L-744,832

BML-G242

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Farnesyltransferase inhibitor

Ras farnesyltransferase inhibitor. Induces tumor regression in transgenic mice with multiple oncogenic mutations by mediating alterations in both cell cycle control and apoptosis. Induces p21 expression and arrests cells at G1. Causes enhanced mitotic sensitivity to taxol.

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Product Details

Appearance	White solid.
CAS	1177806-11-9
Couple Target	Farnesyltransferase
Couple Type	Inhibitor
Formula	C₂₆H₄₇Cl₂N₃O₆S₂
MW	632.7
Purity	≥98% (TLC)
Solubility	Soluble in DMSO, water, or acetonitrile.

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended. Store solutions at -20°C for up to 3 months.
Long Term Storage	-20°C
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

A novel role of farnesylation in targeting a mitotic checkpoint protein, human Spindly, to kinetochores: Moudgil, D. K., Westcott, N., et al.; J. Cell Biol. 208, 881 (2015), Abstract
Disruption of lamin B1 and lamin B2 processing and localization by farnesyltransferase inhibitors: Adam, S. A., Butin-Israeli, V., et al.; Nucleus 4, 142 (2013), Abstract
Niche-based screening identifies small-molecule inhibitors of leukemia stem cells: Hartwell, K. A., Miller, P. G., et al.; Nat. Chem. Biol. 9, 840 (2013), Abstract
Farnesyltransferase inhibitors interact synergistically with the Chk1 inhibitor UCN-01 to induce apoptosis in human leukemia cells through interruption of both Akt and MEK/ERK pathways and activation of SEK1/JNK: Y. Dai, et al.; Blood 105, 1706 (2005), Abstract
Normoxic and hypoxic regulation of vascular endothelial growth factor (VEGF) by astrocytoma cells is mediated by Ras: M.M. Feldkamp, et al.; Int. J. Cancer 81, 118 (1999), Abstract
A farnesyltransferase inhibitor induces tumor regression in transgenic mice harboring multiple oncogenic mutations by mediating alterations in both cell cycle control and apoptosis: R.E. Barrington, et al.; Mol. Cell Biol. 18, 85 (1998), Abstract
A farnesyl-protein transferase inhibitor induces p21 expression and G1 block in p53 wild type tumor cells: L. Sepp-Lorenzino & N. Rosen; J. Biol. Chem. 273, 20243 (1998), Abstract
Farnesyl transferase inhibitors cause enhanced mitotic sensitivity to taxol and epothilones: M.M. Moasser, et al.; PNAS U.S.A. 95, 1369 (1998), Abstract

Last modified: May 29, 2024

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L-744,832

BML-G242

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