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MedKoo Cat#: 562353 | Name: TLR2-IN-C29
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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

TLR2-IN-C29
TLR2-IN-C29
CAS#363600-92-4

Theoretical Analysis

MedKoo Cat#: 562353

Name: TLR2-IN-C29

CAS#: 363600-92-4

Chemical Formula: C16H15NO4

Exact Mass: 285.1001

Molecular Weight: 285.29

Elemental Analysis: C, 67.36; H, 5.30; N, 4.91; O, 22.43

Price and Availability

Size Price Availability Quantity
5mg USD 150.00 Ready to ship
10mg USD 250.00 Ready to ship
25mg USD 450.00 Ready to ship
50mg USD 750.00 Ready to ship
100mg USD 1,250.00 Ready to ship
200mg USD 2,050.00 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/
Solvent mg/mL 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
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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.
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.