PYZD-4409

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更新时间： 2025-09-07 11:06:36

CAS号：423148-78-1

常用名： PYZD-4409

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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：上海化源世纪贸易有限公司推荐

认证状态： 已认证供应商

商品数： 396716件

电话： 53555033

地址： 上海市普陀区金沙江路1759号圣诺亚大厦B座

地区： 上海市普陀区

联系人： 徐经理

联系人电话： 13311869306

邮件：xuqm@chemsrc.com

网址：http://www.chemsrc.com

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公司介绍：
化源网，2015 年正式成立，是专注服务全球精细化学与生物医药研发领域的专业社群电商平台。
平台严选优质品牌商家直供，以正品低价为核心优势，搭配简洁易操作的商城界面，为研发人员提供一站式采购方案，全程保障高效便捷的服务体验。

其他供应商价格：

2022-03-04 价格：￥9999.9 PYZD 4409

2021-02-06 价格：￥15613.0 PYZD-4409

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PYZD-4409价格

PYZD-4409

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