2. Stem Cell/Wnt TGF-beta/Smad
  3. Organoid TGF-β Receptor
  4. LDN193189 Tetrahydrochloride

LDN193189 Tetrahydrochloride  (Synonyms: DM-3189 Tetrahydrochloride)

目录号: HY-12071A 纯度: 99.86%
COA 产品使用指南

摩尔计算器

LDN193189 Tetrahydrochloride 是一种选择性的 BMP I 型受体抑制剂，抑制 ALK2 和 ALK3 的 IC50 分别为 5 nM 和 30 nM。对 ALK4，ALK5 和 ALK7 的作用效果弱 (IC50≥500 nM)。

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LDN193189 Tetrahydrochloride Chemical Structure

LDN193189 Tetrahydrochloride Chemical Structure

CAS No. : 2310134-98-4

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规格 价格 是否有货 数量
10 mM * 1 mL in Water ￥1154
In-stock
2 mg ￥700
In-stock
5 mg ￥950
In-stock
10 mg ￥1600
In-stock
50 mg ￥4800
In-stock
100 mg   询价  
200 mg   询价  

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Customer Review

Other Forms of LDN193189 Tetrahydrochloride:

LDN193189 Tetrahydrochloride 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 58 篇科研文献

IHC
WB

    LDN193189 Tetrahydrochloride purchased from MCE. Usage Cited in: Oxid Med Cell Longev. 2020 Jun 8;2020:4175613.  [Abstract]

    Western blot and grey analysis of CYP11a1, CYP19a1, BCL2, CALR, CHOP, caspase3, caspase12, PERK, and GRP78. qRT-PCR analyzed ATF4, caspase3, and GRP78 mRNAs. The relieving function of BMP4 on ER stress is diminished after blockade of BMP receptor I (BMPRI) with DM-3189.

    LDN193189 Tetrahydrochloride purchased from MCE. Usage Cited in: Cardiovasc Toxicol. 2019 Jun;19(3):264-275.  [Abstract]

    H9c2 cells are treated as following: control, DOX, DOX + rhBMP (Bmpr1a agonist) and DOX + LDN193189 (Bmpr1a inhibitor). Cells with red fluorescence indicate favorable MMP while green fluorescence indicates damage.

    查看 TGF-β Receptor 亚型特异性产品:

    查看所有亚型
    ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    LDN193189 Tetrahydrochloride is a selective BMP type I receptor inhibitor, which efficiently inhibits ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), with weaker effects on ALK4, ALK5 and ALK7 (IC50≥500 nM)[1].

    IC50 & Target[1]

    ACVR1

    5 nM (IC50)

    BMPR1A

    30 nM (IC50)

    体外研究
    (In Vitro)

    LDN193189 有效抑制 BMP4 介导的 Smad1、Smad5 和 Smad8 的激活 (IC50=5 nM)，同时对 BMP 信号的选择性是 TGF-β 信号的 200 倍 (IC50, 对 TGF-β≥1000 nM)[1]。
    LDN193189 有效抑制 BMP-I 型受体 ALK2 和 ALK3 (IC50=5 nM, 30 nM) 以及 TGF-β-I 型受体 ALK4、ALK5 和 ALK7 (IC50≥500 nM) 的转录活性，与母体化合物相比，增加了 BMP 信号通路对 AMP 活化的蛋白激酶、PDGFR 和 MAPK 信号通路的选择性[1]。
    LDN193189 可阻断组成型活性 ALK2R206H 或 ALK2Q207D突变蛋白诱导的转录活性[1]。
    LDN193189 抑制 BMP4 诱导 C2C12 细胞碱性磷酸酶活性，即使在 BMP 刺激后 12 小时给药[1]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    LDN193189 Tetrahydrochloride 相关抗体:
    体内研究
    (In Vivo)

    LDN193189 (Tetrahydrochloride) (腹腔注射；3 mg/kg；每天 2 次) 在前 5 周后，对照组小鼠和 LDN193189 处理小鼠的生长速率无显著差异，但在处理后 6 周和 7 周后发现生长速率差异[2]。
    LDN193189 (皮下注射；5 天) 在处理 6 周和 7 周后肿瘤大小差异显著，在第 7 周研究结束时肿瘤重量也差异显著[2]。
    LDN193189 降低异位骨体积和骨密度[2]。
    LDN193189 与 UK-92480 共孵育完全抑制骨形态发生蛋白 (BMPR2) 和 Cx40 的抗增殖和上调表达[3]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    552.33

