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.
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- CAS No.: 2600795-21-7
- Formule: C24H26FN3O2
- Masse moléculaire:407.48
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
IC50 & Target
|
ALK2 |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
98 nM
Compound: 11b; M4K2163
|
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
|
[PMID: 32787083] |
| HEK293 | IC50 |
7475 nM
Compound: 11b; M4K2163
|
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
|
[PMID: 32787083] |
| HEK293 | IC50 |
2.5 μM
Compound: 11b; M4K2163
|
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
|
[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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Masse moléculaire 407.48
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)