FTase Inhibitor IA potent, selective, peptidomimetic FTase inhibitor

FTase Inhibitor I (CAS 149759-96-6)

FTase Inhibitor I | CAS 149759-96-6 is rated 5.0 out of 5 by 1.
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Synonym: B581
Application: A potent, selective, peptidomimetic FTase inhibitor
CAS Number: 149759-96-6
Purity: ≥98%
Molecular Weight: 470.69
Molecular Formula: C22H38N4O3S2
* Refer to Certificate of Analysis for lot specific data (including water content).
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FTase Inhibitor I is a potent, cell-permeable, selective, peptidomimetic inhibitor of Farnesyl Transferase (FTase). It is ~37-fold more active against Farnesyl Transferase (FTase) than against GGTase (geranylgeranyltransferase). Is also very resistant to proteolysis.


References

1. Cox, A D., et al., 1994. The CAAX peptidomimetic compound B581 specifically blocks farnesylated, but not geranylgeranylated or myristylated, oncogenic ras signaling and transformation. The Journal of biological chemistry. 269(30): 19203-6. PMID: 8034681
2. Garcia, A M., et al., 1993. Peptidomimetic inhibitors of Ras farnesylation and function in whole cells. The Journal of biological chemistry. 268(25): 18415-8. PMID: 8360140
3. Yamaguchi, Mitsuo., et al., 2004. Ras protein contributes to cerebral vasospasm in a canine double-hemorrhage model. Stroke; a journal of cerebral circulation. 35(7): 1750-5. PMID: 15143294

Physical State :
Solid
Solubility :
Soluble in DMSO (5 mg/ml), and water (1 mg/ml).
Storage :
Store at -20° C
Melting Point :
334.02° C (Predicted)
Boiling Point :
716.11° C at 760 mmHg (Predicted)
Density :
1.16 g/cm3 (Predicted)
Refractive Index :
n20D 1.57 (Predicted)
IC50 :
FTase: IC50 = 21 nM; GGTase: IC50 = 790 nM; Sprague-Dawley brain FTase: IC50 = 34 nM (rat)
pK Values :
pKa: 3.04 (Predicted), pKb: 9.41 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
132887
MDL Number :
MFCD00236999
SMILES :
CC(C)[C@@H](CN[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](CCSC)C(=O)O)NC[C@H](CS)N

Download SDS (MSDS)

Certificate of Analysis

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Rated 5 out of 5 by from Cox Cox, AD. et al. (PubMed 8034681) found that B581 (FTase Inhibitor I) specifically blocks farnesylated, but not geranylgeranylated or myristylated, oncogenic ras signaling and transformation in NIH 3T3 cells. -SCBT Publication Review
Date published: 2015-06-25
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