(R,R)-CPI-1612 is the inactive isomer of CPI-1612 and could be utilized as a control compound in experiments. CPI-1612 is a potent orally bioactive EP300/CBP histone acetyltransferase (HAT) inhibitor (antagonist) with IC50 of 8.1 nM for EP300 HAT. CPI-1612 has anti-cancer activity.

Physicochemical Properties

CAS #	2374972-35-5
Related CAS #	CPI-1612;2374971-81-8;(S,S)-CPI-1612;2374971-82-9
PubChem CID	156293396
Appearance	Off-white to light yellow solid powder
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	5
Rotatable Bond Count	8
Heavy Atom Count	34
Complexity	692
Defined Atom Stereocenter Count	2
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

References

[1]. Jonathan E Wilson, et al. Discovery of CPI-1612: A Potent, Selective, and Orally Bioavailable EP300/CBP Histone Acetyltransferase Inhibitor. ACS Med Chem Lett. 2020 Apr 23;11(6):1324-1329.

Solubility Data

Solubility (In Vitro)

DMSO: 130 mg/mL (288.55 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 3.25 mg/mL (7.21 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 32.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)