A TDO inhibitor
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LM-10

Item No. 36291

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-fluoro-3-[(1E)-2-(2H-tetrazol-5-yl)ethenyl]-1H-indole
CAS Number
1316695-35-8
Molecular Formula
C11H8FN5
Formula Weight
229.2
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 10 mg/ml
λmax
226, 328 nm
SMILES
FC1=CC=C2C(/C=C/C3=NN=NN3)=CNC2=C1
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+
InChi Key
JDBSZVDIUIRSDG-DAFODLJHSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    5 mg

    $68

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    10 mg

    $87

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    25 mg

    $200

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    50 mg

    $366

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    Cayman Chemical
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    Product Description

    LM-10 is an inhibitor of tryptophan 2,3-dioxygenase (TDO; IC50 = 2 µM).1 It is selective for TDO over indoleamine 2,3-dioxygenase (IDO), monoamine oxidase A (MAO-A), and MAO-B, as well as a panel of various receptors and transporters, at 10 µM. LM-10 (1 mg/ml in the drinking water) reverses tumoral immune resistance in a TDO-overexpressing P815B mastocytoma syngeneic model using mice immunized with the P815 antigen P1A.2 Oral administration of LM-10 (50 mg/kg) prevents decreases in the number of dopaminergic neurons and increases in microglial cell volume, a marker of neuroinflammation, in the substantia nigra and inhibits decreases in intestinal transit in a mouse model of Parkinson’s disease induced by rotenone (Item No. 13995).3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Dolušić, E., Larrieu, P., Moineaux, L., et al. Tryptophan 2,3-dioxygenase (TDO) inhibitors. 3-(2-(Pyridyl)ethenyl)indoles as potential anticancer immunomodulators. J. Med. Chem. 54(15), 5320-5334 (2011).

    2. Pilotte, L., Larrieu, P., Stroobant, V., et al. Reversal of tumoral immune resistance by inhibition of tryptophan 2,3-dioxygenase. Proc. Natl. Acad. Sci. USA 109(7), 2497-2502 (2012).

    3. Perez-Pardo, P., Grobben, Y., Willemsen-Seegers, N., et al. Pharmacological validation of TDO as a target for Parkinson’s disease. FEBS J. 288(14), 4311-4331 (2021).