TLR2-IN-C29

• CAS: 363600-92-4
• Catalog Number: ACM363600924
• Category: Inhibitors
• Molecular Weight: 285.29
• Molecular Formula: C16H15NO4
• Description: TLR2-IN-C29 is an inhibitor of TLR2/1 and TLR2/6 signaling. It is induced by synthetic and bacterial TLR2 agonists in human HEK-TLR2 and THP-1 cells, but only TLR2/1 signaling in murine macrophages.
• Synonyms: TLR2-IN-C29; TLR2 IN C29; TLR2INC29; TLR2-inhibitor-C29; TLR2 inhibitor-C29; TLR2 inhibitor C29
• IUPAC Name: 3-[[(2-Hydroxy-3-methoxyphenyl)methylene]amino]-2-methyl-benzoic acid
• Canonical SMILES: O=C(O)C1=CC=CC(/N=C/C2=CC=CC(OC)=C2O)=C1C
• InChI: InChI=1S/C16H15NO4/c1-10-12(16(19)20)6-4-7-13(10)17-9-11-5-3-8-14(21-2)15(11)18/h3-9,18H,1-2H3,(H,19,20)/b17-9+
• InChI Key: WTGMGRFVBFDHGQ-RQZCQDPDSA-N
• Solubility: Soluble in DMSO
• Appearance: Solid powder
• Shelf Life: >2 years if stored properly
• Storage: Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
• Biological Target: C29 is a Toll-like receptor 2 (TLR2) inhibitor. C29 blocks hTLR2/1 and hTLR2/6 signaling with IC50s of 19.7 and 37.6 μM, respectively.
• Drug Formulation: This drug may be formulated in DMSO
• Elemental Analysis: C, 67.36; H, 5.30; N, 4.91; O, 22.43
• Exact Mass: 285.1001
• HS Tariff Code: 2934.99.9001
• In Vitro Activity: Compound C29 (Fig. 1A) blocked P3C- and P2C-induced IL-8 mRNA dose-dependently in HEK-TLR2 stable transfectants, although it had no effect on TNF-α-induced signaling or on cytotoxicity (Fig. 1B and Fig. S3). C29 also inhibited P3C- and P2C-induced IL-1β gene expression significantly at both 1 h and 4 h following stimulation (Fig. 1C), as well as both P3C- and P2C-induced NF-κB-luciferase activity in transiently transfected HEK293T cells expressing hTLR2 and an NF-κB-sensitive luciferase reporter construct (Fig. S4). Thus, C29 inhibits both TLR2/1 and TLR2/6 signaling in human cell lines.; Reference: Proc Natl Acad Sci U S A. 2015 Apr 28;112(17):5455-60. https://pubmed.ncbi.nlm.nih.gov/25870276/
• In Vivo Activity: Mice treated twice with C29L before administration of P3C significantly blocked IL-12 p40 and TNF-α liver cytokine mRNA and serum protein (Fig. 4). Importantly, C29L had a significant inhibitory effect at the later time point for IL-12 p40. Collectively, C29L blocks TLR2/1 signaling both in vitro and in vivo.; Reference: Proc Natl Acad Sci U S A. 2015 Apr 28;112(17):5455-60. https://pubmed.ncbi.nlm.nih.gov/25870276/
• Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
• Stock Solution Storage: 0-4 °C for short term (days to weeks), or -20 °C for long term (months).