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

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.

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OD36 Chemical Structure

OD36 Chemical Structure

CAS No. : 1638644-62-8

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Based on 1 publication(s) in Google Scholar

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Description

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)

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].

MedChemExpress (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.
In Vivo

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

MedChemExpress (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.
Molecular Weight

330.77

Formula

C16H15ClN4O2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC(C2=C3N/C(C=CN3N=C2)=N/CCOCCO4)=CC4=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (100.76 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
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OD36 Related Classifications

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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OD36
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