2. M4K3233

M4K3233 is a selective ALK2 PROTAC degrader with a pDC50 of 7.3 and a pIC50 of 6.6. M4K3233 recruits CRBN to form a ternary complex with ALK2, mediating ALK2 degradation via the proteasomal and lysosomal pathways. M4K3233 induces moderate downregulation of RIPK2 and significant downregulation of SIK3 in mammalian cells. M4K3233 is applicable to research related to glioblastoma.
(Pink: ALK2 ligand (HY-149591); Blue: Cereblon ligand (HY-14658); Black: linker).

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M4K3233

M4K3233 Chemical Structure

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M4K3233 Related Antibodies

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Description

M4K3233 is a selective ALK2 PROTAC degrader with a pDC50 of 7.3 and a pIC50 of 6.6. M4K3233 recruits CRBN to form a ternary complex with ALK2, mediating ALK2 degradation via the proteasomal and lysosomal pathways. M4K3233 induces moderate downregulation of RIPK2 and significant downregulation of SIK3 in mammalian cells. M4K3233 is applicable to research related to glioblastoma[1]. (Pink: ALK2 ligand (HY-149591); Blue: Cereblon ligand (HY-14658); Black: linker).

In Vitro

M4K3233 (1 μM; 24 h) is a selective ALK2 degrader in ALK2-overexpressing HEK-293 cells and U87-MG glioblastoma cells, significantly reducing ALK2 levels alongside a small set of off-target proteins including PDE6D, FIZ1, SIK3, and RIPK2, while sparing most other kinases[1].
M4K3233 (serial dilutions; 4 h) promotes ternary complex formation between ALK2 and CRBN in HEK-293 cells with an apparent pEC50 of 7.42, as measured by a NanoBRET PPI assay[1].
M4K3233 (0.0002-30 μM; 8 days) inhibits proliferation of patient-derived PDHGG cell lines with GI50 values from 0.3 μM to 5 μM, but this effect appears independent of CRBN-mediated ALK2 degradation[1].
M4K3233 (0.0002-30 μM; 4 days) reduces viability of U87-MG glioblastoma cells, but this cytotoxic effect is independent of CRBN-mediated ALK2 degradation[1].

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

M4K3233 Related Antibodies

Western Blot Analysis[1]

Cell Line: ALK2-HiBiT transfected HEK-293 cells
Concentration: 1 μM (M4K3233, 24 h incubation); 20 μM pomalidomide (20 min pretreatment); 20 μM M4K2009 (20 min pretreatment); 1 μM MG132 (20 min pretreatment); 1 μM bafilomycin A1 (20 min pretreatment)
Incubation Time: 24 h (M4K3233 treatment); 20 min (pretreatments)
Result: Blocked ALK2 degradation when cells were pretreated with either pomalidomide or M4K2009, confirming reliance on both ALK2 and CRBN binding.
Partially recovered ALK2 levels when cells were pretreated with either MG132 or bafilomycin A1, while combined pretreatment with both inhibitors completely blocked ALK2 degradation.
Molecular Weight

772.89

Formula

C44H48N6O7
SMILES

CC1=C(C2=CC=C(N3CCN(CC4CCN(C5=CC=C(C(N(C6CCC(NC6=O)=O)C7=O)=O)C7=C5)CC4)CC3)C=C2)C=NC=C1C8=CC(OC)=C(OC)C(OC)=C8
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Purity & Documentation
References
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M4K3233 Related Classifications

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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.

Keywords:

M4K3233human liver microsomesmouse liver microsomesALK2SIK3CRBNPDE6DFIZ1HEK-293 cellsALK5RIPK2Inhibitorinhibitorinhibit

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