Theaflavin 3,3'-digallate (TF3) is an antitumor agent. Theaflavin 3,3'-digallate inhibits HCT116 cell growth with an IC50 of 17.26 μM. Theaflavin 3,3'-digallate causes a rapid and sustained decrease in phospho-ERK1/2 and -MEK1/2 protein expression. TF-3 and EGCG have stronger inhibitory effects on Dnmt3a and Dnmt3b than on other methyltransferases. In addition, in silico analysis predicted that TF-3 would bind most specifically to the catalytic domain of Dnmt3a. Injection of TF-3 into control mice 6 weeks after OVX protected against bone loss, which was associated with a lower number of osteoclasts as compared to the numbers in vehicleinjected (saline) OVX mice, but TF-3 had a negligible effect on bone mass and osteoclast number in Dnmt3aRank−/− OVX mice compared to vehicle-injected Dnmt3aRank−/− OVX mice, indicating that, in osteoclasts, TF-3 exerts its effect specifically on Dnmt3a.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO ≥ 20 mg/mL|
|Storage||-20°C, protect from light, dry, sealed|
|Related Akt Products|
Loureirin A is a flavonoid extracted from Dragon's Blood, it can inhibit Akt phosphorylation.
Afuresertib hydrochloride is an orally bioavailable, potent and ATP-competitive inhibitor of the serine/threonine protein kinase Akt with potential antineoplastic activity.
Miransertib, also known as ARQ 092, is an oral activie, potent and selective AKT inhibitor with IC50 values: 5.0 nM (AKT1); 4.5 nM (AKT2); 16 nM (AKT3).
GSK2141795 is a potent and selective pan-Akt inhibitor with IC50 values of 180 nM for Akt1, 328 nM for Akt2, and 38 nM for Akt3 respectively (Clinical phase 1).
GDC-0068(RG 7440) 2Hcl is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5 nM/18 nM/8 nM, 620-fold selectivity over PKA.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.