JET-209

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].

Product Specifications

CAS Number

[3033714-58-5]

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.