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5.30654

c-Rel Inhibitor, IT-603

Name: c-Rel Inhibitor, IT-603
Brand: MM

別名:

c-Rel Inhibitor, IT-603, (5 Z)-5-((5-Bromo-2-hydroxy-3-methoxyphenyl)methylidene)-2-sulfanylideneimidazolidin-4-one, (5 Z)-5-(5-Bromo-2-hydroxy-3-methoxybenzylidene)-2-thioxo-4-imidazolidinone, IT603, (5Z)-5-((5-Bromo-2-hydroxy-3-methoxyphenyl)methylidene)-2-sulfanylideneimidazolidin-4-one, (5Z)-5-(5-Bromo-2-hydroxy-3-methoxybenzylidene)-2-thioxo-4-imidazolidinone, IT603

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この商品について

実験式（ヒル表記法）:

C₁₁H₉BrN₂O₃S

CAS番号:

292168-90-2

分子量:

329.17

MDL number:

MFCD02109025

UNSPSC Code:

51111800

NACRES:

NA.77

PubChem Substance ID:

840180

Assay:

≥97% (HPLC)

Form:

powder

Storage condition:

OK to freeze, protect from light

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特性

assay

≥97% (HPLC)

Quality Segment

100

form

powder

manufacturer/tradename

Calbiochem^®

storage condition

OK to freeze, protect from light

color

dark yellow

solubility

DMSO: 100 mg/mL

storage temp.

2-8°C

SMILES string

COC1=CC(=CC(=C1O)C=C2C(=O)NC(=S)N2)Br

InChI

1S/C11H9BrN2O3S/c1-17-8-4-6(12)2-5(9(8)15)3-7-10(16)14-11(18)13-7/h2-4,15H,1H3,(H2,13,14,16,18)

InChI key

PYLYAEDUIKQBOT-UHFFFAOYSA-N

詳細

General description

A cell-permeable benzylidene-thioxo-imidazolidinone compund that directly and reversibly binds to c-Rel to change its conformation and blocks its DNA binding and transcriptional activity (IC₅₀ = 3 µM in EMSA). Shows good selectivity over Oct1 and AP1. Reduces IL-2 expression in activated T cells without affecting their viability. Induces growth arrest in diffuse large B-cell lymphoma (DLBCL) cell line Ly3 (IC₅₀ = 18 uM). Shown to reduce alloactivation in T cells and diminish graft-versus-host disease (GVHD), but does not impair TCR-mediated killing. Improves the survival rate of lethally irradiated BABL/c mice transplanted with T cell depleted bone marrow cells from C57BL/6 mice (~24 mg/kg, i.p, daily).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
c-Rel

Reversible: yes

Packaging

Packaged under inert gas

Preparation Note

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

Use only fresh DMSO for reconstitution.

Other Notes

Shono, Y., et al. 2014. Cancer Discovery4, 578.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

保管分類

11 - Combustible Solids

一体何が起きているの？

WGK 3

引火点 (F)

Not applicable

引火点（°C）