1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Apoptosis
  2. HSP Apoptosis
  3. PET-16

PET-16 是一种选择性 HSP70 抑制剂,可与底物结合域的变构口袋结合。PET-16 抑制 HSP70 在 ATP 结合状态和 ADP 结合状态之间循环的能力。PET-16 诱导多发性骨髓瘤细胞凋亡 (apoptosis)。

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PET-16 Chemical Structure

PET-16 Chemical Structure

CAS No. : 34387-64-9

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PET-16 is a selective HSP70 inhibitor that binds to an allosteric pocket of the substrate-binding domain. PET-16 inhibits the ability of HSP70 to cycle between ATP-bound and ADP-bound states. PET-16 induces apoptosis in multiple myeloma[1].

体外研究
(In Vitro)

PET-16(0.01-100 μM;72 小时)在多发性骨髓瘤 (MM) 细胞系中表现出细胞毒性,HSP70 稳态水平最高的细胞系表现出最低的 IC50[1]
PET-16(3 μM;24 小时)诱导多发性骨髓瘤细胞凋亡,同时伴有蛋白毒性应激[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: U266, H929, MM1.S, RPMI-8226 and OCI-MY5 cells
Concentration: 0.01 μM, 0.1 μM, 1 μM.10 μM, 100 μM
Incubation Time: 72 h
Result: All of the MM lines showed cytotoxicity.

Apoptosis Analysis[1]

Cell Line: U266, H929, MM1.S, RPMI-8226 and OCI-MY5 cells
Concentration: 3 μM
Incubation Time: 24 h
Result: Induced apoptosis in treated cells.
体内研究
(In Vivo)

PET-16(5-10 mg/kg;腹腔注射;每周两次;持续 3 周)显著降低小鼠的 p-FAK 和 BRAF 染色[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) mice injected with 1205Lu human melanoma cells[1]
Dosage: 5 mg/kg, 10 mg/kg
Administration: i.p. injection; twice a week; for 3 weeks
Result: Markedly decreased p-FAK and BRAF staining.
分子量

443.31

Formula

C26H20BrP

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
PET-16
目录号:
HY-122184
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