| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
- Heme Oxygenase-1 (HO-1, inducible isoform)[2][1]
- IC50 for HO-1 enzymatic activity: 1.9 ± 0.2 μmol/L (determined using rat spleen extracts)[2]
- Heme Oxygenase-2 (HO-2, constitutive isoform)[2]
- IC50 for HO-2 enzymatic activity: >100 μmol/L (determined using rat brain extracts), indicating high selectivity for HO-1[2]
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|---|---|
| ln Vitro |
- Inhibition of HO-1 Activity: In PC3M prostate cancer cells, treatment with 10 μmol/L OB-24 resulted in a 62% decrease in HO-1 activity, whereas 5 nmol/L Taxol had no inhibitory effect but rather slightly (non-significantly) induced HO-1 activity.[1]
- Inhibition of Oxidative Stress: Treatment of PC3M cells with OB-24 (10 μmol/L) led to an approximately 86% decrease in protein carbonylation (from 3.614 to 0.494 (nmol/L)/mg protein) and a 26% decrease in intracellular ROS levels.[1] - Inhibition of Signaling Pathways: OB-24 (5-10 μmol/L) treatment in PC3M cells reduced EGF-stimulated phosphorylation (activation) of the MAPK pathway kinases ERK and p38, but did not significantly affect JNK or AKT phosphorylation.[1] - Anti-proliferative Activity: OB-24 demonstrated broad-spectrum anti-tumor activity against a panel of human cancer cell lines, including PC-3 prostate carcinoma, SKMEL-24 melanoma, HCT-116 colorectal carcinoma, and OVCAR-3 ovarian carcinoma models.[3] |
| ln Vivo |
- Subcutaneous Xenograft Model: In mice bearing subcutaneous PC3M tumors, OB-24 administered i.p. at doses of 10, 30, and 60 mg/kg (on days 1, 3, 5 per cycle for 4 cycles) produced a dose-dependent inhibition of tumor growth. OB-24 at 30 mg/kg showed therapeutic activity similar to that of 10 mg/kg Taxol using the same schedule.[1]
- Synergistic Effect in Combination: The combination of OB-24 (30 mg/kg) with Taxol (10 mg/kg) (same dosing schedule) resulted in >90% reduction in PC3M subcutaneous tumor growth. Isobologram analysis confirmed a combination index (CI) value of 0.74 (P ≤ 0.01), indicating synergy.[1] - Orthotopic Model (Anti-metastatic Activity): PC3M cells implanted orthotopically into the mouse prostate. OB-24 (10 or 30 mg/kg), alone or in combination with Taxol (10 mg/kg), was administered i.v. (on days 1, 3, 5 per cycle for 4 cycles). OB-24 alone significantly inhibited primary tumor growth and the formation of lymph node and lung metastases. More pronounced therapeutic effects were observed when combined with Taxol.[1] - Broad-spectrum Anti-tumor Activity: Anti-tumor activity of OB-24 was observed in various mouse tumor models, including PC-3 prostate, SKMEL-24 melanoma, HCT-116 colorectal, and OVCAR-3 ovarian carcinoma models. OB-24-treated tumors exhibited a significant reduction in vascularization.[3] |
| Enzyme Assay |
- HO Activity Assay: HO activity was determined in rat spleen (HO-1 source) and brain (HO-2 source) microsomal fractions. Reaction mixtures (150 μL) containing 100 mM phosphate buffer (pH 7.4), 50 μM methemalbumin, 1 mg/mL protein, and OB-24 at concentrations ranging from 0.1 to 100 μM were pre-incubated for 10 min at 37°C. Reactions were initiated by adding NADPH to a final concentration of 1 mM and incubated for an additional 15 min at 37°C. Reactions were stopped by instant freezing on dry ice, and CO formation was monitored by gas chromatography. Data were plotted as non-linear regression (sigmoidal dose-response) curves, and IC50 values were calculated.[2]
|
| Cell Assay |
- Cell Proliferation/Viability Assay: Exponentially growing PC3M cells (1×10^3) were seeded in 96-well plates. Eighteen hours later, cells were treated continuously with OB-24. Cell survival was evaluated 96 hours later using the MTT metabolic assay.[1]
