| Bioactivity | LB42708 is a potent, selective and orally active farnesyltransferase inhibitor. LB42708 inhibits farnesylation of H-Ras, N-Ras and K-Ras4B with IC50s of 0.8 nM, 1.2 nM and 2.0 nM, respectively[1]. | |||||||||
| Invitro | LB42708 induces cell death despite K-ras prenylation. Growth inhibition by LB42708 is accompanied by G1 and G2/M cell cycle arrests in H-ras and K-ras-transformed RIE cells, respectively. LB42708 induces the upregulation of p21(CIP1/WAF1) and RhoB above the basal level that leads to the cell cycle arrest and to distinct morphological alterations of ras-transformed rat intestinal epithelial (RIE) cells[2]. | |||||||||
| Name | LB42708 | |||||||||
| CAS | 226929-39-1 | |||||||||
| Formula | C30H27BrN4O2 | |||||||||
| Molar Mass | 555.47 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Hee-Jun Na, et al. Inhibition of farnesyltransferase prevents collagen-induced arthritis by down-regulation of inflammatory gene expression through suppression of p21(ras)-dependent NF-kappaB activation. J Immunol. 2004 Jul 15;173(2):1276-83. [2]. Han-Soo Kim, et al. The farnesyltransferase inhibitor, LB42708, inhibits growth and induces apoptosis irreversibly in H-ras and K-ras-transformed rat intestinal epithelial cells. Toxicol Appl Pharmacol. 2006 Sep 15;215(3):317-29. |
LB42708
CAS: 226929-39-1 F: C30H27BrN4O2 W: 555.47
LB42708 is a potent, selective and orally active farnesyltransferase inhibitor. LB42708 inhibits farnesylation of H-Ras,
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