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SP-100030 

Cat. No. M28589
SP-100030  Structure
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Biological Activity

SP-100030 is a potent NF-κB and activator protein-1 (AP-1) double inhibitor (IC50s=50 and 50 nM, respectively). SP-100030 inhibits IL-2, IL-8, and TNF-alpha production in Jurkat and other T cell lines. SP-100030 decreases murine collagen-induced arthritis (CIA).

Chemical Information
Molecular Weight 437.65
Formula C14H5ClF9N3O
CAS Number 154563-54-9
Form Solid
Solubility (25°C) DMSO 50 mg/mL (ultrasonic)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

References

[1] Na Ye, et al. J Med Chem. Small molecule inhibitors targeting activator protein 1 (AP-1)

[2] Rodrigo Moore-Carrasco, et al. Anticancer Res. Both AP-1 and NF-kappaB seem to be involved in tumour growth in an experimental rat hepatoma

[3] Hajime Fujimoto, et al. Am J Respir Crit Care Med. Inhibition of nuclear factor-kappaB in T cells suppresses lung fibrosis

[4] Rodrigo Moore-Carrasco, et al. Int J Oncol. The AP-1/NF-kappaB double inhibitor SP100030 can revert muscle wasting during experimental cancer cachexia

[5] Deborah Phippard, et al. Methods Mol Biol. Screening for inhibitors of transcription factors using luciferase reporter gene expression in transfected cells

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Keywords: SP-100030  supplier, NF-κB, inhibitors, activators

 
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