A potent and selective FTase inhibitor
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FTase Inhibitor I

Item No. 22755

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(2S)-2-[[(2R)-2-amino-3-mercaptopropyl]amino]-3-methylbutyl]-L-phenylalanyl-L-methionine
CAS Number
149759-96-6
Synonyms
  • Farnesyltransferase Inhibitor I
Molecular Formula
C22H38N4O3S2
Formula Weight
470.7
Purity
≥95%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Water: Soluble
SMILES
O=C(N[C@H](C(O)=O)CCSC)[C@@H](NC[C@H](C(C)C)NC[C@@H](N)CS)CC1=CC=CC=C1
InChi Code
InChI=1S/C22H38N4O3S2/c1-15(2)20(24-12-17(23)14-30)13-25-19(11-16-7-5-4-6-8-16)21(27)26-18(22(28)29)9-10-31-3/h4-8,15,17-20,24-25,30H,9-14,23H2,1-3H3,(H,26,27)(H,28,29)/t17-,18+,19+,20-/m1/s1
InChi Key
QISLMXIYRQCLIR-FUMNGEBKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $81

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    1 mg

    $152

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    Product Description

    FTase inhibitor I is a potent inhibitor of farnesyltransferase (FTase; IC50 = 21 nM) that is greater than 30-fold selective for FTase over geranylgeranyl transferase (GGTase; IC50 = 790 nM).1 It prevents farnesylation of Ras and inhibits proliferation of cells transformed by Ras farnesylation.1,2 In a dog model of subarachnoid hemorrhage, it reduces GTP-Ras in spastic basilar arteries, decreases angiographic vasospasm, and improves clinical scores.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Garcia, A.M., Rowell, C., Ackermann, K., et al. Peptidomimetic inhibitors of Ras farnesylation and function in whole cells. The Journal of Biological Chemisty 268(25), 18415-18418 (1993).

    2. Cox, A.D., Garcia, A.M., Westwick, J.K., et al. The CAAX peptidomimetic compound B581 specifically blocks farnesylated, but not geranylgeranylated or myristylated, oncogenic ras signaling and transformation. The Journal of Biological Chemisty 269(30), 19203-19206 (1994).

    3. Yamaguchi, M., Zhou, C., Nanda, A., et al. Ras protein contributes to cerebral vasospasm in a canine double-hemorrhage model. Stroke 35(7), 1750-1755 (2004).