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MCE 國際站:Dorsomorphin dihydrochloride
品牌:MedChemExpress (MCE)
貨號:HY-13418
CAS:1219168-18-9
Synonyms:Compound C dihydrochloride; BML-275 dihydrochloride
純度:0.9973
存儲(chǔ)條件:4°C,密封保存,遠(yuǎn)離潮濕 *溶劑中:-80°C, 1年; -20°C, 6個(gè)月(密封保存,遠(yuǎn)離潮濕)
運(yùn)輸條件:美國大陸的室溫;其他地方可能有所不同。
產(chǎn)品活性:Dorsomorphin (Compound C) dihydrochloride 是一種有效,選擇性和 ATP 競爭性的 AMPK 抑制劑,Ki 為 109 nM。Dorsomorphin dihydrochloride 通過靶向抑制 I 型受體 ALK2,ALK3 和 ALK6 來抑制 BMP 途徑。Dorsomorphin dihydrochloride 還能夠逆轉(zhuǎn) Urolithin A (HY-100599) 導(dǎo)致的自噬 (autophagy) 激活和抗炎作用。
體外:Dorsomorphin (compound C; 0-10 μM; 18 h) dihydrochloride 以劑量依賴性方式抑制人纖維肉瘤 HT1080 細(xì)胞中 2DG 誘導(dǎo)的 GRP78 啟動(dòng)子活性,但對衣霉素 (HY-A0098) 誘導(dǎo)的 GRP78 啟動(dòng)子活性幾乎沒有影響。Dorsomorphin dihydrochloride 還抑制葡萄糖戒斷誘導(dǎo)的 GRP78 啟動(dòng)子活性。Dorsomorphin dihydrochloride 對 2DG 誘導(dǎo)的 PERK 激活沒有影響,并降低 HT1080 細(xì)胞中基礎(chǔ)和 2DG 誘導(dǎo)的 AMPK 磷酸化水平[2]。 MCE尚未獨(dú)立證實(shí)這些方法的準(zhǔn)確性。僅供參考。
體內(nèi):Dorsomorphin (化合物 C; 10 mg/kg; 靜脈注射一次) dihydrochloride 處理導(dǎo)致總血清鐵濃度增加 60%,降低成年小鼠鐵調(diào)素表達(dá)的基礎(chǔ)水平并增加血清鐵濃度[3]。 Dorsomorphin (0.2 mg/kg,靜脈注射,LPS 注射前 30 分鐘) dihydrochloride 降低注射 LPS 的大鼠主動(dòng)脈中的 ICAM-1 和 VCAM-1 表達(dá)[4]。 Dorsomorphin (25 mg/kg;腹腔注射,在雄性 BALB/c 小鼠中) dihydrochloride 在注射脂多糖 (LPS) 之前進(jìn)行處理,與僅接受 LPS 處理的動(dòng)物相比,顯著降低了致死率[5]。 MCE尚未獨(dú)立證實(shí)這些方法的準(zhǔn)確性。僅供參考。
IC50 & Target:AMPK 109 nM (Ki) ACVR1 BMPR1A ALK6 Autophagy
熱銷產(chǎn)品:Suc-Ala-Leu-Pro-Phe-pNA | 187-1, N-WASP inhibitor | Caftaric acid | Clonidine (hydrochloride) | Lenvatinib-d4 | N-3-Oxo-tetradecanoyl-L-homoserine lactone | BTX161 | Pelargonidin (chloride) | 2-Iminothiolane (hydrochloride) | Adenosine dialdehyde
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides
參考文獻(xiàn):
[1]. Zhou G, et al. Role of AMP-activated protein kinase in mechanism of action. J Clin Invest. 2001 Oct;108(8):1167-74.
[2]. Saito S, et al. Compound C prevents the unfolded protein response during glucose deprivation through a mechanism independent of AMPK and BMP signaling. PLoS One. 2012;7(9):e45845.
[3]. Yu PB, et al. Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism. Nat Chem Biol. 2008 Jan;4(1):33-41.
[4]. Kim YM, et al. Compound C independent of AMPK inhibits ICAM-1 and VCAM-1 expression in inflammatory stimulants-activated endothelial cells in vitro and in vivo. Atherosclerosis. 2011 Nov;219(1):57-64.
[5]. Guo Y, et al. AMPK inhibition blocks ROS-NFκB signaling and attenuates endotoxemia-induced liver injury. PLoS One. 2014 Jan 24;9(1):e86881.
[6]. Zhang Y, et al. Urolithin A suppresses glucolipotoxicity-induced ER stress and TXNIP/NLRP3/IL-1β inflammation signal in pancreatic β cells by regulating AMPK and autophagy. Phytomedicine. 2021 Dec;93:153741.
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