Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T23004 |
ML-SA1
Mucolipin synthetic agonist 1 |
Others; TRP/TRPV Channel | Membrane transporter/Ion channel; Others |
ML-SA1 (Mucolipin synthetic agonist 1) 是一种选择性的TRPML 激动剂,通过促进溶酶体的酸化和蛋白酶活性抑制登格病毒 2 和寨卡病毒,抗 DENV2 RNA 和 ZIKV RNA 的IC50分别为 8.3 μM 和 52.99 μM。ML SA1可诱发自噬。ML SA1可用于广谱抗病毒研究。 | |||
T38089 |
2F-Peracetyl-Fucose
1,3,4-Tri-O-acetyl-2-deoxy-2-fluoro-L-fucopyranos |
Others | Others |
2F-Peracetyl-Fucose (1,3,4-Tri-O-acetyl-2-deoxy-2-fluoro-L-fucopyranos) 是一种有效的岩藻糖基转移酶 (FUT)抑制剂,在体外炎症模型中抑制唾液酸化和岩藻糖基化。 | |||
T37547 |
trans-Urocanic Acid
|
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trans-Urocanic acid is a major epidermal chromophore for the immunosuppressive effects of UV radiation that is produced in mammalian stratum corneum by the action of histidine ammonialyase on L-histidine. It contributes to the acidification of the surface of the stratum corneum, and its function has been proposed as that of an endogenous sunscreen, endowing a low-level of protection (SPF ~ 1.5) against UV-induced DNA damage and excessive keratinocyte apoptosis. Upon UVB exposure, trans-urocanic ... | |||
T11191 |
EN6
|
Proton pump; Autophagy | Autophagy; Membrane transporter/Ion channel |
EN6 是一种小分子体内自噬激活剂,其共价靶向溶酶体v-ATP 酶的 ATP6V1A 亚基中的半胱氨酸 277。它以溶酶体依赖性方式清除 TDP-43 聚集体,这是额颞叶痴呆的病原体。它介导的 ATP6V1A 修饰使 v-ATP 酶与 Rags 分离,从而抑制 mTORC1 信号传导、增加溶酶体酸化和激活自噬。 | |||
T69550 | NS-3736 | ||
NS-3736 is a chloride channel inhibitor that has been shown to prevent osteoclastic acidification and resorption. | |||
T72003 |
SKF-104557
|
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N-Despropyl ropinirole is an active metabolite of the dopamine D2 receptor agonist ropinirole. It increases extracellular acidification rates in CHO cells expressing human dopamine D2, D3, and D4 receptors (EC50s = 0.63, 0.063, and 1.23 µM, respectively). N-Despropyl ropinirole is also a potential impurity found in commercial preparations of ropinirole. | |||
T80516 |
human GALP (3-32)
Galanin-like peptide (3-32) |
Neuropeptide Y Receptor | GPCR/G Protein; Neuroscience |
Human GALP (3-32) (Galanin-like peptide (3-32)) 是一种高效的galanin receptor激动剂。在竞争性结合实验中,该化合物对GalR1 (IC50=33 nM) 及GalR2 (IC50=15 nM) 表现出强烈亲和力。此外,human GALP (3-32) 显著增加了转染GalR2 (EC50=360 nM) 的 SH-SY5Y细胞的胞外酸化速率。 | |||
T36116 | Concanamycin B | ||
Concanamycin B is a macrolide antibiotic that selectively inhibits vacuolar type H+-ATPases, also known as V-ATPases (IC50 = 5 nM). In this way, it blocks the acidification of vacuolar organelles as well as early to late endosomal transport. Concanamycin B interferes with bone resorption and maturation of CD8 T lymphocytes. It also prevents processing of major histocompatibility complex (MHC) class II precursors in human B cells, inhibiting the expression of MHC class II molecules on the cell su... | |||
T76042 |
Angiopeptin TFA
|
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Angiopeptin TFA,一种生长抑素的环状八肽类似物,作为sst2/sst5受体部分激动剂,其IC50值为0.26 nM和6.92 nM。该化合物能够抑制生长激素释放及IGF-1(胰岛素样生长因子-1)的产生,同时抑制腺苷酸环化酶活性或刺激细胞外酸化。Angiopeptin TFA在冠状动脉粥样硬化的研究中显示出潜力。 | |||
T83889 |
C-02
|
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C-02是一种由巨噬细胞抑制剂Lonidamine和Cereblon配体Thalidomide组成的蛋白酶体靶向嵌合体(PROTAC)。在20 µM浓度下使用时,可诱导786-O和PANC-1细胞中的Hexokinase 2降解。C-02对786-O、4T1、PANC-1、HGC-27和MCF-7癌细胞具有细胞毒性(IC50分别为34.07、5.08、31.53、6.11和21.65 µM)。同时,20 µM浓度下减少4T1细胞的细胞外酸化率(ECAR)和氧气消耗率(OCR),表明其抑制糖酵解和引起线粒体损伤。在体内,C-02(50 mg/kg)能减少4T1小鼠乳腺癌模型的肿瘤体积,并诱导肿瘤内细胞因子积累和细胞焦亡。 |