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UNC8153 TFA

Chemical Structure : UNC8153 TFA

CAS No.: 2929304-61-8

UNC8153 TFA (UNC 8153 TFA)

Catalog No.: PC-22591Not For Human Use, Lab Use Only.

UNC8153 (UNC 8153) TFA is a selective NSD2-targeted degrader with binding Kd of 24 nM for NSD2, potently and selectively reduces the cellular levels of both NSD2 protein (DC50=350 nM) and the H3K36me2 chromatin mark.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

UNC8153 (UNC 8153) TFA is a selective NSD2-targeted degrader with binding Kd of 24 nM for NSD2, potently and selectively reduces the cellular levels of both NSD2 protein (DC50=350 nM) and the H3K36me2 chromatin mark.
UNC8153 contains a simple warhead that confers proteasome-dependent degradation of NSD2 through a novel mechanism.
UNC8153 downregulates pathological phenotypes in multiple myeloma cells including mild antiproliferative effects in MM1.S cells containing an activating point mutation and antiadhesive effects in KMS11 cells harboring the t(4;14) translocation.

Physicochemical Properties

M.Wt 697.71
Formula C35H38F3N5O7
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(4-((4-((6-aminohexyl)carbamoyl)phenyl)carbamoyl)benzyl)-N-cyclopropyl-3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazine-7-carboxamide 2,2,2-trifluoroacetate

References

1. Ronan P Hanley, et al. J Am Chem Soc. 2023 Mar 28. doi: 10.1021/jacs.3c01421.

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