B581
Synonym(s):N-[2(S)-(2(R)-2-Amino-3-mercaptopropylamino)-3-methylbutyl]-L -phenylalanyl-L -methionine trifluoroacetate salt
- CAS NO.:149759-96-6
- Empirical Formula: C22H38N4O3S2
- Molecular Weight: 470.69
- MDL number: MFCD00236999
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-05-18 11:31:20
What is B581?
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). It prevents farnesylation of Ras and inhibits proliferation of cells transformed by Ras farnesylation. In a dog model of subarachnoid hemorrhage, it reduces GTP-Ras in spastic basilar arteries, decreases angiographic vasospasm, and improves clinical scores.
The Uses of B581
FTase Inhibitor I is a potent, selective, peptidomimetic FTase inhibitor.
What are the applications of Application
FTase Inhibitor I is a potent, selective, peptidomimetic FTase inhibitor
Definition
ChEBI: A dipeptide obtained from the tetrapeptide Cys-Val-Phe-Met by reduction of the amide carbonyl groups of the Cys and Val residues.
Enzyme inhibitor
This cell-permeable CAAX peptidomimetic (FW = 470.70 g/mol; FWtrifluoracetate-salt = 583.71 g/mol; CAS 149759-96-6), named as N-[2(S)- (2(R)-2-amino-3-mercaptopropylamino)-3-methylbutyl]-L-phenylalanyl-L methionine), binds to and prevents protein farnesyltransferase (IC50 = 21 nM) from interacting with C-terminal L-Cys-L-Val-L-Phe-L-Met substrate recognition sequences that are present in its natural substrates. Otherwise hydrophilic proteins associate with membranes by means of enzymatic attachment of hydrophobic moieties to their C-termini. Whereas prenylation occurs in the cytosol, post-prenylation processing is accomplished on the cytoplasmic surface of the endoplasmic reticulum and Golgi apparatus. B581 inhibits prenylation and processing of H-ras and lamin A. B581 specifically blocks farnesylated, but not geranylgeranylated or myristylated, oncogenic ras signaling and transformation.
Properties of B581
Boiling point: | 716.1±60.0 °C(Predicted) |
Density | 1.161±0.06 g/cm3(Predicted) |
storage temp. | −20°C |
solubility | H2O: soluble |
form | solid |
pka | 3.04±0.10(Predicted) |
color | white |
Safety information for B581
Computed Descriptors for B581
New Products
(R)-3-Aminobutanenitrile Hydrochloride 4-Aminotetrahydropyran-4-carbonitrile Hydrochloride 4-AMINO-TETRAHYDRO-PYRAN-4-CARBOXYLIC ACID HCL 4-AMINO-TETRAHYDRO-PYRAN-4-CARBOXYLIC ACID 1,4-Dioxa-8-azaspiro[4.5]decane 5-Bromo-2-nitropyridine SODIUM AAS SOLUTION ZINC AAS SOLUTION BUFFER SOLUTION PH 10.0(BORATE) GOOCH CRUCIBLE SINTERED AQUANIL 5 BERYLLIUM AAS SOLUTION AMOXICILLIN (AMOXYCILLIN) TRIHYDRATE ACICLOVIR AMLODIPINE SODIUM METHYL PARABEN Methylcobalamin (vitamin B12) SODIUM VALPROATE 5-Fluoro-2-iodo-3-methylaniline Ethyl 3-(furan-2-yl)-3-hydroxypropanoate 1-Methyl-6-oxo-1,6-dihydropyridazine-3-carbonitrile 3-Bromo-2-hydroxybenzeneacetic acid 5-Iodo-3-methyl-2-nitropyridine 1-(3-Chloro-2-hydroxyphenyl)-2-propanoneRelated products of tetrahydrofuran
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