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

IAG933 is a small molecule compound. IAG933 is a direct and selective disruptor of YAP-TEAD protein-protein interaction (PPI). By binding to the Ω-loop pocket of TEAD protein, IAG933 directly prevents YAP/TAZ from forming complexes with TEADs, thereby interfering with YAP's carcinogenic function. IAG933 can be used to study the Hippo signaling pathway and specific types of cancer.

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

IAG933 Chemical Structure

IAG933 Chemical Structure

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IAG933 Related Antibodies

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Description

IAG933 is a small molecule compound. IAG933 is a direct and selective disruptor of YAP-TEAD protein-protein interaction (PPI). By binding to the Ω-loop pocket of TEAD protein, IAG933 directly prevents YAP/TAZ from forming complexes with TEADs, thereby interfering with YAP's carcinogenic function. IAG933 can be used to study the Hippo signaling pathway and specific types of cancer[1].

In Vitro

IAG933 (0.0001-10 μM, 24 h) almost completely inhibits the expression of direct TEAD target genes CCN1, ANKRD1 and CCN2 in both MSTO-211H cells and another Hippo-altered mesothelioma line NCI-H226, with IC50 values between 11 and 26 nM. Particularly in mesothelioma, IAG933 shows half-maximal growth inhibition (GI50) values between 13 and 91 nM irrespective of pathway alterations[1].
IAG933 (0.0001-10 μM, 72 h) shows significant anti-proliferative activity in tumor cell lines with multiple Hippo signaling pathway alterations, especially in pleural mesothelioma cell lines[1].

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

IAG933 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: TEAD-dependent mesothelioma lines
Concentration: 0.37 μM
Incubation Time: 72 h
Result: Showed significant anti-proliferative activity in mesothelioma, hippo altered, and non-hippo mutant cell lines, and the cell line activity decreased to less than 10% after 72 hours of administration
In Vivo

IAG933 (30-240 mg/kg, op.; 24 h) shows rapid and efficient inhibition of TEAD transcription in mouse MSTO-211H cell-derived xenograft (CDX) models in a single dose evaluation experiment[1].
IAG933 (70 and 210 mg/kg, op.; 28 days) prevents mouse morbidity induced by increasing tumor burden in pleura, and antitumor responses are sustained over 4 weeks. IAG933 does not cause weight loss or tolerance problems in mouse models[1].
IAG933 (10 and 30 mg/kg, op.; 14 days) is well tolerated in a rat model where the degree of tumor exposures is proportional to dose and no weight loss was observed[1].
IAG933 (200 mg/kg, op.; 70 days) shows an antitumor response in an NF2-altered PDX model of triple-negative breast cancer[1].

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

Animal Model: NF2-altered PDX model of triple-negative breast cancer[1]
Dosage: 200 mg/kg
Administration: Oral gavage (p.o.)
Result: Demonstrated a favorable tumor response, including deep tumor shrinkage and persistent tumor arrest.
Animal Model: mouse MSTO-211H cell-derived xenograft (CDX) models[1]
Dosage: 30-240 mg/kg
Administration: Oral gavage (p.o.)
Result: Demonstrated dose-dependent antitumor effects, including tumor arrest and significant tumor shrinkage. At a dose of 240 mg/kg, nearly complete regression of the tumor was observed. No weight loss was observed during treatment.
Molecular Weight

529.96

Formula

C27H26ClF2N3O4
SMILES

FC1=C(Cl)[C@]([C@]2=C(C(NC)=O)C=NC(OCCO)=C2F)=C3C(OC([C@@]4(C5=CC=CC=C5)NCCC4)C3)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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IAG933 Related Classifications

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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.

Keywords:

IAG933IAG 933IAG-933YAPYes-associated proteinprotein-protein interactionTEADHippo signaling pathwayMSTO-211H cell-derived xenograft (CDX) modelsInhibitorinhibitorinhibit

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