1. PROTAC Apoptosis
  2. PROTACs IAP Caspase
  3. TD1092

TD1092 是一种泛凋亡抑制蛋白 (IAP) 降解剂,可降解 cIAP1, cIAP2XIAP。TD1092 激活细胞凋亡蛋白酶 (apoptosis 3/7),并通过促进 IAP 降解,导致癌细胞凋亡 (apoptosis)。同时,TD1092 还能够阻断 TNFα 介导的 NF-κB 信号通路,抑制 IKK,IkBα,p65,和 p38 的磷酸化。TD1092 可作为 PROTAC,用于癌症研究。

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TD1092 Chemical Structure

TD1092 Chemical Structure

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1 mg ¥7300
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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TD1092 is a pan-IAP degrader, degrades cIAP1, cIAP2, and XIAP. TD1092 activates Caspase 3/7, and promotes cancer cells apoptosis via IAP degradation. TD1092 inhibits TNFα mediated NF-κB pathway and reduces the phosphorylation of IKK, IkBα, p65, and p38. TD1092 can act as PROTAC, and is used for cancer research[1].

IC50 & Target[1]

cIAP1

 

cIAP2

 

XIAP

 

Caspase 3

 

Caspase-7

 

体外研究
(In Vitro)

TD1092 (0.1 μM-10 μM; 0.5-6 小时) 以剂量和时间依赖的方式有效地降解 cIAP1, cIAP2 和 XIAP [1]
TD1092 (0.01, 0.1 和 1 μM ;18 小时) 能够激活 MCF-7 细胞中的半胱天冬酶 3 和 7[1]
TD1092 (1 μM; 48 或 72 小时) 促进癌细胞死亡[1]
TD1092 (0.1 μM; 24 小时) 抑制受 TNFα 诱导的三阴性乳腺癌细胞的迁徙和入侵[1]
TD1092 (1 μM; 6 小时) 抑制 TNFα 诱导的 NF-κB 信号通路和上皮-间充质转化 (EMT)[1]
TD1092 (1 μM; 72 小时) 抑制 MCF-7 细胞生长,IG50 为 0.395 μM[1]

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

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: (1) 0, 0.1, 1, 10 μM or 0.1 μM
(2) 0.1 μM, with or without 100 ng/mL TNFα
Incubation Time: 18 hours or 0.5, 1, 2, 4, 6 hours for (1) and 4 hours for (2)
Result: Dose- and time-dependently decreases the protein level of cIAP1, cIAP2, and XIAP.
Inhibited the phosphorylation of IKK, IkBα, p65, and p38 mediated by TNFα.
Counterbalanced the effect of TNFα on the levels of E-cadherin (CDH1; an epithelial marker) and vimentin (VIM; a mesenchymal marker).

Cell Migration Assay [1]

Cell Line: MDA-MB-231 and MDA-MB-157 cells
Concentration: 0.1 μM; with or without 100 ng/mL TNFα
Incubation Time: 24 hours
Result: Inhibited TNFα-induced (100 ng/mL) migration and invasion against two triple-negative breast cancer (TNBC; MDA-MB-231 and MDA-MB-157) cell lines.
分子量

987.19

Formula

C55H70N8O9

性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

纯度 & 产品资料
参考文献

TD1092 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • 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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TD1092
目录号:
HY-151966
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