg.
Molecular Weight

529.96

Formula

C27H26ClF2N3O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC(C(F)=CC1=C2C[C@](C3=CC=CC=C3)([C@@H]4CCCN4)O1)=[C@]2[C@@]5=C(C(NC)=O)C=NC(OCCO)=C5F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (235.87 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 1.8869 mL 9.4347 mL 18.8693 mL
5 mM 0.3774 mL 1.8869 mL 3.7739 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. 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

Purity: 99.81%

SDS (251 KB)

COA (256 KB) HNMR (263 KB) LCMS (87 KB)

Handling Instructions (2659 KB)
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. 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 1.8869 mL 9.4347 mL 18.8693 mL 47.1734 mL
5 mM 0.3774 mL 1.8869 mL 3.7739 mL 9.4347 mL
10 mM 0.1887 mL 0.9435 mL 1.8869 mL 4.7173 mL
15 mM 0.1258 mL 0.6290 mL 1.2580 mL 3.1449 mL
20 mM 0.0943 mL 0.4717 mL 0.9435 mL 2.3587 mL
25 mM 0.0755 mL 0.3774 mL 0.7548 mL 1.8869 mL
30 mM 0.0629 mL 0.3145 mL 0.6290 mL 1.5724 mL
40 mM 0.0472 mL 0.2359 mL 0.4717 mL 1.1793 mL
50 mM 0.0377 mL 0.1887 mL 0.3774 mL 0.9435 mL
60 mM 0.0314 mL 0.1572 mL 0.3145 mL 0.7862 mL
80 mM 0.0236 mL 0.1179 mL 0.2359 mL 0.5897 mL
100 mM 0.0189 mL 0.0943 mL 0.1887 mL 0.4717 mL
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IAG933 Related Classifications

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  • 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:

IAG9332714434-21-4YAP-TEAD-IN-3IAG 933IAG-933YAPApoptosisYes-associated proteinInduce apoptosisanti-tumormesothelioma cellsInhibitorinhibitorinhibit

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