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182706

Sigma-Aldrich

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.

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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:
Molecular Weight:
429.54
MDL number:

Quality Level

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

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This Item
182705574661227016
AhR Antagonist The AhR Antagonist, also referenced under CAS 301326-22-7, controls the biological activity of AhR.

Sigma-Aldrich

182705

AhR Antagonist

CCR2 Antagonist The CCR2 Antagonist, also referenced under CAS 445479-97-0, controls the biological activity of CCR2.

Sigma-Aldrich

227016

CCR2 Antagonist

form

solid

form

-

form

solid

form

solid

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, desiccated (hygroscopic), protect from light

color

white

color

orange-brown

color

white

color

white

solubility

DMSO: 100 mg/mL

solubility

DMSO: 10 mg/mL

solubility

DMSO: 50 mg/mL, nearly colorless

solubility

ethanol: 6 mg/mL, DMSO: 60 mg/mL

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


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