532583 TLR1/TLR2 Agonist II, CU-T12-9 - Calbiochem

532583
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₇H₁₃F₃N₄O₂

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      Glass bottle 10 mg
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      Description
      OverviewA diphenyl substituted imidazole based compound that directly and selectively targets TLR1/2 and induces their dimerization and activates TLR1 & 2 signaling leading to NF-κB and AP-1 activation (KD = 182 and 478 nM, respectively; EC50 = 52.9 nM for TLR2 in HEK-Blue cells over-expressing hTLR2). Does not affect the dimerization of TLR2/TLR6 and exhibits poor affinity towards TLR3, TLR4, TLR5, TLR7 and TLR8. Shown to compete with Pam3CSK4 (Cat. No. 506350; Ki = 45.4 nM) for binding to TLR1/2 interface and enhance heterodimerization. Up-regulates the expression of TLR1, TLR2, TNFα, IL-10, and iNOS in RAW 264.7 macrophages in a time-dependent manner. Shown to be non-toxic up to 100 µM concentration.

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number532583
      Brand Family Calbiochem®
      SynonymsN-Methyl-4-nitro-2-(4-(4-(trifluoromethyl)phenyl)-1H-imidazol-1-yl)aniline, CUT129
      References
      ReferencesCheng, K., et al. 2014. Manuscript in preparation.
      Product Information
      FormYellow powder
      Hill FormulaC₁₇H₁₃F₃N₄O₂
      Chemical formulaC₁₇H₁₃F₃N₄O₂
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetTLR1/TLR2
      Purity≥98% by HPLC
      Physicochemical Information
      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 (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      TLR1/TLR2 Agonist II, CU-T12-9 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Cheng, K., et al. 2014. Manuscript in preparation.

      Brochure

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

      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.

      Revision19-December-2014 JSW
      SynonymsN-Methyl-4-nitro-2-(4-(4-(trifluoromethyl)phenyl)-1H-imidazol-1-yl)aniline, CUT129
      DescriptionA non-cytotoxic (up to 100 µM) diphenyl-substituted imidazole compound that exhibits high affinity toward both TLR1 & TLR2 (KD = 182 nM & 478 nM, respectively) and induces TLR1/2 heterodimerization, effectively completing against Pam3CSK4 (Cat. No. 506350) for TLR1/2 binding (Ki = 45.4 nM; [Pam3] = 20 mg/mL; [TLR1/2] = 80 nM). Shown to potently induce secreted embryonic alkaline phosphatase (SEAP) production from human TLR2-, but not TLR3-, 4-, 5-, 7-, 8-, transfected HEK293 (EC50 = 52.9 nM) in an NF-κB inhibitor Triptolide-(Cat. No. 645900) blockable manner via selective TLR1/2, but not TLR2/6, heterodimer activation. Reported to induce comparable NF-κB-dependent reporter transcription as 100 ng/mL Pam3CSK4 when administered to human macrophage U937 cultures at 5 µM concentration (24 h) and effectively trigger NO production in both murine Raw 264.7 and primary rat macrophage cultures (ECmax = 1.2 & 0.4 µM, respectively; 24 h), blockable by TLR1/2 antagonist CU-CPT22 (Cat. No. 614305), but not TLR4 antagonist TAK-242 (Cat. No. 614316 & 508336). Likewise, both CU-T12-9 and Pam3CSK4 (1 µM & 50 ng/mL, respectively) are demonstrated to induce similar time-dependent induction of TLR1, TLR2, TNF-α, iNOS, IL-10 mRNA in Raw 264.7 cells.
      FormYellow powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₇H₁₃F₃N₄O₂
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesCheng, K., et al. 2014. Manuscript in preparation.