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