PYZD-4409

产品详情：

发布时间： 2024-07-15 12:35:15

CAS号：423148-78-1

常用名： PYZD-4409

价格：

纯度： 98.0%

备货期： 10天

库存： 现货

其他详情（用途，包装）：
用途： PYZD-4409 is a novel small molecule inhibitor of Ubiquitin-activating enzyme UBA1/E1 enzyme with an IC50 of 20 uM (cell-free enzymatic assay).IC50 Value: 20 uM (cell-free enzymatic assay) [1]Target: E1 enzyme (Ubiquitin-activating enzyme)in vitro: PYZD-4409 inhibited the ATP-dependent activation of ubiquitin and subsequent transfer of the activated ubiquitin from the E1 to the common human E2 enzyme UBE2E2 in a gel-based assay. The IC50 of inhibition was estimated to be 20μM in a cell-free enzymatic assay. Suggesting specificity of PYZD-4409 for the E1 enzyme, the compound had no effect on unrelated enzymes such as α-Mannosidase II glycosylation enzyme or Luciferase at concentrations up to 100μM (data not shown). It also did not inhibit the summo E1, Uba2, at concentrations up to 100μM. In 5 of 8 leukemia and myeloma cell lines, PYZD-4409 induced cell death with a LD50 less than 10μM. Myeloma cell lines were particularly sensitive to E1 inhibition because PYZD-4409 induced cell death with 3 of 4 myeloma cell lines (ie, LP1, KMS11, and U226) having an LD50 of 3μM or less. In contrast, solid tumor cell lines were less sensitive with an LD50 of approximately 15 to 20μM [1]. in vivo: SCID mice were injected subcutaneously with MDAY-D2 murine leukemia cells and then treated with PYZD-4409 (10 mg/kg) or buffer control intraperitoneally daily on alternate days over 8 days. Sixteen days after tumor implantation, the mice were killed, and the tumors excised and weighed. Compared with control-treated mice, treatment with PYZD-4409 delayed tumor growth and decreased tumor weight without untoward toxicity. Inhibition of the E1 can achieve an antitumor effect in vivo [1]. 物理化学性质： CAS号：423148-78-1 常用中文名：PYZD-4409 常用英文名：PYZD 4409 分子式：C14H7ClFN3O5 分子量：351.67400 密度：N/A 沸点：N/A 熔点：N/A 闪点：N/A 储存条件：2-8℃

供应商信息：

公司名：上海念兴实业有限公司推荐

认证状态： 已认证供应商

商品数： 403768件

电话： 18916513247

地址： 2222 Huancheng Road, Juyuan New District, Jiading District, Shanghai

地区： 上海市普陀区

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2022-03-04 价格：￥9999.9 PYZD 4409

2024-07-15 价格：需询单 PYZD-4409

2021-02-06 价格：￥15613.0 PYZD-4409

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PYZD-4409

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