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MedKoo Cat#: 532113 | Name: LM10
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Description:

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

LM10 is a selective tryptophan 2,3-dioxygenase (TDO) inhibitor (IC50 values are 0.62 and 2 μM for human and mouse TDO, respectively). LM10 exhibits selectivity for TDO over IDO, MAO-A, MAO-B, and a panel of receptors and transporters. LM10 reduces growth of TDO-expressing P815 mastocytoma tumors in mice.

Chemical Structure

LM10
LM10
CAS#1316695-35-8

Theoretical Analysis

MedKoo Cat#: 532113

Name: LM10

CAS#: 1316695-35-8

Chemical Formula: C11H8FN5

Exact Mass: 229.0764

Molecular Weight: 229.22

Elemental Analysis: C, 57.64; H, 3.52; F, 8.29; N, 30.55

Price and Availability

Size Price Availability Quantity
10mg USD 250.00 2 Weeks
25mg USD 450.00 2 Weeks
50mg USD 750.00 2 Weeks
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Related CAS #
No Data
Synonym
LM10; LM 10; LM-10.
IUPAC/Chemical Name
6-fluoro-3-[(E)-2-(1H-1,2,3,4-tetrazol-5-yl)ethenyl]-1H-indole
InChi Key
JDBSZVDIUIRSDG-DAFODLJHSA-N
InChi Code
InChI=1S/C11H8FN5/c12-8-2-3-9-7(6-13-10(9)5-8)1-4-11-14-16-17-15-11/h1-6,13H,(H,14,15,16,17)/b4-1+
SMILES Code
FC1=CC2=C(C=C1)C(/C=C/C3=NN=NN3)=CN2
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
Product Data
Product Data
Instruction
View handling instruction
Biological target:
LM10 is a potent inhibitor of tryptophan 2,3-dioxygenase (TDO).
In vitro activity:
This study investigated the signalling mechanisms regulated by LM-10 in human brain endothelial cell line hCMEC/D3 in response to interleukin(IL)-1beta(β) in vitro. LM-10 promoted endothelial proliferation and repair of an endothelial monolayer after scratch injury, and upregulated IL-1β-induced ICAM-1 and VCAM-1 expression. Reference: J Neuroimmunol. 2022 Dec 15;373:577993. https://pubmed.ncbi.nlm.nih.gov/36327619/
In vivo activity:
To determine whether systemic treatment with LM10 was able to promote rejection of TDO-expressing tumors, this study immunized and challenged mice as above and administered LM10 in the drinking water (Fig. 2B). This study observed that systemic treatment of immunized mice with LM10 (160 mg/kg/day) prevented the growth of TDO-expressing P815 tumor cells. This was true for both TDO-transfected clones. Surprisingly, LM10 treatment also promoted better rejection of control clone P815B cl1, which does not express TDO. Reference: Proc Natl Acad Sci U S A. 2012 Feb 14;109(7):2497-502. https://pubmed.ncbi.nlm.nih.gov/22308364/
Solvent mg/mL mM
Solubility
DMF 1.0 4.36
DMSO 32.2 140.61
Ethanol 4.3 18.72
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 229.22 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. Zhao Y, Tao F, Jiang J, Chen L, Du J, Cheng X, He Q, Zhong S, Chen W, Wu X, Ou R, Xu Y, Tang KF. Tryptophan 2, 3‑dioxygenase promotes proliferation, migration and invasion of ovarian cancer cells. Mol Med Rep. 2021 Jun;23(6):445. doi: 10.3892/mmr.2021.12084. Epub 2021 Apr 13. PMID: 33846800; PMCID: PMC8060793. 2. Thurgur H, Penny J, Pinteaux E. Endothelial cell activation by interleukin-1 and extracellular matrix laminin-10 occurs via the YAP signalling pathway. J Neuroimmunol. 2022 Dec 15;373:577993. doi: 10.1016/j.jneuroim.2022.577993. Epub 2022 Oct 28. PMID: 36327619. 3. Pilotte L, Larrieu P, Stroobant V, Colau D, Dolusic E, Frédérick R, De Plaen E, Uyttenhove C, Wouters J, Masereel B, Van den Eynde BJ. Reversal of tumoral immune resistance by inhibition of tryptophan 2,3-dioxygenase. Proc Natl Acad Sci U S A. 2012 Feb 14;109(7):2497-502. doi: 10.1073/pnas.1113873109. Epub 2012 Jan 30. PMID: 22308364; PMCID: PMC3289319.
In vitro protocol:
1. Zhao Y, Tao F, Jiang J, Chen L, Du J, Cheng X, He Q, Zhong S, Chen W, Wu X, Ou R, Xu Y, Tang KF. Tryptophan 2, 3‑dioxygenase promotes proliferation, migration and invasion of ovarian cancer cells. Mol Med Rep. 2021 Jun;23(6):445. doi: 10.3892/mmr.2021.12084. Epub 2021 Apr 13. PMID: 33846800; PMCID: PMC8060793. 2. Thurgur H, Penny J, Pinteaux E. Endothelial cell activation by interleukin-1 and extracellular matrix laminin-10 occurs via the YAP signalling pathway. J Neuroimmunol. 2022 Dec 15;373:577993. doi: 10.1016/j.jneuroim.2022.577993. Epub 2022 Oct 28. PMID: 36327619.
In vivo protocol:
1. Pilotte L, Larrieu P, Stroobant V, Colau D, Dolusic E, Frédérick R, De Plaen E, Uyttenhove C, Wouters J, Masereel B, Van den Eynde BJ. Reversal of tumoral immune resistance by inhibition of tryptophan 2,3-dioxygenase. Proc Natl Acad Sci U S A. 2012 Feb 14;109(7):2497-502. doi: 10.1073/pnas.1113873109. Epub 2012 Jan 30. PMID: 22308364; PMCID: PMC3289319.
1: Lang ZF, Shen JJ, Cai S, Zhang J, He J, Li SP. Expression, characterization, and site-directed mutation of a multiple herbicide-resistant acetohydroxyacid synthase (rAHAS) from Pseudomonas sp. Lm10. Curr Microbiol. 2011 Aug;63(2):145-50. doi: 10.1007/s00284-011-9953-x. PubMed PMID: 21638043.