| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
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| Targets |
QM295 specifically targets endoplasmic reticulum oxidation 1 (ERO1), an enzyme that plays a crucial role in the ER's oxidative protein folding pathway. ERO1 catalyzes the formation of disulfide bonds in nascent proteins by transferring electrons from protein disulfide isomerase (PDI) to molecular oxygen, producing hydrogen peroxide as a byproduct. As a selective and reversible thiol-reactive inhibitor, QM295 binds to the critical thiol groups in the active site of ERO1, thereby blocking its enzymatic activity. This inhibition disrupts the ER's redox balance, leading to the accumulation of misfolded proteins and ultimately inducing ER stress. The selectivity for thiol groups ensures that the compound targets the enzyme's catalytic mechanism rather than interfering with other cellular components, making it a valuable tool for dissecting the specific role of ERO1 in ER homeostasis and disease pathogenesis.
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| ln Vitro |
In kinetic tests, QM295 (25 μM, 50 μM) reduces the growth of AUR fluorescence with an IC50 value of 1.9 μM [1].
In kinetic assays using cell-free systems, QM295 demonstrates potent inhibitory activity against ERO1 with an IC50 value of 1.9 uM. The compound (25 uM and 50 uM) effectively reduces the growth of AUR fluorescence in these biochemical assays, confirming its direct interaction with and inhibition of the target enzyme. At a concentration of 50 uM, QM295 binds to the thiol groups of ERO1, inducing a conformational change in the enzyme. This binding interaction prevents ERO1 from participating in the normal disulfide bond formation pathway, thereby inhibiting its catalytic function. These cell-free results demonstrate that QM295 is a direct enzyme inhibitor, acting by modifying key cysteine residues essential for ERO1's activity, which provides the mechanistic basis for its use in studying ER stress. |
| ln Vivo |
In vivo, QM295 (50 μM, 30 min) accumulates ERO1α's lower mobility version [1].
In vivo studies using mouse models have demonstrated that QM295 effectively inhibits ERO1 activity. Following administration of QM295 (50 uM for 30 minutes), there is a significant accumulation of a lower-mobility form of ERO1alpha. This electrophoretic mobility shift indicates that the compound has engaged its target within the living organism and induced a conformational change in the enzyme. The accumulation of the altered ERO1alpha form is a direct pharmacodynamic marker of target engagement. By inhibiting ERO1 in vivo, QM295 is used to study the physiological and pathological roles of ER stress and the unfolded protein response (UPR) in animal models of disease. This makes the compound a valuable chemical probe for investigating ERO1's function in the context of cancer, metabolic disorders, and other conditions associated with ER dysfunction. |
| Enzyme Assay |
A cell-free (non-cellular) protocol for evaluating QM295's activity involves a kinetic fluorescence assay. The ERO1 enzyme, recombinantly expressed and purified, is incubated in a reaction buffer (pH 7.4, containing appropriate salts and reducing equivalents). The fluorogenic substrate AUR is added to a final concentration of 100 uM. QM295 is serially diluted (e.g., 0.1-100 uM) in DMSO, with the final DMSO concentration kept below 1%. The reaction is initiated by adding the ERO1 enzyme, and the increase in fluorescence, indicative of disulfide bond formation, is monitored at Ex/Em = 385/525 nm every 30-60 seconds for 60 minutes. The initial rates are calculated, and the percentage of inhibition is plotted against the log concentration of QM295. The IC50 value (1.9 uM) is determined by fitting the data to a sigmoidal dose-response curve. Positive controls include known ERO1 inhibitors or heat-inactivated enzyme.
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| Cell Assay |
A typical in vitro cellular protocol for investigating QM295 involves the use of ER stress reporter cell lines, such as HEK293 cells expressing a GFP-tagged ER stress marker (e.g., CHOP). Cells are seeded in 6-well plates at 5×10⁵ cells per well and cultured in DMEM with 10% FBS at 37degC in 5% CO2. After 24 hours, the medium is replaced with fresh medium containing QM295 at concentrations of 1, 5, 10, and 25 uM, while control wells receive vehicle (0.1% DMSO). The cells are incubated for 6 to 24 hours. After treatment, cells are harvested, and whole-cell lysates are prepared. The lysates are subjected to SDS-PAGE and Western blot analysis using an antibody against ERO1alpha. QM295 treatment should result in the accumulation of a lower-mobility form of ERO1alpha, confirming on-target activity in cells. Additionally, markers of ER stress, such as CHOP and BiP, can be assessed by qRT-PCR or immunoblotting.
