IDO1/TDO-IN-4

• CAT Number: I043304
• CAS Number: 461424-21-5
• Molecular Formula: C14H10N4
• Molecular Weight: 234.26
• Purity: ≥95%
• Synonyms: 1-(1H-imidazol-5-yl)-9H-pyrido[3,4-b]indole
• InChI: InChI=1S/C14H10N4/c1-2-4-11-9(3-1)10-5-6-16-14(13(10)18-11)12-7-15-8-17-12/h1-8,18H,(H,15,17)
• InChIKey: HUTBKGSJEGKJBG-UHFFFAOYSA-N
• SMILES: C1=CC=C2C(=C1)C3=C(N2)C(=NC=C3)C4=CN=CN4

IDO1/TDO-IN-4 is a potent IDO1/TDO dual inhibitor, with IC50 values of 3.53 μM (IDO1) and 1.15 μM (TDO). IDO1/TDO-IN-4 forms hydrogen bond with IDO1, and π−π stacking interaction with TDO. IDO1/TDO-IN-4 can be used in the research of depression, and depression-induced infectious, metabolic, and autoimmune disorders[1].
IDO1/TDO-IN-4 (compound 28, 0-2 μM, 1 h) inhibits the LPS-induced activation of BV2 microglial cells (determined by morphological changes)[1].
IDO1/TDO-IN-4 (0-2 μM, 1 h) inhibits the generation of pro-inflammatory factors and promotes the expression of IL-10[1].
IDO1/TDO-IN-4 (0-2 μM, 1 h) decreases the expression of IDO1 and prevents the excessive degradation of tryptophan via the kynurenine pathway[1].
IDO1/TDO-IN-4 (compound 28, i.p., 20 mg/kg, at day 1, 2, 3) rescues LPS-induced neuroinflammation and depressive-like behavior in mice[1].
IDO1/TDO-IN-4 (I.p. or i.v., 20 mg/kg) displays high exposure and a high volume of distribution at the steady state in normal mice[1].

Reference

[1]. Yu Zhang, et al. B Discovery of 1-(Hetero)aryl-β-carboline Derivatives as IDO1/TDO Dual Inhibitors with Antidepressant Activity. J Med Chem. 2022 Aug 7.
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