UNC10415667
UNC10415667 is a non-competitive, non-prodrug NSD2 degrader with a DC50 of 460 nM in U2OS NSD2 HiBiT cells. UNC10415667 forms a reversible covalent hemithioacetal bond with Cys326 of FBXO22, promoting the formation of a ternary complex with FBXO22 and NSD2, which in turn triggers the polyubiquitination and degradation of NSD2 via the ubiquitin-proteasome system. UNC10415667 can form complexes with FBXO22, NSD2 and BACH1 simultaneously, driving the synchronized degradation of NSD2 and BACH1 without competition. UNC10415667 can be used in research related to multiple myeloma, acute lymphoblastic leukemia, and prostate cancer.
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- Fòrmula: C37H32N4O6
- Peso molecular:628.67
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
NSD2 460 nM (DC50) |
In Vitro
UNC10415667 potently induces polyubiquitination of purified NSD2 PWWP1 domain via SCF-FBXO22 in vitro[1].
UNC10415667 (1 µM; 6 h) potently degrades NSD2 in U2OS NSD2 HiBiT cells with a DC50 of 460 nM, achieving ~75% degradation at 1 µM over 6 hours[1].
UNC10415667 mediates formation of a stable ternary complex between purified FBXO22 FIST domain and NSD2 PWWP1 domain in a Cys326-dependent manner[1].
UNC10415667 binds purified FBXO22 FIST domain in a Cys326-dependent manner, as demonstrated by a significant increase in the domain's melting temperature[1].
UNC10415667 forms a stable covalent ternary complex with SCF-FBXO22 and NSD2 PWWP1 domain, adopting a conformation nearly identical to that of UNC10088C[1].
UNC10415667 mediates positive cooperative binding between purified FBXO22 FIST domain and NSD2 PWWP1 domain, as measured by TR-FRET displacement[1].
UNC10415667 mediates formation of a stable quaternary complex containing purified FBXO22 FIST domain, NSD2 PWWP1 domain, and BACH1 BTB domain, indicating simultaneous binding of both neosubstrate and native substrate to FBXO22[1].
UNC10415667 (10 µM; 6 h) completely degrades NSD2 in HEK293T cells at 10 µM over 6 hours without perturbing BACH1 levels, and simultaneous degradation of NSD2 and native FBXO22 substrate BACH1 is achievable when combined with Hemin (HY-19424)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
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Cell Line:HEK293T cells
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Concentration:10 µM
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Incubation Time:6 h
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Result:Completely degraded NSD2 without affecting BACH1 levels.
Chemical Information
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Peso molecular 628.67
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Fòrmula C37H32N4O6
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SMILES
O=C(C1=CC=C(N2)C(OCC2=O)=C1)N(C3CC3)CC4=CC=C(C(NC5=CC6=C(CN(C(C7=CC=C(C=O)C=C7)=O)CC6)C=C5)=O)C=C4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)