1. Apoptosis TGF-beta/Smad
  2. RIP kinase TGF-β Receptor
  3. OD36

OD36 是一种 RIPK2 抑制剂,IC50 为 5.3 nM。OD36 是一种大环抑制剂,可与 ALK2 激酶 ATP 口袋有效结合。OD36 靶向作用于 ALK2KD 为 37 nM。

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OD36 Chemical Structure

OD36 Chemical Structure

CAS No. : 1638644-62-8

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

OD36 is a RIPK2 inhibitor with an IC50 of 5.3 nM. OD36 is a macrocyclic inhibitor with potent binding to the ALK2 kinase ATP pocket. OD36 shows ALK2-directed activity with KDs of 37 nM[1][2].

IC50 & Target[1][2]

RIPK2

5.3 nM (IC50)

ACVR1

37 nM (Kd)

ACVR1

47 nM (IC50)

ALK2 R206H

22 nM (IC50)

体外研究
(In Vitro)

OD36 also inhibits ALK2 and ALK2 R206H with IC50s of 47 and 22 nM, respevtively[1].
OD36 shows activity against ALK1 with a KD of 90 nM[2].
OD36 potently antagonize mutant ALK2 signaling and osteogenic differentiation[2].
OD36 (0.1-1 μM; 24 h) efficiently inhibits BMP-6 (50 ng/mL)-induced p-Smad1/5 in KS483 cells[2].
Preincubation of fibrodysplasia ossificans progressiva (FOP) endothelial colony-forming cells (ECFCs) with OD36 (0.5 μM) completely prevents the activation of Smad1/5 and gene targets ID-1 and ID-3 in response to activin A[2].

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

Western Blot Analysis[2]

Cell Line: KS483 cells
Concentration: 0.1, 0.2, and 1 μM
Incubation Time:
Result: Inhibited BMP-6 induced p-Smad1/5.
体内研究
(In Vivo)

OD36 (6.25 mg/kg; i.p.; once) alleviates inflammation in an acute peritonitis mice model[3].

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

Animal Model: C57BL/6 mice, muramyl dipeptide (MDP)-induced model of peritonitis[3]
Dosage: 6.25 mg/kg
Administration: Intraperitoneal injection, 30 min prior to MDP
Result: Inhibited the recruitment of inflammatory cells to the peritoneum, specifically that of neutrophils, and, to a lesser extent, lymphocytes. Decreased RIPK2-specific genes as well as inflammatory cytokine and chemokine gene expression.
分子量

330.77

Formula

C16H15ClN4O2

CAS 号
性状

固体

颜色

White to off-white

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
In Vitro: 

DMSO 中的溶解度 : 33.33 mg/mL (100.76 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 3.0232 mL 15.1162 mL 30.2325 mL
5 mM 0.6046 mL 3.0232 mL 6.0465 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

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

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 3.0232 mL 15.1162 mL 30.2325 mL 75.5812 mL
5 mM 0.6046 mL 3.0232 mL 6.0465 mL 15.1162 mL
10 mM 0.3023 mL 1.5116 mL 3.0232 mL 7.5581 mL
15 mM 0.2015 mL 1.0077 mL 2.0155 mL 5.0387 mL
20 mM 0.1512 mL 0.7558 mL 1.5116 mL 3.7791 mL
25 mM 0.1209 mL 0.6046 mL 1.2093 mL 3.0232 mL
30 mM 0.1008 mL 0.5039 mL 1.0077 mL 2.5194 mL
40 mM 0.0756 mL 0.3779 mL 0.7558 mL 1.8895 mL
50 mM 0.0605 mL 0.3023 mL 0.6046 mL 1.5116 mL
60 mM 0.0504 mL 0.2519 mL 0.5039 mL 1.2597 mL
80 mM 0.0378 mL 0.1890 mL 0.3779 mL 0.9448 mL
100 mM 0.0302 mL 0.1512 mL 0.3023 mL 0.7558 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.

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