AhR Antagonist II, SR1 - CAS 1227633-49-10 - Calbiochem

General description

A cell-permeable purine compound that acts as a high affinity (IC₅₀ = 40 nM against [125I]-N3Br2DD binding to human AhR) AhR antagonist (IC₅₀ = 127 nM against 3 nM TCDD-induced luciferase reporter activity in HepG2 cultures), while exhibiting little or no activity against a panel of 61 kinases. AhR expression and function knockouts by shRNAs, CH-223191 (Cat. No. 182705), or SR1 treatment all result in enhanced and sustained CD34⁺ population in long-term proliferating/expanding cultures of cord blood-derived HSCs (hematopoietic setem cells) in serum-free media containing Tpo (Cat. No. 605218), SCF (Cat. No. 569600), Flt3 Ligand (Cat. No. 343010), and IL-6 (Cat. No. 407652) in a reversible manner (11- and 73-fold increase of total nucleated and CD34⁺ cells, respectively, comparing 1 to 0 µM SR1-treated cultures on day 21; 1118-fold increase in CD34⁺ cells in 1 µM SR1 cultures from day 0 to 21). SR1-expanded CD34⁺ cells retain multilineage potential and the SR1-expanded progeny derived from 300 human CB CD34⁺ cells are reported to exhibit the same level of engraftment efficiency as 10,000 unexpanded CB CD34⁺ cells in NSG SCID mice in vivo. SR1 is reactive toward human, monkey, and canine, but not rat or murine, species.

A cell-permeable purine compound that acts as a high affinity AhR antagonist (IC₅₀ = 127 nM against 3 nM TCDD-induced luciferase reporter activity in HepG2 cultures), but not a panel of 61 kinases. AhR expression and function knockouts by shRNAs, CH-223191 (Cat. No. 182705), or SR1 treatment all result in enhanced and sustained CD34⁺ population in long-term proliferating/expanding cultures of cord blood-derived HSCs (hematopoietic setem cells) in serum-free media containing Tpo (Cat. No. 605218), SCF (Cat. No. 569600), Flt3 Ligand (Cat. No. 343010), and IL-6 (Cat. No. 407652) in a reversible manner. SR1 is reactive toward human, monkey, and canine, but not rat or murine, species.

Packaging

Packaged under inert gas

Warning

Toxicity: Regulatory Review (Z)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Boitano, A.E., et al. 2010. Science329, 1345.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany