UNC8153 (TFA)

UNC8153 TFA is a potent and selective nuclear receptor-binding SET domain-containing 2 (NSD2) -targeted degrader with a Kd of 24 nM. UNC8153 TFA reduces the cellular levels of both NSD2 protein (DC50 in cell U2OS is 0.35 μM) and the H3K36me2 chromatin mark. UNC8153 TFA contains a simple warhead that confers proteasome-dependent degradation of NSD2[1].

Product Specifications

CAS Number

[2929304-61-8]

UNSPSC

12352005

Target

Histone Methyltransferase

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/unc8153-tfa.html

Purity

99.92

Solubility

DMSO : 100 mg/mL (ultrasonic) |H2O : 12.5 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(C(F)(F)F)O.O=C(C1=CC=C(CN(C2CC2)C(C3=CC=C4NC(COC4=C3)=O)=O)C=C1)NC5=CC=C(C(NCCCCCCN)=O)C=C5

Molecular Formula

C35H38F3N5O7

Molecular Weight

697.70

References & Citations

[1]Ronan P Hanley, et al. Discovery of a Potent and Selective Targeted NSD2 Degrader for the Reduction of H3K36me2. J Am Chem Soc. 2023 Apr 12;145 (14) :8176-8188.