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LDN193189

促销

ALK 抑制剂

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产品目录号: A11205

库存状态:中国现货中国现货

产品名 目录号 价格 数量
LDN193189 2mg A11205-2
¥ 400.00
LDN193189 5mg A11205-5
¥ 700.00
LDN193189 25mg A11205-25
¥ 1,400.00
LDN193189 50mg A11205-50
¥ 2,400.00

产品仅用于研究,不针对患者销售,望谅解.

产品简介

LDN193189 is a highly potent small molecule BMP inhibitor that inhibits BMP type I receptors ALK2 (IC50: 5 nM), ALK3 (IC50: 30 nM) and ALK6 (TGFβ1/BMP signaling) and subsequent SMAD phosphorylation.

LDN193189

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顾客使用 Adooq 产品发表的高质量科研文献
Adooq 顾客使用 LDN193189 发表的文献 (2)
  • Shizu Aikawa, .et al. Autotaxin每lysophosphatidic acid每LPA 3 signaling at the embryo坼epithelial boundary controls decidualization pathways, EMBO J, 2017, Jul 14; 36(14): 2146每2160 PMID: 28588064
  • HIROTAKA SOMEYA, .et al. Thymosin beta 4 is associated with RUNX2 expression through the Smad and Akt signaling pathways in mouse dental epithelial cells, Int J Mol Med, 2015, May; 35(5): 1169每1178 PMID: 25739055

Chemical Information

目录号 A11205
Mechanism of action Inhibitor
分子量 406.48
化学分子式 C25H22N6
Solubility DMSO
纯度 >98%
储存方式 at -20°C 2 years
CAS No. 1062368-24-4
Synonyms LDN-193189
SMILES code C1CN(CCN1)C2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=CC=NC6=CC=CC=C56)N=C3
化学名称 4-[6-(4-Piperazin-1-yl-phenyl)-pyrazolo[1,5-a]pyrimidin-3-yl]-quinoline hydrochloride

生物活性

Description
LDN193189 is a highly potent small molecule BMP inhibitor that inhibits BMP type I receptors ALK2 (IC50: 5 nM), ALK3 (IC50: 30 nM) and ALK6 (TGFβ1/BMP signaling) and subsequent SMAD phosphorylation.
Targets
ALK2 (C2C12 cells) ALK3 (C2C12 cells)
5 nM30 nM

溶解性

Solubility (25°C) * In vitro DMSO 0.01 mg/mL (<1 mM)
Water 0.01 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo Saline 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

制备储备液

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.1 mM 24.6 mL 123.01 mL 246.01mL
0.5 mM 4.92 mL 24.6 mL 49.2 mL
1 mM 2.46 mL 12.3 mL 24.6 mL
5 mM 0.49 mL 2.46 mL 4.92 mL

*The above data is based on the productmolecular weight 406.48. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

LDN-193189 is a cell permeable small molecule inhibitor of bone morphogenetic protein (BMP) type I receptors ALK2 and ALK3 (IC50 = 5 nM and 30 nM respectively). LDN-193189 was derived from structure-activity relationship studies of Dorsomorphin and functions primarily through prevention of Smad1, Smad5, and Smad8 phosphorylation. LDN-193189 only weakly inhibits ALK4, ALK5, and ALK7. BMP signaling coordinates developmental patterning and has essential physiological roles in mature organisms. LDN-193189  has been used to reduce ectopic ossification in a mouse model of fibrodysplasia ossificans progressiva

Reference:

 1.  Cuny GD, et al.  Structure-activity relationship study of bone morphogenetic protein (BMP) signaling inhibitors. (2008), Bioorg Med Chem Lett. 18(15):4388-92.

2.  Paul B Yu, et al. BMP type I receptor inhibition reduces heterotopic ossification. (2008), Nature Med. 14: 1363-1369.

3.  Yu PB, et al.  Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism. (2008), Nature Chem Biol. 4: 33-41.

4.  Chambers SM, et al. Highly efficient neural conversion of human ES and iPS cells by dual inhibition of SMAD signaling. (2009), Nature Biotechnology 27, 275-280.

5.  Boergermann JH, et al. Dorsomorphin and LDN-193189 inhibit BMP-mediated Smad, p38 and Akt signalling in C2C12 cells. (2010), Int J Biochem Cell Biol. 42(11):1802-7.

6.  Lee YC, et al. BMP4 promotes prostate tumor growth in bone through osteogenesis.  (2011), Cancer Res 71:5194-5203.

7.  Najm FJ, et al. Rapid and robust generation of functional oligodendrocyte progenitor cells from epiblast stem cells. (2011) Nature Methods 8, 957–962

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