| 名称 | 193 D7 |
| 描述 | 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. |
| 体外活性 | 方法： 采用 HTRF 实验与体外去甲基化实验，检测 193 D7 对 JMJD1C 的作用。
结果： 193 D7 可抑制 JMJD1C 与 H3K9me2 肽底物的结合（IC₅₀ = 1.47 μM），并抑制 JMJD1C 对 H3K9me2 的去甲基化活性（IC₅₀ = 0.59 μM）[1]。 |
| 体内活性 | 方法：在荷瘤 C57BL/6 小鼠模型中，腹腔注射193 D7 (10–25 mg/kg)，每日一次，连续 2 周；或口服 25 mg/kg，每日一次，连续 12 天，小鼠分别接种 MCA205 纤维肉瘤、MCA205、B16、LLC 及 EL4 细胞。
结果：193 D7 在上述荷瘤小鼠中呈现剂量依赖性的抗肿瘤效果 [1]。 |
| 存储条件 | 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. |
| 溶解度 | DMSO : 8 mg/mL (25.21 mM), Sonication is recommended.
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| 相关产品 | Pulrodemstat HCl | TFMB-(R)-2-HG | Zavondemstat | Procaine | FY-21 | Procaine hydrochloride | Phenelzine sulfate | GSK-J4 | Eicosapentaenoic Acid | LSD1-IN-24 | Daminozide | AS8351 |
