BiochemProbe — Life Science Research Reagents

BAY-593 free base · Synonyms: BAY 593 · BAY593

BAY-593 is an orally active inhibitor of geranylgeranyltransferase-I.

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

Target YAP GGTase
Research area Cancer
Purity >98% Stock Inquire

BAY-593 structure

CAS No.: 2413020-56-9

Download structure (.mol)

Pack sizes & pricing

Size Price SKU Stock
50 mg USD 734.00 BP-02274-50mg In stock Get quote
100 mg USD 1,136.00 BP-02274-100mg In stock Get quote
250 mg USD 1,942.00 BP-02274-250mg In stock Get quote
1 g Inquire BP-02274-1g In stock Inquire
5 g Inquire BP-02274-5g In stock Inquire

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Description

BAY-593 is an orally active inhibitor of geranylgeranyltransferase-I (GGTase-I) that effectively blocks the activation of Rho-GTPases, leading to the inactivation of YAP1/TAZ signaling pathways and demonstrating significant antitumor activity. In cellular assays, BAY-593 exhibits potent antiproliferative effects, with an IC50 of 38.4 nM in HT-1080 fibrosarcoma cells and 564 nM in MDA-MB-231 breast cancer cells.

Biological activity

In Vitro BAY-593 (0.5 nM-10 μM; 72 h) inhibits the proliferation of HT-1080 and MDA-MB-231 cells with the IC50 values of 0.038 and 0.564 μM, respectively In Vivo BAY-593 (2.5-20 mg/kg; oral administration; 14 days) shows dose-dependent antitumor activity in HT-1080 fibrosarcoma and MDA-MB-231 triple negative breast cancer xenotransplantation mouse models

Identifiers

SMILES
O(C)C1=C([C@H]2C3(CCN(C([C@]([C@@](F)(F)F)(OC)C4=CC=CC=C4)=O)CC3)CCNC2)C=CC=C1
InChIKey
CUNCJCWHVHIRLT-SQJMNOBHSA-N

Specifications

MW (average)
476.5311
Formula
C26H31F3N2O3
CAS No.
2413020-56-9
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 4℃, sealed storage, away from moisture, 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

In vitro
DMSO : 116.67 mg/mL

References

[1]. Graham K, et al. Discovery of YAP1/TAZ pathway inhibitors through phenotypic screening with potent anti-tumor activity via blockade of Rho-GTPase signaling. Cell Chem Biol. 2024 Mar 19:S2451-9456(24)00087-4.

Same target

Search YAP

Same research area

Search Cancer