2. TGF-beta/Smad
  3. TGF-β Receptor
  4. LDN-214117

LDN-214117 是一种 ALK2 抑制剂，具有口服活性，耐受性好，脑穿透性好。LDN-214117 对 ALK2 具有较高的选择性和较低的细胞毒性，其 IC50 值为 24 nM。LDN-214117 也是一种特异性的骨形态发生蛋白 (BMPs) 信号抑制剂，对 BMP6 具有相对选择的抑制作用，其 IC50 值为 100 nM。LDN-214117 可用于进行性骨化性纤维发育不良 (FOP) 和弥漫性内源性桥脑胶质瘤 (DIPG) 的研究。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

LDN-214117 Chemical Structure

LDN-214117 Chemical Structure

CAS No. : 1627503-67-6

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥660
In-stock
5 mg ￥600
In-stock
10 mg ￥1100
In-stock
25 mg ￥2200
In-stock
50 mg ￥3800
In-stock
100 mg ￥5900
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

LDN-214117 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

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

  • 纯度 & 产品资料

  • 参考文献

生物活性

LDN-214117 is an orally active ALK2 inhibitor with well-tolerated and good brain penetration. LDN-214117 has a high selectivity and low cytotoxicity for ALK2 with an IC50 value of 24 nM. LDN-214117 also is a specific bone morphogenetic proteins (BMPs) signaling inhibitor and has relatively selective inhibition for BMP6 with an IC50 value of 100 nM. LDN-214117 can be used for the research of fibrodysplasia ossificans progressiva (FOP), diffuse intrinsic pontine glioma (DIPG) [1][2]

IC50 & Target

IC50: 24 nM (ALK2); 27 nM (ALK1); 1,171 nM (ALK3); 3,000 nM (ALK5); 1,022 nM (BMP6); 27 nM (BMP2); 960 nM (BMP4); 16,000 nM (TGF-β1)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
C2C12 IC50
100 nM
Compound: 10, LDN-214117
Inhibition of BMP6-induced BMP receptor type 1 ALK2 in mouse C2C12 cells after 30 mins by luciferase reporter gene assay
Inhibition of BMP6-induced BMP receptor type 1 ALK2 in mouse C2C12 cells after 30 mins by luciferase reporter gene assay
[PMID: 25101911]
C2C12 IC50
1022 nM
Compound: 10, LDN-214117
Inhibition of BMP4-induced BMP receptor in mouse C2C12 cells after 30 mins by luciferase reporter gene assay
Inhibition of BMP4-induced BMP receptor in mouse C2C12 cells after 30 mins by luciferase reporter gene assay
[PMID: 25101911]
C2C12 IC50
960 nM
Compound: 10, LDN-214117
Inhibition of BMP2-induced BMP receptor type 1 ALK2 in mouse C2C12 cells after 30 mins by luciferase reporter gene assay
Inhibition of BMP2-induced BMP receptor type 1 ALK2 in mouse C2C12 cells after 30 mins by luciferase reporter gene assay
[PMID: 25101911]
HEK-293T IC50
1171 nM
Compound: 10, LDN-214117
Inhibition of ALK3 (unknown origin) expressed in HEK293T cells after 30 mins by luciferase reporter gene assay
Inhibition of ALK3 (unknown origin) expressed in HEK293T cells after 30 mins by luciferase reporter gene assay
[PMID: 25101911]
HEK-293T IC50
16000 nM
Compound: 10, LDN-214117
Inhibition of TGFbeta1-induced TGFbeta type 1 ALK5 in HEK293T cells after 30 mins by luciferase reporter gene assay
Inhibition of TGFbeta1-induced TGFbeta type 1 ALK5 in HEK293T cells after 30 mins by luciferase reporter gene assay
[PMID: 25101911]
HEK-293T IC50
27 nM
Compound: 10, LDN-214117
Inhibition of ALK1 (unknown origin) expressed in HEK293T cells after 30 mins by luciferase reporter gene assay
Inhibition of ALK1 (unknown origin) expressed in HEK293T cells after 30 mins by luciferase reporter gene assay
[PMID: 25101911]
HEK-293T IC50
27 nM
Compound: 10, LDN-214117
Inhibition of ALK2 (unknown origin) expressed in HEK293T cells after 30 mins by luciferase reporter gene assay
Inhibition of ALK2 (unknown origin) expressed in HEK293T cells after 30 mins by luciferase reporter gene assay
[PMID: 25101911]
体外研究
(In Vitro)

