Thiazovivin is a selective small molecule Rho-associated kinase (ROCK) inhibitor. When used in combination with ALK5 inhibitor SB-431542 and MEK inhibitor PD-0325901 , it significantly improves (200-fold) the efficiency of iPSC generation from human fibroblast reprogramming. Thiazovivin also improves the survival of human embryonic stem cells upon trypsinization. More over, by regulating E-cadherin mediated cell-cell interaction, Thiazovivin can protects human ES cells from death in the absence of ECM.
|Cell lines||hESCs cells|
|Preparation method||For clonal survival assays, single hESCs were diluted to clonal density and plated onto 96-well Matrigel-coated plate. For lowdensity survival assays, 500 cells were plated onto 96-well Matrigelcoated plate. To visualize hESC colonies, cultures were fixed in 4% paraformaldehyde in phosphate buffered saline (PBS) for 5 min, washed once in PBS, then stained for alkaline phosphatase (ALP) activity as described in the manufacturer’s instructions. ALP positive colonies were counted on an inverted microscope.|
|Incubation time||4 days|
|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 25 mg/mL|
Direct conversion of porcine embryonic fibroblasts into adipocytes by chemical molecules.
Zhu et al. Cell Reprogram. 2012 Apr;14(2):99-105. PMID: 22372576.
|Related ROCK Products|
SAR407899 is a potent and selective, ATP-competitive ROCK inhibitor with IC50 of 135 nM for ROCK-2, and Kis of 36 nM and 41 nM for human and rat ROCK-2, respectively.
Belumosudil mesylate (SLx-2119 mesylate) is an orally bioavailable inhibitor of ROCK-II that is greater than 200-fold selective over ROCK-I (IC50s = 105 nM and 24 µM, respectively).
BDP5290 is a potent inhibitor of both ROCK and MRCK with IC50s of 5 nM, 50 nM, 10 nM and 100 nM for ROCK1, ROCK2, MRCKα and MRCKβ, respectively.
SLx-2119, also known as KD-025, is an orally bioavailable inhibitor of ROCK-II with IC50 of 105 nM.
ZINC00881524 is a potent and selective ROCK inhibitor.
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