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PYZD-4409 Sale

目录号 : GC17801

PYZD-4409 是泛素激活酶 UBA1 的特异性抑制剂,IC50 为 20 μM(无细胞酶测定)。 PYZD-4409 在恶性细胞中诱导细胞死亡并优先抑制原发性急性髓细胞白血病细胞的克隆形成。

PYZD-4409 Chemical Structure

Cas No.:423148-78-1

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥2,302.00
现货
5mg
¥2,093.00
现货
10mg
¥3,181.00
现货
50mg
¥7,533.00
现货
100mg
¥11,718.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

PYZD-4409 is a novel small molecule inhibitor of the ubiquitin-activating enzyme E1 with IC50 value of 20μM [1].

The ubiquitin-activating enzyme E1 is involved in the fist step of protein degradation. It uses ATP to adenylate and transfers the ubiquitin molecule to the next enzyme E2. It is demonstrated that the ubiquitination pathway is increased in the primary leukemia cells. Thus, inhibition of E1 can be a target of hematologic malignancies treatment. PYZD-4409 is screened out from a chemical library based on the pyrazolidine pharmacophore. The IC50 value(20μM) of it has been evaluated in a cell-free enzymatic assay. PYZD-4409 can also inhibit E1 in cultured K562 leukemia cells. PYZD-4409 causes cell death in leukemia, myeloma and solid tumor cell lines. In clonogenic growth assays, PYZD-4409 is found to reduce the growth of AML cells over normal hematopoietic cells. As an essential role of protein degradation, the inhibition of E1 resluts in the increased amounts of cyclin D3 and p53 [1].

References:
[1] G. Wei Xu, Mohsin Ali, Tabitha E. Wood et al. The ubiquitin-activating enzyme E1 as a therapeutic target for the treatment of leukemia and multiple myeloma. Blood. 2010, 115(11): 2251-2259.

Chemical Properties

Cas No. 423148-78-1 SDF
化学名 (4E)-1-(3-chloro-4-fluorophenyl)-4-[(5-nitrofuran-2-yl)methylidene]pyrazolidine-3,5-dione
Canonical SMILES C1=CC(=C(C=C1N2C(=O)C(=CC3=CC=C(O3)[N+](=O)[O-])C(=O)N2)Cl)F
分子式 C14H7ClFN3O5 分子量 351.67
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.8436 mL 14.2179 mL 28.4357 mL
5 mM 0.5687 mL 2.8436 mL 5.6871 mL
10 mM 0.2844 mL 1.4218 mL 2.8436 mL
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