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Lonafarnib (SCH 66336) is a selectively farnesyl protein transferase (FPT) inhibitor, inhibiting H-ras, K-ras-4B and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM, respectively. Lonafarnib (8 μM) suppresses PKB/Akt activity as well as the phosphorylation of the Akt substrates glycogen synthase kinase (GSK)-3β, forkhead transcription factor, and BAD in SqCC/Y1 cells. Lonafarnib induces a CCAAT/enhancer-binding protein homologous protein (CHOP)-dependent transactivation of the DR5 promoter, thus induces CHOP-dependent DR5 up-regulation.
| Molecular Weight | 638.82 |
| Formula | C27H31Br2ClN4O2 |
| CAS Number | 193275-84-2 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[2] Nan Soon Wong, et al. Lonafarnib for cancer and progeria
| Related Transferase Products |
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APO866 is an effective inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase; NAMPT) with an IC50 of 0.09 nM. |
| Tolcapone
Tolcapone is a selective, potent and reversible of catechol-O-methyl transferase (COMT) inhibitor with Ki of 30 nM. |
| Tunicamycin
Tunicamycin is a mixture of nucleoside antibiotics that inhibits N-glycosylation and blocks GlcNAc phosphotransferase (GPT). Tunicamycin can cause the accumulation of unfolded proteins within the endoplasmic reticulum (ER) and induce ER stress, leading to impaired DNA synthesis and G1 phase cell cycle arrest. |
| Sandoz 58-035
Sandoz 58-035 is a cholesterol acyltransferase (ACAT) inhibitor. Sandoz 58-035 inhibits the accumulation of cholesteryl esters and inhibits the esterification of cholesterol by 95% in arterial smooth muscle cells in culture. Sandoz 58-035 was used to induce simultaneous activation of unfolded protein response (UPR) and pattern recognition receptors (PRRs) in mouse peritoneal macrophages. |
| OSMI-1
OSMI-1 is a cell permeable inhibitor of OGT (O-GlcNAc transferase) with an IC50 value of 2.7 μM. |
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