LDN-214117 has high inhibition and selectivity for ALK2 kinase proteins with an IC50 value of 24 nM[1].
LDN-214117 has kinase activity for ALK1, ALK3 and ALK5 with IC50 values of 27 nM, 1,171 nM and 3,000 nM, respectively[1].
LDN-214117 exhibits relatively selective inhibition for BMP6, BMP2 and BMP4 with IC50 values of 100 nM, 1,022 nM and 960 nM, respectively[1].
LDN-214117 has inhibition of TGF-β1-induced transcriptional activity with an IC50 values of 16,000 nM[1].
LDN-214117 (5 μM, 30 min, 3 h and 24 h) has time-dependent effect activity on gene regulation level and/ or a BMP signaling pathway other than SMAD-dependent that is responsible for ID1 targeting[2].
LDN-214117 (5 μM, 24-120 h) reduces viability, proliferation and causes apoptosis of lung carcinoma cells LCLC-103H[2].
LDN-214117 (5 μM, 0-48 h) suppresses wound healing and chemotactic potential of LCLC-103H cells[2].
LDN-214117 (5 μM, 48 h) hinders growth of multicellular LCLC-103H spheroids[2].

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

LDN-214117 相关抗体:

Cell Viability Assay[2]

Cell Line: LCLC-103H cells
Concentration: 5 μM
Incubation Time: 24 h, 48 h, 72 h and 96 h
Result: Decreased markedly with time, counting approximately 60% of the vehicle control level at the 96-h measurement point.

Western Blot Analysis[2]

Cell Line: LCLC-103H cells
Concentration: 5 μM
Incubation Time: 30 min, 3 h and 24 h
Result: Diminished the increase of ID1 protein.

Apoptosis Analysis[2]

Cell Line: LCLC-103H cells
Concentration: 5 μM
Incubation Time: 24 h, 48 h, 72 h and 96 h
Result: Induced considerable death of LCLC-103H cells.

RT-PCR[2]

Cell Line: LCLC-103H cells
Concentration: 5 μM
Incubation Time: 24 h, 48 h and 72 h
Result: Induced distinct gene expression patterns for the two EMTTFs.

Cell Migration Assay [2]

Cell Line: LCLC-103H cells
Concentration: 5 μM
Incubation Time: 0 h, 24 h and 48 h
Result: Significantly hindered the migration of LCLC-103H cells into the wound area by Inhibiting of BMP signaling.
体内研究
(In Vivo)

LDN-214117 (p.o., 25 mg/kg, daily, for 14 days) has well-tolerated in mice[3].

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

Animal Model: NOD.SCID mice[3]
Dosage: 25 mg/kg
Administration: p.o., daily, for 14 days
Result: Showed good-tolerated in mice.
分子量

419.52

Formula

C25H29N3O3
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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 20 mg/mL (47.67 mM; 超声助溶 (<60°C); 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 2.3837 mL 11.9184 mL 23.8368 mL
5 mM 0.4767 mL 2.3837 mL 4.7674 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 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

动物实验：

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2 mg/mL (4.77 mM); 澄清溶液

    此方案可获得 ≥ 2 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2 mg/mL (4.77 mM); 澄清溶液

    此方案可获得 ≥ 2 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

    2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
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
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.92%

COA (191 KB) LCMS (94 KB)

产品使用指南 (1538 KB)
参考文献

LDN-214117 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3837 mL 11.9184 mL 23.8368 mL 59.5919 mL
5 mM 0.4767 mL 2.3837 mL 4.7674 mL 11.9184 mL
10 mM 0.2384 mL 1.1918 mL 2.3837 mL 5.9592 mL
15 mM 0.1589 mL 0.7946 mL 1.5891 mL 3.9728 mL
20 mM 0.1192 mL 0.5959 mL 1.1918 mL 2.9796 mL
25 mM 0.0953 mL 0.4767 mL 0.9535 mL 2.3837 mL
30 mM 0.0795 mL 0.3973 mL 0.7946 mL 1.9864 mL
40 mM 0.0596 mL 0.2980 mL 0.5959 mL 1.4898 mL
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:

LDN-2141171627503-67-6LDN214117LDN 214117TGF-β ReceptorTransforming growth factor beta receptorsoralbone morphogenetic proteins (BMPs)type I receptor kinasesALK1ALK2ALK3ALK5BMP6BMP2BMP4transforming growth factor-beta (TGF-β)fibrodysplasia ossificans progressiva (FOP)diffuse intrinsic pontine glioma (DIPG)Inhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
LDN-214117
目录号：
HY-16712
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z