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This enzyme, along with protein geranylgeranyltransferase types I (EC 2.5.1.59) and II (EC 2.5.1.60), constitutes the protein prenyltransferase family of enzymes. Catalyses the formation of a thioether linkage between the C-1 of an isoprenyl group and a cysteine residue fourth from the C-terminus of the protein. These protein acceptors have the C-terminal sequence CA1A2X, where the terminal residue, X, is preferably serine, methionine, alanine or glutamine; leucine makes the protein a substrate for EC 2.5.1.59. The enzymes are relaxed in specificity for A1, but cannot act if A2 is aromatic. Substrates of the prenyltransferases include Ras, Rho, Rab, other Ras-related small GTP-binding proteins, γ-subunits of heterotrimeric G-proteins, nuclear lamins, centromeric proteins and many proteins involved in visual signal transduction. A zinc metalloenzyme that requires Mg2+ for activity. Group: Enzymes. Synonyms: FTase. Enzyme Commission Number: EC 2.5.1.58. CAS No. 131384-38-8. Storage: Store it at +4 ?C for short term. For long term storage, store it at -20 ?C?-80 ?C. Form: Liquid or lyophilized powder. EXWM-2795; protein farnesyltransferase; EC 2.5.1.58; 131384-38-8; FTase. Cat No: EXWM-2795.
2-Acetylcyclohexanone
2-Acetylcyclohexanone is used in the synthesis of 1-(pyridyl)ethanol derivatives that can reduce keto-esters and ketones. Also used in the synthesis of phenothiazine derivatives that can inhibit protein farnesyltransferase molecules and some that show anti-proliferative activity. Group: Biochemicals. Alternative Names: 2-Acetylcyclohexanone; 2-Acetyl-1-cyclohexanone; 2-Acetylcyclohexanone; NSC 7713; α-Acetylcyclohexanone. Grades: Highly Purified. CAS No. 874-23-7. Pack Sizes: 5g. US Biological Life Sciences.
Worldwide
BMS-214662
BMS-214662 is a Farnesyltransferase inhibitor and a nonsedating benzodiazepine derivative with potential antineoplastic activity. BMS-214662 inhibits the enzyme farnesyltransferase and the post-translational farnesylation of number of proteins involved in signal transduction, which may result in the inhibition of Ras function and apoptosis in susceptible tumor cells. Synonyms: BMS 214662; BMS214662; ARQ-171; ARQ 171; ARQ171; (R)-1-((1H-imidazol-5-yl)methyl)-3-benzyl-4-(thiophen-2-ylsulfonyl)-2,3,4,5-tetrahydro-1H-benzo[e][1,4]diazepine-7-carbonitrile. Grade: 98%. CAS No. 195987-41-8. Molecular formula: C25H23N5O2S2. Mole weight: 489.61.
BMS-214662 hydrochloride
BMS-214662, a nonsedating benzodiazepine derivative, inhibits the enzyme farnesyltransferase and the post-translational farnesylation of number of proteins involved in signal transduction. Treatment with BMS-214662 may result in the inhibition of Ras function and apoptosis in susceptible tumor cells. BMS-214662 may be a useful drug for treating B-CLL and, in particular, an alternative for the therapy of purine analog-resistant or relapsed B-CLL. Synonyms: (3R)-3-benzyl-1-(1H-imidazol-5-ylmethyl)-4-thiophen-2-ylsulfonyl-3,5-dihydro-2H-1,4-benzodiazepine-7-carbonitrile; 7-cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine; ARQ171; ARQ 171; ARQ-171; BMS214662; BMS214662; BMS-214662. Grade: >98%. CAS No. 195981-08-9. Molecular formula: C25H24ClN5O2S2. Mole weight: 526.1.
BMS-214662 mesylate
BMS-214662 mesylate is a potent and selective inhibitor of farnesyltransferase that induces mitochondrial apoptosis in chronic myeloid leukemia stem/progenitor cells, including CD34+38- cells, through activation of protein kinase Cβ. Uses: A potent and selective inhibitor of farnesyltransferase. Synonyms: BMS-214662 mesylate; BMS 214662 mesylate; BMS214662 mesylate; (R)-2,3,4,5-Tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-Benzodiazepine-7-carbonitrile monohydrochloride, (R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine mesylate. Grade: ≥98%. CAS No. 474010-58-7. Molecular formula: C25H25N5O6S3. Mole weight: 585.72.
Chaetomellic Acid A Anhydride
A potent inhibitor of Ras protein farnesyltransferase. Group: Biochemicals. Alternative Names: 3-Methyl-4-tetradecyl-2,5-furandione; Chaetomellic Anhydride; Chaetomellic Anhydride A. Grades: Highly Purified. CAS No. 150240-39-4. Pack Sizes: 25mg. US Biological Life Sciences.
