PYZD-4409
更新时间：2025-09-07 11:06:36
采购访问：20次
| 常用名 | PYZD-4409 | CAS号 | 423148-78-1 |
|---|---|---|---|
| 价格 | 纯度 | 98.0% | |
| 备货期 | 10天 | 库存 | 现货 |
| 产品详情（用途，包装等）
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℃ |
上海化源世纪贸易有限公司
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商品数：396716件
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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 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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- 上海阿拉丁生化科技股份有限公司
- 上海市 上海市 浦东新区
- 产品名：PYZD 4409
- 价格： ￥9999.9/100mg ￥2202.9/10mg ￥4819.9/25mg ￥6749.9/50mg
- 纯度：98.0%
- 备货期：1天
- 联系人：阿拉丁
- 上海化源世纪贸易有限公司
- 上海市 上海市 普陀区
- 产品名：PYZD-4409
- 价格：
- 纯度：98.0%
- 备货期：10天
- 联系人：徐经理
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参考价格：$119/10mM*1mLinDMSO