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Dorsomorphin dihydrochloride

CAS号

1219168-18-9

分子式

C24H25N5O·2HCl

主要靶点

AMPK|Autophagy|TGF-beta/Smad

仅限科研使用

Cat No : CM00933

Print datasheet

Synonyms

Autophagy|ATP-competitive|BML275|BML-275|BML-275 2HCl|BML275 Dihydrochloride|BML-275 Dihydrochloride|BML-275 dihydrochloride|BMP|BML 275|BML 275 Dihydrochloride|Compound C|Compound C Dihydrochloride|Compound C dihydrochloride|Compound C 2HCl|AMP-activated protein kinase|AMPK|6-[4-[2-(1-哌啶基)乙氧基]苯基]-3-(4-吡啶基)吡唑并[1,5-A]嘧啶|Dorsomorphin|Dorsomorphin (Compound C)|Dorsomorphin (Compound C) 2HCl|Dorsomorphin Dihydrochloride|Dorsomorphin dihydrochloride|inhibit|TGF-β/Smad|TGF-β Receptor|TGFβ|TGFbeta/Smad|TGF-beta|TGFbeta|TGF-b/Smad|TGFb|Smad|type|Transforming growth factor beta receptors|Inhibitor|pathway|receptors

验证数据展示

  • CAS No.: 1219168-18-9

    Dorsomorphin dihydrochloride
    CAS#: 1219168-18-9

产品信息

CAS号 1219168-18-9
分子式 C24H25N5O·2HCl
主要靶点 AMPK|Autophagy|TGF-beta/Smad
主要通路 表观遗传|PI3K/Akt/mTOR 信号通路|自噬|干细胞
分子量 472.41
纯度 99.89%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 Autophagy|ATP-competitive|BML275|BML-275|BML-275 2HCl|BML275 Dihydrochloride|BML-275 Dihydrochloride|BML-275 dihydrochloride|BMP|BML 275|BML 275 Dihydrochloride|Compound C|Compound C Dihydrochloride|Compound C dihydrochloride|Compound C 2HCl|AMP-activated protein kinase|AMPK|6-[4-[2-(1-哌啶基)乙氧基]苯基]-3-(4-吡啶基)吡唑并[1,5-A]嘧啶|Dorsomorphin|Dorsomorphin (Compound C)|Dorsomorphin (Compound C) 2HCl|Dorsomorphin Dihydrochloride|Dorsomorphin dihydrochloride|inhibit|TGF-β/Smad|TGF-β Receptor|TGFβ|TGFbeta/Smad|TGF-beta|TGFbeta|TGF-b/Smad|TGFb|Smad|type|Transforming growth factor beta receptors|Inhibitor|pathway|receptors

靶点活性

AMPK:109 nM (cell free)

体内活性

方法：为检测体内抗肿瘤活性，将 Dorsomorphin dihydrochloride (10 mg/kg) 腹腔注射给携带人类肿瘤 S1T 的 NOD/SCID 小鼠，每天一次，持续二十八天。 结果：Dorsomorphin 抑制了 NOD/SCID 小鼠中人 ATL 肿瘤异种移植物的生长。[2] 方法：为检测体内对 SMAD 活性的影响，将 Dorsomorphin dihydrochloride (10 mg/kg) 单次腹腔注射给 iron-dextran 处理的 C57BL/6 小鼠。 结果：Dorsomorphin 消除了 iron-dextran 引起的铁介导的肝脏 SMAD1/5/8 磷酸化的增加。[3]

体外活性

方法：人肿瘤细胞 HeLa 和 HCT116 用 Dorsomorphin dihydrochloride (1.25-80 μM) 处理 24 h，使用 CCK-8 assay 检测细胞活力。 结果：Dorsomorphin 抑制 HeLa 和 HCT116 细胞的活力，IC50 值分别为 10.71 μM 和 11.34 μM。[1] 方法：ATL 患者来源的 PBMCs 细胞用 Dorsomorphin dihydrochloride (5-25 μM) 处理 24 h，使用 Flow Cytometry 检测细胞凋亡情况。 结果：Dorsomorphin 以剂量依赖的方式增加了急性和慢性型 ATL 患者 PBMC 中早期凋亡细胞的频率。[2]

溶解度

DMSO:6.88 mg/mL (14.55 mM);H2O:47.2 mg/mL (99.91 mM)

细胞实验

C2C12 cells were seeded into 96-well plates at 2,000 cells per well in DMEM supplemented with 2% FBS. Wells were treated in quadruplicate with BMP ligands and dorsomorphin or vehicle. Cells were harvested after 5 d in culture with 50 μl Tris-buffered saline, 1% Triton X-100. Lysates were added to p-nitro-phenylphosphate reagent in 96-well plates for 1 h, and alkaline phosphatase activity expressed as absorbance at 405 nM. Cell viability and quantity were measured by Cell-titer Glo and binding of nuclear dye CyQuant, respectively, using replicate wells treated identically to those used for alkaline phosphatase measurements [3].

动物实验

12-week-old C57BL/6 mice raised on a standard diet were injected via the tail vein with 0.2 g kg?1 of dextran (average MW = 5,000) or 0.2 g kg?1 of iron-dextran USP. Dextran was injected with vehicle only, whereas iron-dextran was injected with either vehicle or dorsomorphin (10 mg/kg). 1 h after injection, mice were killed and liver segments were collected in 500 μl of SDS-lysis buffer and mechanically homogenized. 20 μl of liver extracts were resolved by SDS-PAGE and immunoblotted. Total RNA was harvested using Trizol from mechanically homogenized mouse livers (6 h after injection with a single intraperitoneal dose of dorsomorphin (10 mg/kg) or DMSO) [3].

参考文献

1.Li N, et al. Dorsomorphin induces cancer cell apoptosis and sensitizes cancer cells to HSP90 and proteasome inhibitors by reducing nuclear heat shock factor 1 levels. Cancer Biol Med. 2019 May;16(2):220-233.
2.Aikawa A, et al. Cell death induced by dorsomorphin in adult T-cell leukemia/lymphoma is AMPK-independent. FEBS J. 2020 Sep;287(18):4005-4015.
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.Fan C, Feng J, Tang C, et al. Melatonin suppresses ER stress-dependent proapoptotic effects via AMPK in bone mesenchymal stem cells during mitochondrial oxidative damage[J]. Stem Cell Research & Therapy. 2020, 11(1): 1-22.

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