5.30654

c-Rel Inhibitor, IT-603

• 동의어(들): 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
• 실험식(Hill 표기법): C₁₁H₉BrN₂O₃S
• CAS Number: 292168-90-2
• Molecular Weight: 329.17
• UNSPSC 코드: 51111800
• PubChem Substance ID: 840180
• NACRES: NA.77

속성

• 분석: ≥97% (HPLC)
• Quality Level: 100
• 형태: powder
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: dark yellow
• solubility: DMSO: 100 mg/mL
• 저장 온도: 2-8°C
• SMILES string: COC1=CC(=CC(=C1O)C=C2C(=O)NC(=S)N2)Br

설명

일반 설명

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).

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.

생화학적/생리학적 작용

Cell permeable: yes

Primary Target
c-Rel

Reversible: yes

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

재구성

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.

기타 정보

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

법적 정보

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

안전성 정보

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