182706

SR1

≥98% (HPLC), solid, AhR antagonist, Calbiochem^®

• Synonym(s): AhR Antagonist II, SR1, 4-(2-(2-(Benzo[b]thiophen-3-yl)-9-isopropyl-9H-purin-6-ylamino)ethyl)phenol, 4-[2-[[2-Benzo[b]thien-3-yl-9-(1-methylethyl)-9H-purin-6-yl]amino]ethyl]phenol, StemRegenin 1
• Empirical Formula (Hill Notation): C₂₄H₂₃N₅OS
• CAS Number: 1227633-49-9
• Molecular Weight: 429.54
• MDL number: MFCD16987861
• UNSPSC Code: 51111800
• NACRES: NA.51

Properties

• product name: AhR Antagonist II, SR1, The AhR Antagonist II, SR1 controls the biological activity of AhR. This small molecule/inhibitor is primarily used for Biochemicals applications.
• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: DMSO: 100 mg/mL
• shipped in: wet ice
• storage temp.: 2-8°C
• InChI: 1S/C24H23N5OS/c1-15(2)29-14-26-21-23(25-12-11-16-7-9-17(30)10-8-16)27-22(28-24(21)29)19-13-31-20-6-4-3-5-18(19)20/h3-10,13-15,30H,11-12H2,1-2H3,(H,25,27,28)
• InChI key: BGFHMYJZJZLMHW-UHFFFAOYSA-N

Description

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable