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Formula | C22H30O2S |
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Molecular Weight | 358.54 | CAS No. | 162520-00-5 | |
Solubility (25°C)* | In vitro | DMSO | 72 mg/mL (200.81 mM) | |
Ethanol | 72 mg/mL (200.81 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Salirasib (Farnesylthiosalicylic acid, FTS) is a potent competitive prenylated protein methyltransferase (PPMTase) inhibitor with Ki of 2.6 μM, which inhibits Ras methylation. Salirasib exerts antitumor effects and induces autophagy. Phase 2. | ||||
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In vitro | Salirasib inhibits the growth of human Ha-ras-transformed Rat1 cells, which correlates well with their inhibition for PPMTase. [1] Salirasib inhibits Ras methylation in Rat-1 fibroblasts, Ras-transformed Rat-1, and B16 melanoma cells. Salirasib also reduces the levels of Ras in cell membranes and inhibits Ras-dependent cell growth, independently of methylation, but via modulation of Ras-Raf communication. [2] In Ras-transformed EJ cells, Salirasib interferes with the activation of Raf-1 and MAPK and inhibits DNA synthesis. [3] | ||||
In vivo | In Panc-1 xenografted nude mice, Salirasib (5 mg/kg i.p.) markedly inhibits tumor growth without systemic toxicity. [4] In male Wistar rats, Salirasib (5 mg/kg i.p.) markedly inhibits thioacetamide-induced -induced liver cirrhosis. [5] In the dy(2J)/dy(2J) mouse model of congenital muscular dystrophy, Salirasib (5 mg/kg i.p.) attenuates fibrosis and improves muscle strength. [6] |
Kinase Assay:[2] |
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Cell Assay:[2] |
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Animal Study:[4] |
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Crosstalk between protein kinase C α and transforming growth factor β signaling mediated by Runx2 in intestinal epithelial cells [ J Biol Chem, 2023, 299(4):103017] | PubMed: 36791912 |
Vemurafenib Inhibits Acute and Chronic Enterovirus Infection by Affecting Cellular Kinase Phosphatidylinositol 4-Kinase Type IIIβ [ Microbiol Spectr, 2023, 11(4):e0055223] | PubMed: 37436162 |
BRAF activation by metabolic stress promotes glycolysis sensitizing NRASQ61-mutated melanomas to targeted therapy [ Nat Commun, 2022, 13(1):7113] | PubMed: 36402789 |
ATAD3A mediates activation of RAS-independent mitochondrial ERK1/2 signaling, favoring head and neck cancer development [ J Exp Clin Cancer Res, 2022, 41(1):43] | PubMed: 35093151 |
A novel antiproliferative PKCα-Ras-ERK signaling axis in intestinal epithelial cells [ J Biol Chem, 2022, 298(7):102121] | PubMed: 35697074 |
Oxymatrine Inhibits Proliferation and Migration of Vulvar Squamous Cell Carcinoma Cells via Attenuation of the RAS/RAF/MEK/ERK Pathway [ Cancer Manag Res, 2020, 12:2057-2067] | PubMed: 32256113 |
MAPK inhibitors induce serine peptidase inhibitor Kazal type 1 (SPINK1) secretion in BRAF V600E-mutant colorectal adenocarcinoma. [ Mol Oncol, 2018, 12(2):224-238] | PubMed: 29193645 |
Dasatinib synergizes with ATRA to trigger granulocytic differentiation in ATRA resistant acute promyelocytic leukemia cell lines via Lyn inhibition-mediated activation of RAF-1/MEK/ERK [ Food Chem Toxicol, 2018, 119:464-478] | PubMed: 29097117 |
The dynamics of ERK signaling in melanoma, and the response to BRAF or MEK inhibition, are cell cycle dependent [ SSRN, 2018, 10.2139/ssrn.3188455] | PubMed: None |
The N-terminal tail coordinates with carbohydrate recognition domain to mediate galectin-3 induced apoptosis in T cells. [ Oncotarget, 2017, 8(30):49824-49838] | PubMed: 28548942 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
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