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Cat. No. | Product Name | Target | Signaling Pathways |
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T71092 |
Proteasome-IN-3
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Proteasome-IN-3 is an inhibitor of proteasome-associated DUBs. | |||
T74793 |
USP28-IN-3
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DUB | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Ubiquitination |
USP28-IN-3是一种高选择性 USP28 抑制剂,对USP28的IC50 值为 0.1 μM。USP28-IN-3 具有抗癌活性,抑制 USP2、USP7、USP8、USP9x、UCHL3和UCHL5。USP28-IN-3 对人结直肠癌和肺鳞癌细胞具有细胞毒性,通过泛素-蛋白酶体系统对c-Myc的细胞水平进行剂量依赖性下调。 | |||
T77620 |
LMTK3-IN-1
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c-Met/HGFR | Tyrosine Kinase/Adaptors |
LMTK3-IN-1 是一种有效的 ATP 竞争性狐猴酪氨酸激酶 3 (LMTK3) (Kd=2.5 μM) 抑制剂,通过泛素蛋白酶体途径降解 LMTK3 发挥特性。LMTK3-IN-1 在多种癌细胞系和体内 BC 小鼠模型中展现出抗癌活性。 LMTK3-IN-1(10-20 μM) 可诱导 BC 细胞系凋亡。 | |||
T69668 |
CCW 28-3
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CCW 28-3 is a novel potent covalent BRD4 degrader, degrading BRD4 in a proteasome- and RNF4-dependent manner without inhibiting RNF4 autoubiquitination activity. | |||
T76038 |
Ac-Nle-Pro-Nle-Asp-AMC
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Ac-Nle-Pro-Nle-Asp-AMC 是26S 蛋白酶体(26Sproteasome)的特异性底物,适用于分析26S 蛋白酶体中caspase样活性。 | |||
T35481 |
DD 03-171
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Potent and selective BTK Degrader (IC50 = 5.1 nM); degrades BTK in a proteasome- and CRBN-dependent manner. Suppresses BTK signaling and proliferation in mantle cell lymphoma (MCL) cells by degrading BTK, IKFZ1, and IKFZ3 (3 validated targets in B-cell malignancies). Also degrades Ibrutinib (Cat. No. 6813) -resistant C481S-BTK mutant cancer cells. Exhibits no binding against a panel of 468 kinases at 1 μM. Reduces tumor burden and extends survival in lymphoma patient-derived xenograft models. | |||
T37419 | Zetomipzomib | ||
KZR-616, a first-in-class inhibitor of the immunoproteasome, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7) subunits of the immunoproteasome. KZR-616 has the potential for the research of multiple autoimmune diseases[1][2]. KZR-616 also inhibits MECL-1 subunit (IC50=623 nM) and constitutive proteasome β5 subunit (IC50=688 nM). KZR-616 maintains LMP7 and LMP2 selective inhibition in MOLT-4 cells. KZR-616 (250 nM) shows a comparable cytokine inhib... |
Cat. No. | Product Name | Target | Signaling Pathways |
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T2S1837 |
Steviol
甜菊醇,NSC 226902,Hydroxydehydrostevic acid |
Others | Others |
Steviol (NSC-226902) 是一种甜菊糖甙的主要代谢物。它能降低 AQP2 的表达,并促进 AQP2 的降解,从而减缓肾囊肿的生长。 |