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Chemical Structure| 446859-33-2 Chemical Structure| 446859-33-2

Structure of RepSox
CAS No.: 446859-33-2

Chemical Structure| 446859-33-2

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RepSox (E-616452) is a potent and selective TGF-β-RI/ALK5 inhibitor.

Synonyms: E-616452; SJN 2511

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Product Details of RepSox

CAS No. :446859-33-2
Formula : C17H13N5
M.W : 287.32
SMILES Code : CC1=CC=CC(=N1)C1=NNC=C1C1=CC=C2N=CC=CC2=N1
Synonyms :
E-616452; SJN 2511
MDL No. :MFCD09037561
InChI Key :LBPKYPYHDKKRFS-UHFFFAOYSA-N
Pubchem ID :449054

Safety of RepSox

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • TGFβRI/ALK5

    TGFβR1(ALK5), IC50:4 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
mouse embryonic fibroblasts (MEFs) 1 μM 10 days induction of compact cell colonies and activation of Sox2 expression PMC4042166
mouse tail-tip fibroblasts (TTFs) 1 μM 10 days upregulation of Sox2 expression and formation of neural progenitor-like cells PMC4042166
Mouse embryonic fibroblasts (MEFs) 7.5 µM 14-17 days RepSox, as a TGF-β inhibitor, in combination with p53DD and hRasG12V, significantly increased the efficiency of induced motor neuron (iMN) reprogramming, reduced genomic stress, and expanded the population of hypertranscribing and hyperproliferating cells (HHCs). PMC6778044
human urinary cells (HUCs) 1 μM 20 days formation of compact cell colonies and induction of neural progenitor-like cells PMC4042166
hCMEC/d3 cells 100 μM 24 hours RepSox significantly increased Cldn5 mRNA expression and enhanced barrier properties, as indicated by increased transendothelial electrical resistance (TEER) and reduced permeability to 40 kDa FITC-dextran (FD40). PMC9010415
hPSC-ECs 10 μM 48 hours RepSox significantly elevated endothelial cell barrier stability, reduced paracellular permeability, and prevented VEGFA-induced barrier breakdown. PMC7443870
hBMECs 10 μM 48 hours RepSox significantly elevated endothelial cell barrier stability, reduced paracellular permeability, and prevented VEGFA-induced barrier breakdown. PMC7443870
hRMECs 10 μM 48 hours RepSox significantly elevated endothelial cell barrier stability, reduced paracellular permeability, and prevented VEGFA-induced barrier breakdown. PMC7443870
cardiomyocytes 20 μM 5 days Evaluate the effects of RepSox on cardiomyocyte viability and proliferation, results showed that RepSox significantly improved cardiomyocyte survival and proliferation. PMC7942842
cardiac fibroblasts 20 μM 5 days Evaluate the effects of RepSox on cardiac fibroblast proliferation and myodifferentiation, results showed that RepSox inhibited fibroblast proliferation and myodifferentiation. PMC7942842
endothelial cells 20 μM 5 days Evaluate the effects of RepSox on endothelial cell proliferation and vascular network formation, results showed that RepSox significantly enhanced endothelial cell proliferation and vascular network formation. PMC7942842
human epidermal stem cells (hESC) 5 µM 6 to 8 days Conversion of human epidermal stem cells into intestinal goblet cells with an efficiency of ~95% PMC8046373
Oct4∷GFP transgenic mouse embryonic fibroblasts (MEFs) 25 μM 7-11 days RepSox replaces Sox2 in reprogramming by inhibiting Tgf-β signaling and inducing Nanog expression. PMC3335195
SH-SY5Y/6TR(EU)/pTrex-Dest-30/MYCN (SY5Y-MYCN) 1 - 100 nM 72 hours RepSox significantly attenuated RA-mediated neuronal differentiation, indicating that TGF-β signaling inhibition plays a crucial role in retinoid-mediated differentiation in neuroblastoma cells. PMC5303304
Adult tail tip fibroblasts 25 μM RepSox effectively replaces Sox2 in adult tail tip fibroblasts, inducing reprogramming. PMC3335195

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6J mice Kainic acid-induced epilepsy model via intrahippocampal injection Intraperitoneal injection 10 mg/kg Every other day for 7 days RepSox significantly reduced the severity of seizures and attenuated blood-brain barrier disruption. PMC9010415
rats myocardial infarction model intramyocardial injection 20 mg/mL single injection, lasting 5 weeks Evaluate the therapeutic effects of RepSox on myocardial infarction in rats, results showed that RepSox significantly improved cardiac function, reduced fibrosis and inflammatory response, and promoted angiogenesis. PMC7942842
Mice neonatal mouse retina model exogenous delivery 3 mg/kg not specified RepSox significantly altered vascular patterning in the neonatal mouse retina, reducing the propagation of the angiogenic front but not changing the number of tip-cell microvilli. PMC7443870

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.48mL

0.70mL

0.35mL

17.40mL

3.48mL

1.74mL

34.80mL

6.96mL

3.48mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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