Dorsomorphin dihydrochloride

SKU: orb1301035

描述

Dorsomorphin dihydrochloride (BML-275 2HCl) is a selective, ATP-competitive AMPK inhibitor (Ki=109 nM) that also blocks BMP receptors ALK2, ALK3, and ALK6. This compound induces autophagy and exhibits antitumor activity, making it a valuable tool for studying metabolic signaling, bone morphogenesis, and cancer biology in both cellular and animal models.

研究领域

Cell Biology, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

图片与验证

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关键属性

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CAS 号	1219168-18-9
MW	472.41
纯度	99.89% (May vary between batches)
分子式	C₂₄H₂₅N₅O·2HCl
SMILES	Cl.Cl.C(CN1CCCCC1)Oc1ccc(cc1)-c1cnc2c(cnn2c1)-c1ccncc1
靶点	AMPK,TGF-beta/Smad,Autophagy
溶解性	DMSO:7.4 mg/mL (15.66 mM);H2O:47.2 mg/mL (99.91 mM)

生物活性

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靶点 IC50	MCF-7 cells:4.9 μM (EC50)\|A2780 cells:0.9 μM (EC50)\|MP46 cells:10.13 µM\|AMPK:109 nM (Ki)\|OMM2.5 cells:31.45 µM\|92-1 cells:6.526 µM\|HeLa cells:10.71 μM\|Mel 270 cells:8.39 µM\|HCT116 cells:11.34 μM
体内	6 h after dorsomorphin was administered intravenously, hepatic hepcidin mRNA levels were reduced to one-third of that of vehicle-injected mice. Alterations in hepcidin levels affect serum iron concentrations within 24 h via the altered mobilization of intracellular iron by ferroportin33. Administration of dorsomorphin over 24 h led to a 60% increase in total serum iron concentrations .
体外	Dorsomorphin (compound C) is a potent reversible inhibitor that is competitive with ATP, with Ki = 109 ± 16 nM in the absence of AMP. Incubation of cultured hepatocytes with compound C inhibited ACC inactivation by either AICAR or metformin . Compound C suppressed 2-deoxy-D-glucose (2DG)-induced GRP78 promoter activity in a dose-dependent manner but had little effect on tunicamycin-induced GRP78 promoter activity. Compound C also suppressed GRP78 promoter activity induced by glucose withdrawal .
细胞研究	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 .
动物研究	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) .

储存与操作

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储存	-20°C
有效期	12 months from date of receipt.
免责声明	For research use only

别名

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inhibit, pathway, Inhibitor, Compound C Dihydrochloride, Compound C, Compound C 2HCl, Compound C dihydrochloride, Dorsomorphin, Dorsomorphin (Compound C), Dorsomorphin Dihydrochloride, Dorsomorphin dihydrochloride, Dorsomorphin (Compound C) 2HCl, AMPK, AMP-activated protein kinase, Autophagy, ATP-competitive, BML 275, BML 275 Dihydrochloride, BML275, BML-275, BML-275 2HCl, BML275 Dihydrochloride, BML-275 Dihydrochloride, BML-275 dihydrochloride, BMP, receptors, Smad, type, Transforming growth factor beta receptors, TGF-b/Smad, TGFb, TGFbeta/Smad, TGF-beta, TGFbeta, TGFβ, TGF-β Receptor, TGF-β/Smad

相似产品

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Dorsomorphin dihydrochloride [orb1226770]
纯度：
>98% (HPLC)
CAS 号：
1219168-18-9
MW:
472.4
分子式：
C₂₄H₂₇Cl₂N₅O
可选规格： 5 mg, 10 mg, 25 mg, 100 mg, 500 mg, 1 g, 50 mg

质量保证

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化合物标识

PubChem CID

49761481 ↗

关键属性

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暂无计算属性。

实验方案信息

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纯度：	>98% (HPLC)
CAS 号：	1219168-18-9
MW:	472.4
分子式：	C₂₄H₂₇Cl₂N₅O

Dorsomorphin dihydrochloride

描述

研究领域

图片与验证

关键属性

生物活性

储存与操作

别名

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