JET-209

• Description :

  JET-209 is a potent CBP/p300 PROTAC degrader, with DC50 values of 0.05 nM and 0.2 nM for CBP and p300. JET-209 demonstrates remarkable anti-tumor activity against various acute leukemia cell lines and effectively inhibits tumor growth in xenograft tumor models. JET-209 can be used for the study of acute leukemia (Pink: CBP/p300 ligand (HY-175620) ; Blue: CRBN ligand (HY-132248) ; Black: Linker; CBP/p300 ligand + Linker (HY-175621) ) [1].

• UNSPSC :

  12352005

• Target :

  Histone Acetyltransferase; PROTACs

• Type :

  Reference compound

• Related Pathways :

  Epigenetics; PROTAC

• Applications :

  Cancer-programmed cell death

• Field of Research :

  Cancer

• Assay Protocol :

  https://www.medchemexpress.com/jet-209.html

• Concentration :

  10mM

• Purity :

  98.09

• Solubility :

  DMSO : 100 mg/mL (ultrasonic)

• Smiles :

  CC(N1CCC2=C(C(C3=CC=CC4=C3C=NC(C5=CN=C(C=C5)C(NC6CCN(CC6)C7=CC8=C(C(N(C8)C9CCC(NC9=O)=O)=O)C=C7)=O)=C4)=NN2C%10CCOCC%10)C1)=O

• Molecular Formula :

  C46H47N9O6

• Molecular Weight :

  821.92

• References & Citations :

  [1]Thomas JE 2nd, et al. Discovery of Exceptionally Potent, Selective, and Efficacious PROTAC Degraders of CBP and p300 Proteins. J Med Chem. 2023 Jun 22;66 (12) :8178-8199.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  CBP/p300; Cereblon

• CAS Number :

  [3033714-58-5]