EGR240 (Synonyms: ERG240) |
Catalog No.GC67742
One-Click Copy Product Info
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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.
Products are for research use only. Not for human use. We do not sell to patients.
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.
| 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 | |
| Synonyms | ERG240 | ||
| Formula | C7H11NaO3 | M.Wt | 166.15 |
| Solubility | DMSO : 100 mg/mL (601.87 mM; Need ultrasonic) | Storage | 4°C, away from moisture and light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)