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Pifithrin-α (hydrobromide)

产品编号: DC9505
Pifithrin-α (hydrobromide)
结构式
63208-82-2
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中国地区超过5000个高品质化合物库存
应用领域
Pifithrin-α is an inhibitor of p53, inhibiting p53-dependent transactivation of p53-responsive genes.
化学性质生物活性化合物的使用COA & MSDS相关产品产品说明书
Cas No.: 63208-82-2
名称:
别名: Pifithrin hydrobromide; Pifithrin-α hydrobromide; PFTα hydrobromide
SMILES: N=C1N(CC(C2=CC=C(C)C=C2)=O)C(CCCC3)=C3S1.Br
分子式: C16H19BrN2Os
分子量: 367.3039
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: Pifithrin-α is an inhibitor of p53, inhibiting p53-dependent transactivation of p53-responsive genes. Pifithrin-α (PFTα) was originally thought to be a specific inhibitor of signaling by the tumor suppressor protein p53. Pifithrin-α can protect cells from p53-mediated apoptosis induced by various stimuli and reduce sensitivity of mice to gamma radiation. Pifithrin-α, in addition to p53, can inhibit heat shock and glucocorticoid receptor (GR) signaling, and they suggested that Pifithrin-α targets a factor common to all three signal transduction pathways, such as the hsp90/hsp70-based chaperone machinery. Moreover, it reduces activation of glucocorticoid receptor and rescues mouse thymocytesin vitro and in vivo from apoptotic death after dexamethasone treatment. Pifithrin-α affected both signaling pathways in a p53-independent manner. These observations suggest that Pifithrin-α targets some unknown factor that is common for three major signal transduction pathways. Pifithrin-α has potent antiapoptotic activity (EC50 of 4.16 μM ). Pifithrin-α has a pKa of 9.11 and is an ionic species in physiological medium, whereas the tricyclic derivative has a pKa of 4.36 and exists as the neutral free base at pH 7. The tricyclic derivative is very hydrophobic, with a log P of 4.26. Although Pifithrin-α is generally used at 10?30 μM concentration, the aqueous solubility of its derivative is only 0.2 μM, and it can form a visible precipitate under conditions of typical use. Modification of the carbonyl function creates a stable analogue of Pifithrin-α that remains soluble indefinitely.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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