Millipore Sigma Vibrant Logo

531535 AP-1/NF-κB Dual Inhibitor, SP100030 - CAS 154563-54-9 - Calbiochem

A cell-permeable, potent, reversible T-cell specific inhibitor of both AP-1 and NF-κB transcriptional activation (IC₅₀ = 50 nM)

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 2-Chloro-4-(trifluoromethyl)pyrimidine-5-N-(3ʹ,5ʹ-bis(trifluoromethyl)phenyl)-carboxamide, N-(3,5-bis(Trifluoromethyl)phenyl)-2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxamide, Activator Protein-1 Activation Inhibitor; AP-1 Activation Inhibitor, NF-κB Activation Inhibitor XI, SP-100030, Nuclear Factor-κB Activation Inhibitor XI

Primary Target: AP-1 and NF-κB
View Products on Sigmaaldrich.com
531535
가격 및 재고 조회

개요

Replacement Information

주요 사양표

CAS #Empirical Formula
154563-54-9C₁₄H₅ClF₉N₃O

가격 및 재고여부

카탈로그 번호 재고 정보패킹 포장 단위 가격(VAT 별도) 수량
5.31535.0001
재고 정보 검색...
—
현재 재고 없음 현재 재고 없음
예상 출고 가능일 
단종품
제한된 수량 가능
재고여부 확인
    Remaining: will advise
      Remaining: will advise
      추천사항
      고객 서비스로 문의
      Contact Customer Service

      		 Glass bottle 10 mg
      가격 검색...
      가격을 검색할 수 없습니다
      Minimum Quantity needs to be mulitiple of
      Maximum Quantity is
      가격 문의 추가 정보
      ()이 할인됨
       
      —
      가격 문의
      		 —
      Description
      OverviewA cell-permeable, non-toxic, conformationally restricted pyrimidinecarboxamide compound that acts as a potent, reversible T-cell specific inhibitor of both AP-1 and NF-κB transcriptional activation (IC50 = 50 nM). Reduces DNA binding activity of NF-κB and downregulates NF-κB driven cytokine gene expression. Displays only trivial inhibitory effect against cytokine induction in a variety of other cells. Exhibits anti-inflammatory activity in a murine model of collagen-induced arthritis (~ 10 mg/kg/d, i.p.) and suppresses the expansion of AH-130 Yoshida ascites hepatoma in rats (~ 5 mg/kg/d, i.p.).

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number531535
      Brand Family Calbiochem®
      Synonyms2-Chloro-4-(trifluoromethyl)pyrimidine-5-N-(3ʹ,5ʹ-bis(trifluoromethyl)phenyl)-carboxamide, N-(3,5-bis(Trifluoromethyl)phenyl)-2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxamide, Activator Protein-1 Activation Inhibitor; AP-1 Activation Inhibitor, NF-κB Activation Inhibitor XI, SP-100030, Nuclear Factor-κB Activation Inhibitor XI
      References
      ReferencesYe, N., et al. 2014. J. Med. Chem. 57, 6930.
      Moore-Carrasco, R., et al. 2009. Anticancer Res. 29, 1315.
      Huang, T.J., et al. 2001. Br. J. Pharmacol. 134, 1029.
      Gerlag, D.M., et al. 2000. J. Immunol. 165,1652.
      Sullivan, R.W., et al. 1998. J. Med. Chem. 41, 413.
      Goldman, M.E., et al. 1996. Transplant. Proc. 28, 3106.
      Product Information
      CAS number154563-54-9
      FormOff-white solid
      Hill FormulaC₁₄H₅ClF₉N₃O
      Chemical formulaC₁₄H₅ClF₉N₃O
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetAP-1 and NF-κB
      Purity≥95% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      카탈로그 번호 GTIN
      5.31535.0001 04055977260359

      Documentation

      AP-1/NF-κB Dual Inhibitor, SP100030 - CAS 154563-54-9 - Calbiochem MSDS

      타이틀

      물질안전보건자료(MSDS) 

      References

      참고문헌 보기
      Ye, N., et al. 2014. J. Med. Chem. 57, 6930.
      Moore-Carrasco, R., et al. 2009. Anticancer Res. 29, 1315.
      Huang, T.J., et al. 2001. Br. J. Pharmacol. 134, 1029.
      Gerlag, D.M., et al. 2000. J. Immunol. 165,1652.
      Sullivan, R.W., et al. 1998. J. Med. Chem. 41, 413.
      Goldman, M.E., et al. 1996. Transplant. Proc. 28, 3106.

      Brochure

      Title
      NPI Flyer- Epigenetics and Nuclear Function Feature
      New Products - Antibodies, Small Molecule, Inhibitors

      Technical Info

      Title
      White Paper: Further considerations of antibody validation and usage.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision12-September-2014 JSW
      Synonyms2-Chloro-4-(trifluoromethyl)pyrimidine-5-N-(3ʹ,5ʹ-bis(trifluoromethyl)phenyl)-carboxamide, N-(3,5-bis(Trifluoromethyl)phenyl)-2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxamide, Activator Protein-1 Activation Inhibitor; AP-1 Activation Inhibitor, NF-κB Activation Inhibitor XI, SP-100030, Nuclear Factor-κB Activation Inhibitor XI
      DescriptionA cell-permeable, conformationally restricted pyrimidinecarboxamide compound that is reported to inhibit against the activation of AP-1- & NF-κB-, but not &beta-actin-, mediated transcriptions (IC50 = 50 nM in Jurkat-based reporter assays; 0.5 h drug pretreatment prior to 5 h stimulation with 1 µg/mL PHA/526511 & 50 ng/mL PMA/500582 & 524400) and target genes expressions, including IL-2, IL-8, TNF-α, in 6 T cell cultures (by >85% at 3 µM), while exhibiting little inhibitory potency against cytokine inductions in 10 non-T cell cultures (by <5% at 10 µM), including endothelial, epithelial, fibroblast, monocytic, and osteoblast cultures. Intraperitoneal injection is shown to display in vivo anti-inflammatory efficacy in a murine model of collagen-induced arthritis (10 mg/kg/d) and a rodent model of Ova-induced asthma response (20 mg/kg/d). Dual AP-1 & NF-κB inhibition via daily SP100030 subcutaneous injection is also reported to suppress AH-130 Yoshida ascites hepatoma tumor expansion in rats in vivo (5 mg/kg/d).
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number154563-54-9
      Chemical formulaC₁₄H₅ClF₉N₃O
      Purity≥95% by HPLC
      SolubilityDMSO (100 mg/ml). Use only fresh DMSO for reconstitution.
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.
      Toxicity Standard Handling
      ReferencesYe, N., et al. 2014. J. Med. Chem. 57, 6930.
      Moore-Carrasco, R., et al. 2009. Anticancer Res. 29, 1315.
      Huang, T.J., et al. 2001. Br. J. Pharmacol. 134, 1029.
      Gerlag, D.M., et al. 2000. J. Immunol. 165,1652.
      Sullivan, R.W., et al. 1998. J. Med. Chem. 41, 413.
      Goldman, M.E., et al. 1996. Transplant. Proc. 28, 3106.