[CAS NO. 937039-45-7] PimelicDiphenylamide106
PRODUCTS SPECIFICATIONS [937039-45-7]
DESCRIPTION [937039-45-7]
Overview
| MDL | MFCD17010287 |
|---|---|
| Molecular Weight | 339.43 |
| Molecular Formula | C20H25N3O2 |
| SMILES | O=C(NC1=CC=CC=C1N)CCCCCC(NC2=CC=C(C)C=C2)=O |
3 Publications Citing Use of MCE
Summary
Pimelic Diphenylamide 106 is a slow, tight-binding inhibitor of class I HDAC (HDAC 1, 2, and 3, with IC50 values of 150 nM , 760nM, and 370 nM, respectively), demonstrating no activity against class II HDACs. IC50 value: 150 nM (HDAC1), 370 nM (HDAC3), 760nM(HDAC2) Target: HDAC in vitro: Pimelic Diphenylamide 106 has preference toward HDAC3 with Ki of 14 nM, 15 times lower than the Ki for HDAC1 . Pimelic Diphenylamide 106 exhibits weaker inhibitory activities against HDAC 8 with IC50 of 5 μM after a 3-h preincubation with HDAC8 .
IC50 & Target
|
HDAC1 150 nM (IC 50 ) |
HDAC3 370 nM (IC 50 ) |
HDAC2 760 nM (IC 50 ) |
HDAC8 5000 nM (IC 50 ) |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 125 mg/mL ( 368.26 mM ; ultrasonic and warming and heat to 60°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.9461 mL | 14.7306 mL | 29.4612 mL |
| 5 mM | 0.5892 mL | 2.9461 mL | 5.8922 mL |
| 10 mM | 0.2946 mL | 1.4731 mL | 2.9461 mL |
References
- [1] Chou CJ, et al. Pimelic diphenylamide 106 is a slow, tight-binding inhibitor of class I histone deacetylases. J Biol Chem. 2008 Dec 19;283(51):35402-35409.
- [2] Xu C, et al. Chemical probes identify a role for histone deacetylase 3 in Friedreich's ataxia gene silencing. Chem Biol. 2009 Sep 25;16(9):980-989.