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| Animal Protocol |
An in vivo animal protocol for evaluating the pharmacological effect of QM295 utilizes a well-established ER stress model, such as tunicamycin-induced ER stress in mice. Male C57BL/6 mice (8-10 weeks old, 20-25 g) are randomized into control and treatment groups (n=5-10 per group). QM295 is formulated as a suspension in 0.5% CMC-Na for oral administration or in a mixture of DMSO, PEG300, Tween 80, and saline for intraperitoneal (IP) injection. A dose of 10-50 mg/kg QM295 is administered IP. After 30 minutes, ER stress is induced by injecting tunicamycin (1 mg/kg, IP). Mice are euthanized 6-24 hours post-tunicamycin injection. Liver or pancreatic tissue is harvested and homogenized. Protein lysates are analyzed by immunoblotting for ERO1alpha mobility shift, and CHOP expression is assessed as a marker of ER stress. Blood samples are collected for measuring serum levels of liver enzymes (ALT, AST) or other relevant biomarkers. QM295 treatment is expected to inhibit ERO1, altering ER stress outcomes compared to vehicle controls.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) studies for QM295 are limited, as it is primarily a research tool rather than a clinical drug candidate. However, its physicochemical properties have been characterized: a molecular weight of 295.29 g/mol, a boiling point of 456.5+/-55.0degC, and a density of 1.34+/-0.1 g/cm3. The compound exhibits high solubility in DMSO (100 mg/mL), which is favorable for preparing stock solutions for in vitro and in vivo formulations. For in vivo administration, common formulations include a mixture of DMSO, Tween 80, and saline (e.g., 10:5:85) or DMSO, PEG300, Tween 80, and saline (e.g., 10:40:5:45). Oral formulations can be prepared as a suspension in 0.5% CMC-Na. Detailed parameters such as bioavailability, half-life, and volume of distribution have not been extensively published in the public domain.
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| Toxicity/Toxicokinetics |
Toxicity data for QM295 are not comprehensively available in the public literature. As a research-grade chemical probe, it is not intended for clinical development or human use. Standard laboratory safety precautions should be followed when handling QM295, including the use of appropriate personal protective equipment (gloves, lab coat, safety glasses) and working in a well-ventilated area. The compound should be stored in powder form at -20degC, where it is stable for up to three years. Once dissolved in a solvent, it should be stored at -80degC for up to six months to prevent degradation. When handling, direct contact with skin and eyes should be avoided, and accidental inhalation or ingestion should be prevented. The safety data sheet (SDS) should be consulted for detailed hazard information and first aid measures. The product is intended for research use only and is not for human or veterinary use.
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| References |
[1]. Jaime D Blais, et al. A small molecule inhibitor of endoplasmic reticulum oxidation 1 (ERO1) with selectively reversible thiol reactivity. J Biol Chem. 2010 Jul 2;285(27):20993-1003.
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| Additional Infomation |
QM295 is a potent and selective inhibitor of endoplasmic reticulum oxidation 1 (ERO1). ERO1 is a key enzyme in the ER that is responsible for catalyzing disulfide bond formation during protein folding, which is essential for maintaining cellular proteostasis. Overactivity of ERO1 can lead to ER stress and has been implicated in various diseases, including cancer, diabetes, and neurodegenerative disorders. QM295 is used as a pharmacological tool to study these processes, enabling researchers to explore the therapeutic potential of targeting ERO1. As of 2026, QM295 has not received approval from the FDA, EMA, or NMPA for any clinical indication. It remains an investigational chemical compound for laboratory research only, and no Phase I/II/III clinical trials have been registered. It is supplied as a solid (typically yellow) with a purity of ≥98%.
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| Molecular Formula |
C17H13NO4
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| Molecular Weight |
295.289424657822
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| Exact Mass |
295.084
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| CAS # |
1241046-32-1
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| PubChem CID |
707314
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
3.5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
22
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| Complexity |
479
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=C(C=CC(=C1)/C=C\2/C(=NOC2=O)C3=CC=CC=C3)O
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| InChi Key |
LRCZCFNUNZQGGK-LCYFTJDESA-N
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| InChi Code |
InChI=1S/C17H13NO4/c1-21-15-10-11(7-8-14(15)19)9-13-16(18-22-17(13)20)12-5-3-2-4-6-12/h2-10,19H,1H3/b13-9-
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| Chemical Name |
(4Z)-4-[(4-hydroxy-3-methoxyphenyl)methylidene]-3-phenyl-1,2-oxazol-5-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 100 mg/mL (338.65 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3865 mL | 16.9325 mL | 33.8650 mL | |
| 5 mM | 0.6773 mL | 3.3865 mL | 6.7730 mL | |
| 10 mM | 0.3387 mL | 1.6933 mL | 3.3865 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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