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Synonyms: JMJD1C-IN-1, 193-D7, 193D7


| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 1 mg | $137 | - | In Stock | |
| 5 mg | $337 | - | In Stock | |
| 10 mg | $490 | - | In Stock | |
| 25 mg | $816 | - | In Stock | |
| 50 mg | $1,130 | - | In Stock | |
| 100 mg | $1,530 | - | In Stock |
| Description | 193 D7 is an orally bioavailable and selective JMJD1C inhibitor with an IC₅₀ of 0.59 μM and a Kd of 1.96 μM. In HTRF assays, it blocks the binding of JMJD1C to the H3K9me2 peptide substrate with an IC₅₀ of 1.47 μM. 193 D7 regulates the fitness of regulatory T cells (Tregs) in the tumor microenvironment via a dual mechanism: it promotes H3K9me2 enrichment to downregulate PD-1 expression and inhibits STAT3 demethylation to enhance STAT3 activation. It exhibits dose-dependent antitumor activity in multiple mouse tumor models, including MCA205 fibrosarcoma, B16-F10 melanoma, LLC lung cancer, Hepa1-6 hepatoma, and CT26 colorectal cancer, and can be used as a tool molecule for selectively targeting intratumoral Tregs in tumor immunity research. |
| Targets & IC50 | JMJD1C:0.59 μM, JMJD1C-H3K9me2:1.47 μM (IC50), JMJD1C:1.96 μM (Kd) |
| In vitro | Methods: The effects of 193 D7 on JMJD1C were determined using HTRF assays and in vitro demethylation assays. Results: 193 D7 inhibited the binding of JMJD1C to the H3K9me2 peptide substrate (IC₅₀ = 1.47 μM) and suppressed the demethylase activity of JMJD1C toward H3K9me2 (IC₅₀ = 0.59 μM) [1]. |
| In vivo | Methods: In tumor-bearing C57BL/6 mouse models, 193 D7 (10–25 mg/kg) was intraperitoneally injected once daily for 2 consecutive weeks, or orally administered at 25 mg/kg once daily for 12 consecutive days. Mice were inoculated with MCA205 fibrosarcoma, MCA205, B16, LLC, and EL4 cells, respectively. Results: 193 D7 exhibited dose-dependent antitumor effects in the above tumor-bearing mice [1]. |
| Synonyms | JMJD1C-IN-1, 193-D7, 193D7 |
| Molecular Weight | 317.36 |
| Formula | C16H15NO4S |
| Cas No. | 861224-48-8 |
| Smiles | O=C(O)CC1C(=O)N2C(SCC2)=C(C(=O)C=3C=CC=CC3)C1 |
| Storage | Keep away from moisture Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 8 mg/mL (25.21 mM), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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