Cat. No.: HY-112815

ALK2-IN-2

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ALK2-IN-2 is an orally active and selective inhibitor of ALK2 (ACVR1), with an IC₅₀ value of 9 nM, and over 700-fold selectivity against ALK3. ALK2-IN-2 can inhibit oxidative stress and protect endothelial cells.

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Pureté: 99.93%
CAS No.: 2254409-25-9
Formule: C₂₈H₂₇N₅O₂S
Masse moléculaire:497.61

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

ALK2-IN-2 Chemical Structure

CAS No.: 2254409-25-9

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

ACVR1

9 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform TGF-β Receptor :

In Vitro

ALK2-IN-2 (Compound 23) can inhibit BMP6-induced transcriptional activity in C2C12 cells, with an EC₅₀ of 8 nM^[1].
ALK2-IN-2 (3-100 nM; 6-24 h) has a protective effect on human umbilical vein endothelial cells (HUVECs) and can reduce the damage of oxidative stress to the migration and vascular formation functions of endothelial cells^[2].

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

Cell Viability Assay^[2]

Cell Line:

H₂O₂ treated HUVECs
Concentration:

3, 9, 27, 50 and 100 nM
Incubation Time:

24 h
Result:

Increased cell viability in a dose-dependent manner.

In Vivo

Pharmacokinetic Analysis in mice^[1]

Route	Dose (mg/kg)	AUC_0→∞ (hr·ng/mL)	t_1/2 (h)	C_max (ng/mL)	CL (mL/min/kg)	V_dss (L/kg)	%F
i.v.	3	3220	3.5	/	16	4.6	/
p.o.	3	782	4.3	67	/	/	24

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

Chemical Information

CAS No. 2254409-25-9
Appearance Solid
Masse moléculaire 497.61
Formule C₂₈H₂₇N₅O₂S
Color Light yellow to yellow
SMILES

CC(N1CCCC1)C(C=C2)=CC=C2C(C=N3)=CN4C3=C(C5=CC=C(S(=O)(N)=O)C6=C5C=CC=C6)C=N4
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Journal Impact Factor

J Cell Mol Med

Circulating exosomes repair endothelial cell damage by delivering miR-193a-5p. [Abstract]

2021 Feb;25(4):2176-2189. PMID: 33354912

Solvant et solubilité

In Vitro:

DMSO : 125 mg/mL (251.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0096 mL

10.0480 mL

20.0961 mL

5 mM

0.4019 mL

2.0096 mL

4.0192 mL

10 mM

0.2010 mL

1.0048 mL

2.0096 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (4.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (4.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (277 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Jiang JK, et al. Discovery of 3-(4-sulfamoylnaphthyl)pyrazolo[1,5-a]pyrimidines as potent and selective ALK2 inhibitors. Bioorg Med Chem Lett. 2018 Nov 1;28(20):3356-3362. [Content Brief]

[2]. Cao C, et al. Circulating exosomes repair endothelial cell damage by delivering miR-193a-5p. J Cell Mol Med. 2021 Feb;25(4):2176-2189. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0096 mL	10.0480 mL	20.0961 mL	50.2401 mL
	5 mM	0.4019 mL	2.0096 mL	4.0192 mL	10.0480 mL
	10 mM	0.2010 mL	1.0048 mL	2.0096 mL	5.0240 mL
	15 mM	0.1340 mL	0.6699 mL	1.3397 mL	3.3493 mL
	20 mM	0.1005 mL	0.5024 mL	1.0048 mL	2.5120 mL
	25 mM	0.0804 mL	0.4019 mL	0.8038 mL	2.0096 mL
	30 mM	0.0670 mL	0.3349 mL	0.6699 mL	1.6747 mL
	40 mM	0.0502 mL	0.2512 mL	0.5024 mL	1.2560 mL
	50 mM	0.0402 mL	0.2010 mL	0.4019 mL	1.0048 mL
	60 mM	0.0335 mL	0.1675 mL	0.3349 mL	0.8373 mL
	80 mM	0.0251 mL	0.1256 mL	0.2512 mL	0.6280 mL
	100 mM	0.0201 mL	0.1005 mL	0.2010 mL	0.5024 mL

Keywords

ALK2-IN-2

1 Cited Publications

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ALK2-IN-2

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

TGF-beta/Smad Compound Library

Anti-Aging Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Anti-Cardiovascular Disease Compound Library

Orally Active Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Targeted Diversity Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Osteogenesis Compound Library

Cancer Stem Cells Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) ALK2-IN-2

Voir tous les produits spécifiques à Isoform TGF-β Receptor

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

ALK2-IN-2

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

TGF-beta/Smad Compound Library

Anti-Aging Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Anti-Cardiovascular Disease Compound Library

Orally Active Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Targeted Diversity Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Osteogenesis Compound Library

Cancer Stem Cells Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) ALK2-IN-2

Voir tous les produits spécifiques à Isoform TGF-β Receptor

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

ALK2-IN-2 Related Classifications

HY-112815 Related Classifications