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KM91104

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Chemical Structure| 304481-60-5 同义名 : -
CAS号 : 304481-60-5
货号 : A1249487
分子式 : C14H12N2O4
纯度 : 98%
分子量 : 272.256
MDL号 : MFCD00587366
存储条件:

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(385.67 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 The vacuolar H+ adenosine-triphosphatase (v-ATPase) multi-subunit complex is a key regulator of intracellular pH homeostasis. KM91104 is a cell-permeable inhibitor of v-ATPase. In hHSC (human hepatic stellate cells), KM91104 (1 nM and 10 nM; 48 hr) reduced v-ATPase expression and activity. Serum starved hHSC displayed a higher neutral red uptake compared to cells in complete medium reflecting a more acidic pH inside the lysosomes and endosomes. KM91104 (10 nM) in serum free condition reversed this effect as demonstrated by a decreased uptake of neutral red when compared to the control cells. Likewise, treatment with 10 nM KM91104 was followed by a significant decrease in cytosolic pH. Specific inhibition of v-ATPase with KM91104 induced a down-regulation of the HSC fibrogenic gene profile, which coincided with increased lysosomal pH, decreased pHi, activation of AMPK, reduced proliferation, and lower metabolic activity[3].
作用机制 KM91104 specifically targets the interaction between v-ATPase subunit a3 and subunit B2[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.67mL

0.73mL

0.37mL

18.37mL

3.67mL

1.84mL

36.73mL

7.35mL

3.67mL

参考文献

[1]Marrone G, De Chiara F, Böttcher K, Levi A, Dhar D, Longato L, Mazza G, Zhang Z, Marrali M, Fernández-Iglesias A, Hall A, Luong TV, Viollet B, Pinzani M, Rombouts K. The adenosine monophosphate-activated protein kinase-vacuolar adenosine triphosphatase-pH axis: A key regulator of the profibrogenic phenotype of human hepatic stellate cells. Hepatology. 2018 Sep;68(3):1140-1153. doi: 10.1002/hep.30029. Epub 2018 Jul 16. PMID: 29663481.

[2]Kartner N, Yao Y, Li K, Crasto GJ, Datti A, Manolson MF. Inhibition of osteoclast bone resorption by disrupting vacuolar H+-ATPase a3-B2 subunit interaction. J Biol Chem. 2010 Nov 26;285(48):37476-90. doi: 10.1074/jbc.M110.123281. Epub 2010 Sep 13. PMID: 20837476; PMCID: PMC2988353.

[3]Marrone G, et al. The adenosine monophosphate-activated protein kinase-vacuolar adenosine triphosphatase-pH axis: A key regulator of the profibrogenic phenotype of human hepatic stellate cells. Hepatology. 2018 Sep;68(3):1140-1153