IDO-IN-2

Catalog No.S7111 Batch:S711104

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Technical Data

Formula

C18H22N2O
Molecular Weight 282.38 CAS No. 1402836-58-1
Solubility (25°C)* In vitro DMSO 56 mg/mL (198.31 mM)
Ethanol 30 mg/mL (106.23 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description IDO-IN-2 (RG 6078, NLG-919 analogue, GDC-0919 analogue) is a a potent IDO1 inhibitor with IC50 of 38 nM.
Targets
IDO1 [2]
(Cell-free assay)
38 nM
In vitro

IDO-IN-2 (NLG-919 analogue, Compound 24) contains an imidazoleisoindole core and exhibits potent inhibitory activity to IDO1 with the IC50 value of 38 nM. IDO-IN-2 inhibits IDO activity with EC50 of 61 nM in HeLa cellular assay. The binding mode of IDO-IN-2 to IDO1 is experimentally available and shows a direct coordinative interaction to the sixth coordination site of ferric heme.[2] IDO-IN-2 (Compound 7) has been used as reference compound in other studies to validate high-throughput screening assay for IDO1 inhibition and develop immunostimulatory nanomicellar carrier.[1]

Protocol (from reference)

References

  • https://pubmed.ncbi.nlm.nih.gov/29031064/
  • https://pubmed.ncbi.nlm.nih.gov/26642377/

Customer Product Validation

<p>Inhibitor sensitivity of tryptophan 2,3-dioxygenase (TDO) in N-formylkynurenine (NFK) Green assay. Dose-response curves of INCB024360, S7111, and NTRC 0820-0 with IC50 values 67 nM and 75 nM, respectively.</p>

Data from [ J Biomol Screen , 2014 , 10.1177/1087057114536616 ]

B) Cellular IC50 value (μM) of VIS351 (14, filled circle) and NLG919 (as reference inhibitor, open circle) obtained from a dose–response curve. P1.IDO1 cells were exposed to six times 3-fold serial dilutions of NLG919 (concentrations ranging from 0.0003 to 0.1 μM) and eight times 3-fold serial dilutions of VIS351 (concentrations ranging from 0.03 to 90 μM). Results are the mean ± SD of the Kyn fold change (Kyn FC) of three independent experiments, each performed in triplicate. D) Enzymatic IC50 of VIS351 (14, filled circle) and NLG919 (open circle) are determined on recombinant human IDO1, using seven times 10-fold dilutions of the molecules, starting from 2 mM. Kyn FC values are represented as the mean ± SD of three independent experiments, each performed in triplicate.

Data from [ , , Biochem Pharmacol, 2018, 158:286-297 ]

Selleck's IDO-IN-2 Has Been Cited by 15 Publications

Bispecific prodrug nanoparticles circumventing multiple immune resistance mechanisms for promoting cancer immunotherapy [ Acta Pharm Sin B, 2022, 12(6):2695-2709] PubMed: 35755274
Cascade Immune Activation of Self-Delivery Biomedicine for Photodynamic Immunotherapy Against Metastatic Tumor [ Small, 2022, e2205694] PubMed: 36366925
Downregulation of miR-26 promotes invasion and metastasis via targeting interleukin-22 in cutaneous T-cell lymphoma [ Int J Mol Sci, 2022, 23(7)3981] PubMed: 35409342
Tryptophan potentiates CD8+ T cells against cancer cells by TRIP12 tryptophanylation and surface PD-1 downregulation [ J Immunother Cancer, 2021, 9(7)e002840] PubMed: 34326168
Decreased IDO1 Dependent Tryptophan Metabolism in Aged Lung during Influenza [ Eur Respir J, 2020, 2000443] PubMed: 33243840
Ultrasound-Driven Biomimetic Nanosystem Suppresses Tumor Growth and Metastasis through Sonodynamic Therapy, CO Therapy, and Indoleamine 2,3-Dioxygenase Inhibition [ ACS Nano, 2020, 14(7):8985-8999] PubMed: 32662971
Discovery of Novel Indoleamine 2,3-Dioxygenase 1 (IDO1) and Histone Deacetylase 1 (HDAC1) Dual Inhibitors Derived from the Natural Product Saprorthoquinone [ Molecules, 2020, 25(19)E4494] PubMed: 33007982
Discovery of Novel Indoleamine 2,3-Dioxygenase 1 (IDO1) and Histone Deacetylase 1 (HDAC1) Dual Inhibitors Derived from the Natural Product Saprorthoquinone [ Molecules, 2020, 25(19)E4494] PubMed: 33007982
Inhibition of the BET family reduces its new target gene IDO1 expression and the production of L-kynurenine. [ Cell Death Dis, 2019, 10(8):557] PubMed: 31324754
Displacement Induced Off-On Fluorescent Biosensor Targeting IDO1 Activity in Live Cells. [ Anal Chem, 2019, 91(23):14943-14950] PubMed: 31714063

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.