Art. -Nr.: HY-148234

M4K2234

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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).

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Reinheit: 98.31%
CAS. Nr.: 2421141-51-5
Formel: C₂₇H₃₁FN₄O₂
Molecular Weight:462.56

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

M4K2234 Chemical Structure

CAS. Nr.: 2421141-51-5

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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)

Alle TGF-beta/Smad Isoform-spezifische Produkte anzeigen :

Smad1
Smad3

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]

In Vitro

M4K2234 (16 nM) potently inhibits BMP7-stimulated reporter gene activity in HEK293 cells, while showing 50-fold and 150-fold weaker inhibition on activin A and TGF-β1-induced CAGA-responsive reporter, respectively^[1].
M4K2234 (0.5-1 μM) specifically inhibits phosphorylation of SMAD1/5/8 induced by BMP family ligands in HEK293T cells, without affecting SMAD2/3 phosphorylation induced by activin A or TGF-β1^[1].
M4K2234 shows an IC₅₀ of 7 nM for ALK1 and 14 nM for ALK2 in enzyme kinetic assays, with weak inhibition on ALK6 (88 nM) and negligible activity on ALK4/5 (>10,000 nM)^[1].

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

Parmacokinetics

Species	Dose	Route	T_1/2	C_max	V_ss
Mice^[1]	10 mg/kg	p.o.	1.3 h	0.3 μM	3

In Vivo

1.19 Pharmacokinetic Properties of M4K2234 in Mice ^[1].

	Mice PO 3 mg/kg
C_max(ng/mL)	1650
AUC_inf(ng·h/mL)	4630
t_1/2(h)	2.61

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

Chemical Information

CAS. Nr. 2421141-51-5
Appearance Solid
Molecular Weight 462.56
Formel C₂₇H₃₁FN₄O₂
Color Light brown to brown
SMILES

O=C(C1=C(C=C(C2=CN=CC(C3=CC=C(N4CCN(C(C)C)CC4)C=C3)=C2C)C=C1OC)F)N
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (216.19 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

2.1619 mL

10.8094 mL

21.6188 mL

5 mM

0.4324 mL

2.1619 mL

4.3238 mL

10 mM

0.2162 mL

1.0809 mL

2.1619 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, 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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)
Handling Instructions (2659 KB)

Verweise

[1]. Němec V, et al. Discovery of Two Highly Selective Structurally Orthogonal Chemical Probes for Activin Receptor-like Kinases 1 and 2. J Med Chem. 2024 Aug 8;67(15):12632-12659. [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, 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	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

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M4K2234

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

TGF-beta/Smad Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Orally Active Compound Library

Angiogenesis-Related Compound Library

Transcription Factor-Targeted 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

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle TGF-beta/Smad Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

M4K2234

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

TGF-beta/Smad Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Orally Active Compound Library

Angiogenesis-Related Compound Library

Transcription Factor-Targeted 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

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle TGF-beta/Smad Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

M4K2234 Related Classifications

HY-148234 Related Classifications