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Manumycin A

Ras farnesyltransferase inhibitor
 
ALX-350-241-M001 1 mg 217.00 USD
 
ALX-350-241-M005 5 mg 653.00 USD
 
ALX-350-241-M010 10 mg 951.00 USD
Do you need bulk/larger quantities?
 
Replaces Prod. #: BML-G236

Potent, selective and competitive inhibitor of Ras farnesyltransferase (IC50=30nM). Does not affect geranylgeranyltransferase (IC50=180µM). Inhibition is competitive with respect to farnesyl pyrophosphate and non-competitive with respect to Ras. Inhibits neutral sphingomyelinase. Cell permeable. Blocks insulin-induced MAP kinase activation in rat cardiac myocytes (19µM).

Product Specification

Formula:C31H38N2O7
 
MW:550.6
 
Source:Isolated from Streptomyces parvulus.
 
CAS:52665-74-4
 
Purity:≥96% (HPLC)
 
Identity:Determined by 1H-NMR.
 
Appearance:Yellow to brown powder.
 
Solubility:Soluble in methanol or DMSO; insoluble in water.
 
Shipping:Shipped on Blue Ice
 
Short Term Storage:+4°C
 
Long Term Storage:-20°C
 
Use/Stability:Store, as supplied, at -20°C for up to 1 year. Store solutions at -20°C for up to 3 months.
 
Handling:Protect from light.
 
350-241
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350-241

Product Literature References

Pathobiology of renal-specific oxidoreductase/myo-inositol oxygenase in diabetic nephropathy: its implications in tubulointerstitial fibrosis: P. Xie, et al.; Am. J. Physiol. Renal Physiol. 298, F1393 (2010), Abstract; Full Text
An HTS approach to screen for antagonists of the nuclear export machinery using high content cell-based assays: F. Zanella, et al.; Assay Drug Dev. Technol. 5, 333 (2007), Abstract;
Binding of manumycin A inhibits IkappaB kinase beta activity: M. Bernier, et al.; J. Biol. Chem. 281, 2551 (2006), Abstract;
Enhancement of manumycin A-induced apoptosis by methoxyamine in myeloid leukemia cells: M. She, et al.; Leukemia 19, 595 (2005), Abstract;
Manumycin A and its analogues are irreversible inhibitors of neutral sphingomyelinase: C. Arenz, et al.; ChemBioChem 2, 141 (2001), Abstract;
Manumycin inhibits ras signal transduction pathway and induces apoptosis in COLO320-DM human colon tumour cells: A. Di Paolo, et al.; Br. J. Cancer 82, 905 (2000), Abstract;
Protein kinase C, but not tyrosine kinases or Ras, plays a critical role in angiotensin II-induced activation of Raf-1 kinase and extracellular signal-regulated protein kinases in cardiac myocytes: Y. Zou et al.; J. Biol. Chem. 271, 33592 (1996), Abstract;
Farnesyltransferase inhibitors: Ras research yields a potential cancer therapeutic: J.B. Gibbs, et al.; Cell 77, 175 (1994), Abstract;
Identification of Ras farnesyltransferase inhibitors by microbial screening: M. Hara et al.; PNAS 90, 2281 (1993), Abstract;
Inhibitors of Ras farnesyltransferases: F. Tamanoi; TIBS 18, 349 (1993), (Review), Abstract;

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