IAG933 free base · Synonyms: YAP-TEAD-IN-3

IAG933 is a selective and orally efficacious YAP1/WWTR1-panTEAD protein-protein interaction inhibitor.

For research use only. Not for human or veterinary use.

Target YAP Apoptosis

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

IAG933 structure

CAS No.: 2714434-21-4

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 850.00	BP-02250-100mg	In stock	Get quote
250 mg	USD 1,450.00	BP-02250-250mg	In stock	Get quote
500 mg	USD 1,980.00	BP-02250-500mg	In stock	Get quote
1 g	USD 2,980.00	BP-02250-1g	In stock	Get quote
2 g	Inquire	BP-02250-2g	In stock	Inquire
5 g	Inquire	BP-02250-5g	In stock	Inquire

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Description

IAG933 is a selective and orally efficacious YAP1/WWTR1(TAZ)-panTEAD protein-protein interaction inhibitor.

Biological activity

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. IAG933 (0-1 μM, 4 h) directly inhibits the interaction between YAP/TAZ and all four TEAD isoforms, selectively suppressing TEAD-driven transcriptional activity. 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. 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. 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. IAG933 (3-30 mg/kg, i.g., once a day, 2 weeks) causes tumor regression in the MSTO-211H rat xenograft model.

Identifiers

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
InChIKey: HUVOYQMXUNTUAI-DCFHFQCYSA-N

Specifications

MW (average): 529.9630
Formula: C₂₇H₂₆ClF₂N₃O₄
CAS No.: 2714434-21-4
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 year

Solubility

Soluble in DMSO

In vitro: DMSO : 116.67 mg/mL

Documents

References

[1]. Bordas V, et al. Preparation of biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors. World Intellectual Property Organization, WO2021186324 A1. 2021-09-23.

[2]. Emilie A Chapeau， et al. Direct and selective pharmacological disruption of the YAP-TEAD interface by IAG933 inhibits Hippo-dependent and RAS-MAPK-altered cancers. Nat Cancer. 2024 Jul;5(7):1102-1120.

Same target

Search YAP

Same research area

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