    Formula

    C25H26Cl4N6
    CAS 号
    性状

    固体

    颜色

    Light yellow to yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

    溶解性数据
    细胞实验： 

    H2O 中的溶解度 : 33.33 mg/mL (60.34 mM; 超声助溶)

    DMSO 中的溶解度 : 4.17 mg/mL (7.55 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.8105 mL 9.0526 mL 18.1051 mL
    5 mM 0.3621 mL 1.8105 mL 3.6210 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    该产品水溶性佳，请具体参考实测 水 / PBS / Saline 中的溶解度数据。
    您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。
    纯度 & 产品资料

    纯度: 99.86%

    COA (203 KB) LCMS (93 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [1]

    Mouse PASMCs grown are transiently transfected to 50% confluence in six-well plates with 0.3 μg Id1promoter luciferase reporter construct (BRE-Luc) in combination with 0.6 μg of plasmid expressing constitutively active forms of BMP type I receptors (caALK2, caALK3 or caALK6). For both reporter plasmids, 0.2 μg of pRL-TKRenilla luciferase are used to control for transfection efficiency. PASMCs are incubated with LDN193189 (2 nM-32 μM) or vehicle starting 1 h after transfection. Cell extracts are harvested and quantified relative promoter activity by the ratio of firefly to Renilla luciferase activity with the dual luciferase assay kit[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2][3]

    Mice[2]
    In the first experiment, SCID mice are implanted with MDA-PCa-118b tumors. After 7 days when tumors reached measurable sizes, mice are injected with LDN193189 (3 mg/kg) or with vehicle intraperitoneally twice a day. Tumor sizes and body weights are measured weekly. Mice are injected with calcein at three days and one day prior to sacrifice. Blood is collected and tumors are weighed. A portion of the tumors are fixed in formaldehyde for micro-computed tomography (microCT), using EVS CT, or further decalcified for bone histomorphometric analysis, using OsteoMeasure Analysis System, or flash frozen for RNA preparation. Osteocalcin in the mouse serum is determined by ELISA. In the second experiment, PCa-118b tumors are first digested with Accumax, and the isolated cells are plated overnight, resuspended in Matrigel in 1:1 ratio, and injected into SCID mice (1×106 cells/mouse) subcutaneously. Mice are treated with LDN193189 five days post-injection.
    Rats[3]
    Male Sprague-Dawley (SD) rats, 8 weeks of age, weighing 200-220 g, are purchased from Nanjing Medical University animal center. Rats are randomly assigned to one of seven experiment groups (n=6 per group). Rats are housed with free access to food and water under a natural 12/12 h day/night cycle. The Monocrotaline is administered (60 mg/kg) to rats by subcutaneous injection into the back region. The animal’s lungs are harvested at 28th day of the study after hemodynamic assessment. The UK-92480 group received daily intragastric administration of UK-92480 after the administration of MCT (60 mg/kg). The LDN193189 group received daily intragastric administration of UK-92480 (50 mg/kg) and intraperitoneal injection of LDN193189 (10 mg/kg). In other groups, the same volume saline is given.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    参考文献

    LDN193189 Tetrahydrochloride 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO / H2O 1 mM 1.8105 mL 9.0526 mL 18.1051 mL 45.2628 mL
    5 mM 0.3621 mL 1.8105 mL 3.6210 mL 9.0526 mL
    H2O 10 mM 0.1811 mL 0.9053 mL 1.8105 mL 4.5263 mL
    15 mM 0.1207 mL 0.6035 mL 1.2070 mL 3.0175 mL
    20 mM 0.0905 mL 0.4526 mL 0.9053 mL 2.2631 mL
    25 mM 0.0724 mL 0.3621 mL 0.7242 mL 1.8105 mL
    30 mM 0.0604 mL 0.3018 mL 0.6035 mL 1.5088 mL
    40 mM 0.0453 mL 0.2263 mL 0.4526 mL 1.1316 mL
    50 mM 0.0362 mL 0.1811 mL 0.3621 mL 0.9053 mL
    60 mM 0.0302 mL 0.1509 mL 0.3018 mL 0.7544 mL

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    LDN193189 Tetrahydrochloride2310134-98-4DM-3189 TetrahydrochlorideOrganoidTGF-β ReceptorTransforming growth factor beta receptorsInhibitorinhibitorinhibit

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