2. Protein Tyrosine Kinase/RTK TGF-beta/Smad Stem Cell/Wnt
  3. Anaplastic lymphoma kinase (ALK) TGF-beta/Smad
  4. M4K2234

M4K2234 是一种化学探针，是一种口服活性的高选择性 ALK1 和 ALK2 抑制剂，IC50 值分别为 7 nM 和 14 nM。M4K2234 通过抑制 SMAD1/5/8 的磷酸化特异性阻断 BMP 信号传导。M4K2234 抑制 BMP7 刺激的报告基因活性 (IC50 = 16 nM)。M4K2234 可用于研究 ALK1/2 介导的生物学过程及相关疾病，如弥漫性中线胶质瘤 (DMG) 和进行性骨化纤维发育不良 (FOP)。

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M4K2234

M4K2234 Chemical Structure

CAS No. : 2421141-51-5

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1526
In-stock
5 mg ￥1500
In-stock
10 mg ￥2400
In-stock
25 mg ￥4800
In-stock
50 mg 现货 询价
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Customer Review

M4K2234 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

M4K2234, a chemical probe, is an orally active, highly selective inhibitor of ALK1 and ALK2 with IC50 values of 7 nM and 14 nM, respectively. M4K2234 specifically blocks BMP signaling by inhibiting the phosphorylation of SMAD1/5/8. M4K2234 inhibits BMP7-stimulated reporter gene activity (IC50 = 16 nM). M4K2234 can be used for the investigation of ALK1/2-mediated biological processes and related diseases such as diffuse midline glioma (DMG) and fibrodysplasia ossificans progressiva (FOP)[1].

IC50 & Target[1]

ALK1

7 nM (IC50)

ALK2

14 nM (IC50)

ALK3

168 nM (IC50)

ALK4

1660 nM (IC50)

ALK5

1950 nM (IC50)

ALK6

88 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
> 30 μM
Compound: 26b
Inhibition of human ERG expressed in HEK293 cells measured after 5 mins by whole cell patch clamp method
Inhibition of human ERG expressed in HEK293 cells measured after 5 mins by whole cell patch clamp method
[PMID: 32369358]
HEK293 IC50
3900 nM
Compound: 26b
Inhibition of ALK5 (unknown origin) expressed in HEK293 cells transfected with CAGA-luciferase and Renilla luciferase reporter measured after 24 hrs by dual luciferase reporter assay
Inhibition of ALK5 (unknown origin) expressed in HEK293 cells transfected with CAGA-luciferase and Renilla luciferase reporter measured after 24 hrs by dual luciferase reporter assay
[PMID: 32369358]
HEK293 IC50
52 nM
Compound: 26b
Inhibition of C-terminal nanoluciferase-fused ALK2 (unknown origin) expressed in HEK293 cells incubated for 2 hrs followed by NanoBRET NanoGlo Substrate addition by NanoBRET assay
Inhibition of C-terminal nanoluciferase-fused ALK2 (unknown origin) expressed in HEK293 cells incubated for 2 hrs followed by NanoBRET NanoGlo Substrate addition by NanoBRET assay
[PMID: 32369358]
体外研究
(In Vitro)

M4K2234 (16 nM) 在 HEK293 细胞中强效抑制 BMP7 刺激的报告基因活性，对激活素 A 和 TGF-β1 诱导的 CAGA 反应性报告基因的抑制作用分别弱 50 倍和 150 倍[1]。
M4K2234 (0.5-1 μM) 在 HEK293T 细胞中特异性抑制 BMP 家族配体诱导的 SMAD1/5/8 磷酸化，不影响激活素 A 或 TGF-β1 诱导的 SMAD2/3 磷酸化[1]。
M4K2234 在酶动力学实验中对 ALK1 和 ALK2 的 IC50 分别为 7 nM 和 14 nM，对 ALK6 的抑制较弱 (88 nM)，对 ALK4/5 的活性可忽略 (>10,000 nM)[1]。

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

M4K2234 相关抗体:
体内研究
(In Vivo)

1.19 Pharmacokinetic Properties of M4K2234 in Mice [1].

Mice
PO 3 mg/kg
Cmax(ng/mL) 1650
AUCinf(ng·h/mL) 4630
t1/2(h) 2.61

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

462.56

Formula

C27H31FN4O2
CAS 号
性状

固体

颜色

Light brown to brown

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 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (216.19 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 2.1619 mL 10.8094 mL 21.6188 mL
5 mM 0.4324 mL 2.1619 mL 4.3238 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, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 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
纯度 & 产品资料
参考文献

M4K2234 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, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1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 1 mM 2.1619 mL 10.8094 mL 21.6188 mL 54.0470 mL
5 mM 0.4324 mL 2.1619 mL 4.3238 mL 10.8094 mL
10 mM 0.2162 mL 1.0809 mL 2.1619 mL 5.4047 mL
15 mM 0.1441 mL 0.7206 mL 1.4413 mL 3.6031 mL
20 mM 0.1081 mL 0.5405 mL 1.0809 mL 2.7024 mL
25 mM 0.0865 mL 0.4324 mL 0.8648 mL 2.1619 mL
30 mM 0.0721 mL 0.3603 mL 0.7206 mL 1.8016 mL
40 mM 0.0540 mL 0.2702 mL 0.5405 mL 1.3512 mL
50 mM 0.0432 mL 0.2162 mL 0.4324 mL 1.0809 mL
60 mM 0.0360 mL 0.1802 mL 0.3603 mL 0.9008 mL
80 mM 0.0270 mL 0.1351 mL 0.2702 mL 0.6756 mL
100 mM 0.0216 mL 0.1081 mL 0.2162 mL 0.5405 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:

M4K22342421141-51-5Anaplastic lymphoma kinase (ALK)TGF-beta/SmadAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246Transforming growth factor betadiffuse midline gliomafibrodysplasia ossificans progressiveALK1/2Inhibitorinhibitorinhibit

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