UNC8153 (TFA)

• Description:

  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].

• 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.

• Shipping Conditions:

  Blue Ice

• Storage Conditions:

  -20°C (Powder, sealed storage, away from moisture)

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• CAS Number:

  2929304-61-8