EGR240 (ERG240)是一种具有口服活性的支链氨基酸转氨酶1（BCAT1）选择性抑制剂（IC₅₀=0.1-1nM）。
Cas No.:1415683-79-2
Sample solution is provided at 25 µL, 10mM.
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EGR240 (ERG240) is an orally active, selective inhibitor of branched-chain amino acid transaminase 1 (BCAT1) with an IC₅₀ of 0.1–1nM[1-2]. EGR240 is suitable for research in cancer, rheumatoid arthritis, and bone diseases[3-4].
In vitro, THP-1 macrophages were pretreated with EGR240 (20μM) for 3 hours, followed by LPS (200ng/mL) and Nigericin (10μM) to induce pyroptosis. EGR240 significantly suppressed BCAT1-mediated NF-κB signaling activation and reduced the secretion of key pyroptosis-related proteins, GSDMD-NT and IL-1β[5]. Ovarian cancer persistent cells (OVCAR8-Persister and A2780-Persister) were treated with EGR240 (60μM) for 24 hours. EGR240 did not significantly affect cell viability, and EGR240 combination with paclitaxel did not enhance paclitaxel cytotoxicity[6].
In vivo, collagen-induced arthritis mice were orally administered EGR240 (720–1000mg/kg). EGR240 significantly alleviated arthritis severity, reducing joint inflammation, pannus formation, cartilage degradation, and bone erosion[7]. db/db diabetic retinopathy mice received intravitreal injections of EGR240 (100–200μM; 1μL) for 2 or 4 weeks. EGR240 significantly downregulated retinal inflammatory gene mRNA expression, such as Gfap and Il6, and reduced retinal vascular leakage[8].
References:
[1] Papathanassiu, et al. Methods for treatment of cancer, inflammatory autoimmune disorders and bone diseases using branched-chain amino acid aminotransferase-1 (BCAT1) inhibitors. Patent. WO2012173987.
[2] Angana A.H, Jozefina Dzanan, Ali, et al. Aging promotes lung cancer metastasis through epigenetic ATF4 induction. bioRxiv 2024.07.03.601209.
[3] Chen L, Shi Y, Xiao D, et al. NR4A1 deficiency promotes carotid plaque vulnerability by activating integrated stress response via targeting Bcat1. Cell Mol Life Sci. 2025 Feb 22;82(1):91.
[4] Yuan Z, Li M, Tang Z. BCAT1 promotes cell proliferation, migration, and invasion via the PI3K-Akt signaling pathway in oral squamous cell carcinoma. Oral Dis. 2025 Feb;31(2):364-375.
[5] Feng J, Zhang H, Zhu M, et al. CHI3L1 promotes macrophage pyroptosis in ulcerative colitis via the BCAT1/NF-κB axis. Life Sci. 2026 Jan 1;384:124108.
[6] Lin H, Wang L, Chen H, et al. Mitochondrial fatty acid oxidation as the target for blocking therapy-resistance and inhibiting tumor recurrence: The proof-of-principle model demonstrated for ovarian cancer cells. J Adv Res. 2026 Jan;79:571-585.
[7] Papathanassiu AE, Ko JH, Imprialou M, et al. BCAT1 controls metabolic reprogramming in activated human macrophages and is associated with inflammatory diseases. Nat Commun. 2017 Jul 12;8:16040.
[8] Wang J, Yin Z, Yang J, et al. BCAT1 Activation Reprograms Branched-Chain Amino Acid Metabolism and Epigenetically Promotes Inflammation in Diabetic Retinopathy. Invest Ophthalmol Vis Sci. 2025 Jun 2;66(6):59.
EGR240 (ERG240)是一种具有口服活性的支链氨基酸转氨酶1（BCAT1）选择性抑制剂（IC₅₀=0.1-1nM）[1-2]。EGR240可用于癌症、类风湿性关节炎及骨病的相关研究[3-4]。
在体外，EGR240（20μM）预处理THP-1巨噬细胞3小时，随后在LPS（200ng/mL）和Nigericin（10μM）诱导的焦亡模型中，EGR240显著抑制BCAT1介导的NF-κB信号通路活化，并降低焦亡关键蛋白GSDMD-NT和IL-1β的分泌[5]。EGR240（60μM）处理卵巢癌耐受细胞（OVCAR8-Persister和A2780-Persister）24小时，EGR240未显著影响细胞存活率。EGR240联合紫杉醇处理后未增强紫杉醇的细胞毒性[6]。
在体内，EGR240（720–1000mg/kg）口服给药处理胶原诱导关节炎小鼠，EGR240显著减轻关节炎严重程度，减少关节炎症、血管翳形成、软骨降解和骨侵蚀[7]。EGR240（100–200μM；1μL）玻璃体内注射处理db/db糖尿病视网膜病变小鼠2周或4周。EGR240显著降低视网膜中Gfap和Il6等炎症基因mRNA表达，并减轻视网膜血管渗漏[8]。
| Cell experiment [1]: | |
Cell lines | THP-1 macrophages (human monocytic cell line) |
Preparation Method | THP-1 cells were differentiated into macrophages using PMA (50ng/mL) for 48 hours, followed by priming with LPS (200ng/mL, 4 hours) and Nigericin (10μM, 30 minutes) to induce pyroptosis. Cells were pretreated with EGR240 (20μM) for 3 hours prior to LPS/Nigericin stimulation. |
Reaction Conditions | 20µM; 3-hour pretreatment. |
Applications | EGR240 significantly suppressed BCAT1-mediated NF-κB activation, reduced phosphorylation of p65, and attenuated pyroptosis execution by decreasing cleavage of GSDMD and caspase-1. EGR240 also inhibited IL-1β and TNF-α secretion in cell supernatants and preserved cell membrane integrity by reducing pyroptosis-associated pore formation. |
| Animal experiment [2]: | |
Animal models | db/db diabetic mice (C57BL/6J background) and WT mice. |
Preparation Method | Mice received intravitreal injections of EGR240 (100μM or 200μM; 1μL) under anesthesia with ketamine (80mg/kg) and xylazine (4mg/kg). Injections were administered weekly for 2 or 4 weeks. Retinal tissues and plasma were collected for analysis. |
Dosage form | 100–200μM of 1μL; intravitreal injection; weekly for 2–4 weeks. |
Applications | EGR240 significantly reduced retinal inflammatory gene expression (Gfap and Il6) and attenuated vascular leakage in diabetic retinas. EGR240 suppressed BCAT1-mediated metabolic reprogramming and epigenetic activation of inflammation by restoring α-KG levels, thereby mitigating diabetic retinopathy progression. |
References: | |
| Cas No. | 1415683-79-2 | SDF | Download SDF |
| 别名 | ERG240 | ||
| 分子式 | C7H11NaO3 | 分子量 | 166.15 |
| 溶解度 | DMSO : 100 mg/mL (601.87 mM; Need ultrasonic) | 储存条件 | 4°C, away from moisture and light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 6.0187 mL | 30.0933 mL | 60.1866 mL |
| 5 mM | 1.2037 mL | 6.0187 mL | 12.0373 mL |
| 10 mM | 601.9 μL | 3.0093 mL | 6.0187 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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