TTP 22 is a high affinity, ATP-competitive casein kinase 2 (CK2) inhibitor with (IC50= 0.1μM, Ki=40nM). TTP 22 shows selectivity for CK2 over JNK3, ROCK1, and MET(IC50> 10 uM). TTP 22 turns to be selective for CK2 over JNK3, ROCK1, and MET (inhibitory effects displayed at greater than 10 μM). TTP 22 is highly conserved serine/threonine protein kinase and it is also involved in cell proliferation, cell differentiation and apoptosis.
|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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 100 mg/mL|
Synthesis and biological evaluation of substituted (thieno[2,3-d]pyrimidin-4-ylthio)carboxylic acids as inhibitors of human protein kinase CK2.
Golub AG, et al. Eur J Med Chem. 2011 Mar;46(3):870-6. PMID: 21276643.
|Related Casein Kinase Products|
LH846 is a selective inhibitor of casein kinase with IC50 values of 290 nM, 1.3 μM and 2.5 μM for CK1δ, ε and α, respectively.
SR-3029 is a potent and ATP competitive CK1δ and CK1ε inhibitor, with IC50s of 44 nM and 260 nM, respectively.
TA-01 potently inhibits CK1ε, CK1δ,and p38α (IC50values are 6.4, 6.8, and 6.7 nM respectively).
TBB(NSC 231634) is a highly selective, ATP/GTP-competitive inhibitor of casein kinase-2 (CK2)with IC50s of 0.9 and 1.6 μM for rat liver and human recombinant CK2 respectively).
D4476 is a selective inhibitor of casein kinase 1 (CK1) and TGF-β type-I receptor (ALK5) with IC50 of 0.3 µM and 0.5 µM, respectively.
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