TLR2-IN-C29
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MedKoo CAT#: 562353

CAS#: 363600-92-4

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.

Chemical Structure

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TLR2-IN-C29
CAS# 363600-92-4
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 562353
Name: TLR2-IN-C29
CAS#: 363600-92-4
Chemical Formula: C16H15NO4
Exact Mass: 285.10
Molecular Weight: 285.290
Elemental Analysis: C, 67.36; H, 5.30; N, 4.91; O, 22.43

Price and Availability

Size Price Availability Quantity
5mg USD 110 Ready to ship
10mg USD 190 Ready to ship
25mg USD 350 Ready to ship
50mg USD 550 Ready to ship
100mg USD 950 Ready to ship
200mg USD 1650 Ready to ship
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Synonym: TLR2-IN-C29; TLR2 IN C29; TLR2INC29; TLR2-inhibitor-C29; TLR2 inhibitor-C29; TLR2 inhibitor C29;

IUPAC/Chemical Name: 3-[[(2-Hydroxy-3-methoxyphenyl)methylene]amino]-2-methyl-benzoic acid

InChi Key: WTGMGRFVBFDHGQ-RQZCQDPDSA-N

InChi Code: 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+

SMILES Code: O=C(O)C1=CC=CC(/N=C/C2=CC=CC(OC)=C2O)=C1C

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: 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.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

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.
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/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMF 10.0 35.05
DMSO 32.7 114.50
Ethanol 3.3 11.39
PBS (pH 7.2) 0.3 1.05

Preparing Stock Solutions

The following data is based on the product molecular weight 285.29 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Mistry P, Laird MH, Schwarz RS, Greene S, Dyson T, Snyder GA, Xiao TS, Chauhan J, Fletcher S, Toshchakov VY, MacKerell AD Jr, Vogel SN. Inhibition of TLR2 signaling by small molecule inhibitors targeting a pocket within the TLR2 TIR domain. Proc Natl Acad Sci U S A. 2015 Apr 28;112(17):5455-60. doi: 10.1073/pnas.1422576112. Epub 2015 Apr 13. PMID: 25870276; PMCID: PMC4418912.
In vitro protocol: 1. Mistry P, Laird MH, Schwarz RS, Greene S, Dyson T, Snyder GA, Xiao TS, Chauhan J, Fletcher S, Toshchakov VY, MacKerell AD Jr, Vogel SN. Inhibition of TLR2 signaling by small molecule inhibitors targeting a pocket within the TLR2 TIR domain. Proc Natl Acad Sci U S A. 2015 Apr 28;112(17):5455-60. doi: 10.1073/pnas.1422576112. Epub 2015 Apr 13. PMID: 25870276; PMCID: PMC4418912.
In vivo protocol: 1. Mistry P, Laird MH, Schwarz RS, Greene S, Dyson T, Snyder GA, Xiao TS, Chauhan J, Fletcher S, Toshchakov VY, MacKerell AD Jr, Vogel SN. Inhibition of TLR2 signaling by small molecule inhibitors targeting a pocket within the TLR2 TIR domain. Proc Natl Acad Sci U S A. 2015 Apr 28;112(17):5455-60. doi: 10.1073/pnas.1422576112. Epub 2015 Apr 13. PMID: 25870276; PMCID: PMC4418912.

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1: Mistry P, Laird MH, Schwarz RS, Greene S, Dyson T, Snyder GA, Xiao TS, Chauhan J, Fletcher S, Toshchakov VY, MacKerell AD Jr, Vogel SN. Inhibition of TLR2 signaling by small molecule inhibitors targeting a pocket within the TLR2 TIR domain. Proc Natl Acad Sci U S A. 2015 Apr 28;112(17):5455-60. doi: 10.1073/pnas.1422576112. Epub 2015 Apr 13. PubMed PMID: 25870276; PubMed Central PMCID: PMC4418912.