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532310 | c-Myc Inhibitor IV, KJ-Pyr-9 - Calbiochem

532310
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₂H₁₅N₃O₄

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.32310.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable, blood-brain barrier permeant, bioavailable trisubstituted pyridine compound that inhibits c-Myc transcriptional activity. Shown to directly bind to both the monomeric c-Myc (Kd = 6.5 nM) and to c-Myc-Max heterodimer (Kd = 13.4 nM) with high affinity and disrupt c-Myc-Max interaction. Displays a very weak affinity towards Max-Max homodimer (Kd > 1 µM). Also interferes with Max homodimerization, albeit to a lesser extent than c-Myc-Max heterodimerization. Shown to inhibit the c-Myc-driven proliferation of NCI-H460, MDA-MB-231, and SUM-159PT and several other cancer cell lines (IC50 = 5-10 µM). Also diminishes the proliferation of Burkitt lymphoma cell lines expressing high levels of c-Myc (IC50 = 2.5 µM). Suppresses the growth of MDA-MB-231 cells in a xenografted nude mice model (10 mg/kg, i.p., q.d.).

          Please note that the molecular weight for this compound is batch-specific due to variable water content.
          Catalogue Number532310
          Brand Family Calbiochem®
          Synonyms4-(2-(Furan-2-yl)-6-(4-nitrophenyl)pyridin-4-yl)benzamide, KJPyr9, Krohnke Pyridine-9
          References
          ReferencesHart, J.R., et al. 2014. Proc. Natl. Acad. Sci. USA. 111, 12556.
          Product Information
          FormBrown powder
          Hill FormulaC₂₂H₁₅N₃O₄
          Chemical formulaC₂₂H₁₅N₃O₄
          Applications
          Biological Information
          Primary TargetMyc homodimer
          Secondary targetMyc-Max
          Purity≥97% 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 (-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

          References

          Reference overview
          Hart, J.R., et al. 2014. Proc. Natl. Acad. Sci. USA. 111, 12556.

          Brochure

          Title
          New Products Flyer, Volume 2, 2015, Immunology Feature (EMD)

          Technical Info

          Title
          White Paper: Further considerations of antibody validation and usage. (EMD)
          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.

          Revision27-January-2015 JSW
          Synonyms4-(2-(Furan-2-yl)-6-(4-nitrophenyl)pyridin-4-yl)benzamide, KJPyr9, Krohnke Pyridine-9
          DescriptionA cell-permeable, trisubstituted pyridine compound that displays Myc-selective affinity (Kd = 6.5 nM/Myc homodimer, 13.4 nM/Myc-Max dimer, >1.0 µM/Max homodimer) and is 4-times more potent against Myc-Max than Max-Max in DNA-binding assays. Effectively prevents focal microtumors formation following N-Myc, c-Myc, as well as ATG- or CAG-c-Myc transformation of cultured chick embryo fibroblasts/CEF (>99.9% inhibition at 10 µM in ATG-c-Myc-transformed cultures), while exhibiting much reduced or little potency against cultures transformed by v-Src (no inhibition up to 20 µM), v-Jun or PI 3-K H1047R (45.5% inhibition at 10 µM). Selectively inhibits Myc-dependent proliferation of human & avian cultures (Effective conc. 25 to 50 µM; IC50 1 to 10 µM), while exhibiting little potency against Myc-independent growths of human skin fibroblasts, non-transformed, v-jun-transformed, or methylcholanthrene-transformed quail embryo fibroblasts even at a high concentration of 50 µM. Reported to suppress MDA-MB-231-derived tumor expansion in mice (10 mg/kg/d i.p.) in vivo with a concomitant upregulation of N-Myc downregulated gene 1/NDRG1 protein level in tumor tissue. Pharmacokinetics studies reveal good blood-brain barrier permeability in mice ([Drug] = 3.5 µM/plasma & 12.4 µM/brain 4 h post single 10 mg/kg i.p. dosage) and a plasma half-life of 1.84 h in rats following a single i.v. dose of 1 mg/kg.
          FormBrown powder
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₂H₁₅N₃O₄
          Purity≥97% by HPLC
          SolubilityDMSO (50 mg/ml). Use only fresh DMSO for reconstitution.
          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
          ReferencesHart, J.R., et al. 2014. Proc. Natl. Acad. Sci. USA. 111, 12556.