TD1092 是一种泛凋亡抑制蛋白 (IAP) 降解剂，可降解cIAP1,cIAP2和XIAP。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。
| 生物活性 | TD1092 is a pan-IAPdegrader, degradescIAP1,cIAP2, andXIAP. TD1092 activatesCaspase3/7, and promotescancercellsApoptosisviaIAPdegradation. TD1092 inhibitsTNFαmediatedNF-κBpathway and reduces the phosphorylation ofIKK, IkBα, p65, and p38. TD1092 can act asPROTAC, and is used forcancerresearch[1]. |
| IC50& Target[1] | cIAP1 | cIAP2 | XIAP | Caspase 3 | Caspase-7 |
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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]。
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. |
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| 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. |
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