M4K2163
M4K2163 is a ALK2 inhibitor that serves as a target protein ligand for the synthesis of PROTACs, such as M4K3250 (HY-183718). M4K2163 induces cytotoxic effects in glioblastoma cells. M4K2163 can be used in the research of diffuse intrinsic pontine glioma and glioblastoma.
For research use only. We do not sell to patients.
- CAS No.: 2600795-21-7
- Formula: C24H26FN3O2
- Molecular Weight:407.48
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
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ALK2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
98 nM
Compound: 11b; M4K2163
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Competitive displacement of PBI-6908 from nanoluciferase-fused ALK2 (unknown origin) expressed in HEK293 cells incubated for 2 hrs by NanoBRET NanoGlo substrate based NanoBRET assay
Competitive displacement of PBI-6908 from nanoluciferase-fused ALK2 (unknown origin) expressed in HEK293 cells incubated for 2 hrs by NanoBRET NanoGlo substrate based NanoBRET assay
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[PMID: 32787083] |
| HEK293 | IC50 |
7475 nM
Compound: 11b; M4K2163
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Inhibition of recombinant human ALK5 expressed in HEK293 cells transfected with CAGA-luciferase and Renilla luciferase reporter after 24 hrs by dual luciferase reporter assay
Inhibition of recombinant human ALK5 expressed in HEK293 cells transfected with CAGA-luciferase and Renilla luciferase reporter after 24 hrs by dual luciferase reporter assay
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[PMID: 32787083] |
| HEK293 | IC50 |
2.5 μM
Compound: 11b; M4K2163
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Inhibition of human ERG expressed in HEK293 cells after 5 mins by IonWorks barracuda patch clamp method
Inhibition of human ERG expressed in HEK293 cells after 5 mins by IonWorks barracuda patch clamp method
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[PMID: 32787083] |
In Vitro
M4K2163 (96 h) reduces viability of U87-MG glioblastoma cells in a dose-dependent manner over 96 h, with cytotoxic activity independent of CRBN recruitment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2600795-21-7
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Molecular Weight 407.48
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Formula C24H26FN3O2
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SMILES
CC1=C(C2=CC=C(N3CCNCC3)C=C2)C=NC=C1C4=CC(OC)=C(F)C(OC)=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
M4K2163 Related Classifications
HY-183720 Related Classifications
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