Worldwide
Chaetomellic Acid B Anhydride
A potent inhibitor of Ras protein farnesyltransferase. Group: Biochemicals. Alternative Names: (Z)-3-(7-Hexadecenyl)-4-methyl-2,5-furandione; Chaetomellic Anhydride B. Grades: Highly Purified. CAS No. 84306-79-6. Pack Sizes: 10mg. US Biological Life Sciences.
Worldwide
GGTI-2154
GGTI-2154 is a geranylgeranyltransferase I (GGTase I) inhibitor. GGTI-2154 results not only in halting the growth of aggressive breast tumors but actually in inducing the regression (54 +/- 3%) of all 19 tumors analyzed. The farnesyltransferase (FTase) inhibitor FTI-2148 induced an average of 87 +/- 3% regression in the 13 tumors analyzed. GGTase I, but not FTase, is inhibited in breast tumors after treatment with GGTI-2154, whereas in tumors from mice treated with FTI-2148, only FTase is inhibited. The processing of the geranylgeranylated proteins RhoA, Rap1, and R-Ras, but not the farnesylated proteins H-Ras and HDJ-2, is inhibited in tumors obtained from mice treated with GGTI-2154. GGTI-2154 and FTI-2148 suppress constitutively activated phospho-Erk1/2 and phospho-Akt, induce apoptosis, and induce differentiation toward ductolobular breast epithelium. Synonyms: GGTI-2154; GGTI 2154; GGTI2154. Grade: 98%. CAS No. 251577-10-3. Molecular formula: C24H28N4O3. Mole weight: 420.51.
protein geranylgeranyltransferase type I
This enzyme, along with protein farnesyltransferase (EC 2.5.1.58) and protein geranylgeranyltransferase type II (EC 2.5.1.60), constitutes the protein prenyltransferase family of enzymes. Catalyses the formation of a thioether linkage between the C-1 atom of the geranylgeranyl group and a cysteine residue fourth from the C-terminus of the protein. These protein acceptors have the C-terminal sequence CA1A2X, where the terminal residue, X, is preferably leucine; serine, methionine, alanine or glutamine makes the protein a substrate for EC 2.5.1.58. The enzymes are relaxed in specificity for A1, but cannot act if A2 is aromatic. Known targets of this enzyme include most γ-subunits of heterotrimeric G proteins and Ras-related GTPases such as members of the Ras and Rac/Rho families. A zinc metalloenzyme. The Zn2+ is required for peptide, but not for isoprenoid, substrate binding. Group: Enzymes. Synonyms: GGTase-I; GGTaseI. Enzyme Commission Number: EC 2.5.1.59. CAS No. 135371-29-8. Storage: Store it at +4 ?C for short term. For long term storage, store it at -20 ?C?-80 ?C. Form: Liquid or lyophilized powder. EXWM-2796; protein geranylgeranyltransferase type I; EC 2.5.1.59; 135371-29-8; GGTase-I; GGTaseI. Cat No: EXWM-2796.
protein geranylgeranyltransferase type II
This enzyme, along with protein farnesyltransferase (EC 2.5.1.58) and protein geranylgeranyltransferase type I (EC 2.5.1.59), constitutes the protein prenyltransferase family of enzymes. Attaches geranylgeranyl groups to two C-terminal cysteines in Ras-related GTPases of a single family, the Rab family (Ypt/Sec4 in lower eukaryotes) that terminate in XXCC, XCXC and CCXX motifs. Reaction is entirely dependent on the Rab substrate being bound to Rab escort protein (REP). Post-translational modification with the geranylgeranyl moiety is essential for Rab GTPases to be able to control the processes of membrane docking and fusion. Group: Enzymes. Synonyms: GGTaseII; Rab geranylgeranyltransferase; RabGGTase; geranylgeranyl-diphosphate,geranylgeranyl-diphosphate:protein-cysteine geranyltransferase. Enzyme Commission Number: EC 2.5.1.60. CAS No. 135371-29-8. Storage: Store it at +4 ?C for short term. For long term storage, store it at -20 ?C?-80 ?C. Form: Liquid or lyophilized powder. EXWM-2798; protein geranylgeranyltransferase type II; EC 2.5.1.60; 135371-29-8; GGTaseII; Rab geranylgeranyltransferase; RabGGTase; geranylgeranyl-diphosphate,geranylgeranyl-diphosphate:protein-cysteine geranyltransferase. Cat No: EXWM-2798.
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