- Western Blot Analysis: To investigate signaling pathway changes following HO-1 silencing or inhibition, serum-starved control and HO-1 shRNA-expressing PC3M cells were stimulated with 5 ng/mL EGF. Cell extracts were prepared and immunoblotted using antibodies specific for phosphorylated ERK, p38, JNK, or AKT. Antibodies recognizing total and non-phosphorylated ERK, p38, JNK, and AKT were used as internal controls.[1] - Measurement of Reactive Oxygen Species (ROS): Intracellular ROS levels were determined using the H2-DCF-DA reagent. Results, in arbitrary fluorescence units (AFU), were expressed as the ratio [AFU in treated cells / AFU in control cells] × 100. Cell fluorescence was also confirmed using a flow cytometer. Data are presented as the ratio of mean fluorescence intensity (MFI) for 10,000 cells to MFI for 10,000 control cells.[1] - Measurement of Protein Carbonylation: Quantification of protein carbonyl content was investigated by ELISA.[1] - Cell Invasion Assay: Cell invasion assay was performed using 8-μm porous chambers coated with Matrigel. HO-1 shRNA or control PC3M cells were seeded into the upper chamber, and a chemoattractant was placed in the lower chamber. After incubation, non-invading cells on the upper side of the membrane were removed with a cotton swab. Invaded cells on the lower side were stained with crystal violet and counted under a microscope.[1] |
| Animal Protocol |
- Subcutaneous Xenograft Model (i.p. administration): PC3M cells were implanted subcutaneously into mice (strain not specified, likely nude or SCID based on context). Treatment commenced when tumors reached approximately 100 mm³. OB-24 was dissolved in an appropriate vehicle and administered intraperitoneally at doses of 10, 30, or 60 mg/kg on days 1, 3, and 5 per cycle for a total of four cycles. Taxol was administered i.p. at 10 mg/kg as a positive control or in combination using the same schedule. Tumor size and body weight were measured weekly.[1]
- Orthotopic Xenograft Model (i.v. administration): 1×10^6 PC3M cells in 50 μL Hank's Buffered Salt Solution were implanted into the prostate of male Scid mice through a lower midline incision. One week after implantation (palpable tumors), mice were randomized and treatment was initiated. OB-24 was administered intravenously at 10 or 30 mg/kg, and Taxol was administered intravenously at 10 mg/kg. Dosing schedule was on days 1, 3, and 5 per cycle for a total of four cycles. Control group received vehicle alone. At study termination, animals were sacrificed, prostate tumors were isolated and weighed, and lymph node and lung metastatic nodules were counted under a stereomicroscope.[1] |
| Toxicity/Toxicokinetics |
- Tolerability in Mice: OB-24 was well tolerated by mice at multiple doses up to 100 mg/kg when administered via both intraperitoneal and intravenous routes.[3]
- Body Weight Effect: No body weight loss was observed in in vivo anti-tumor studies using OB-24 at doses from 10 to 60 mg/kg i.p.[1]
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| References |
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| Additional Infomation |
- Mechanism of Action: OB-24 is a selective inhibitor of HO-1. By inhibiting HO-1 activity, it reduces intracellular oxidative stress and ROS levels, leading to suppression of MAPK signaling pathways (particularly ERK and p38), ultimately inhibiting cancer cell proliferation, survival, and invasion.[1]
- Indications: Research suggests OB-24 has potential for treating hormone-refractory prostate cancer (HRPCA) and may also be effective against other cancers, including melanoma, colorectal cancer, and ovarian cancer.[3][1]
- Synergy: OB-24 exhibits synergistic anti-tumor effects when combined with the chemotherapeutic drug Taxol, suggesting its potential use in combination therapy to overcome chemoresistance or enhance efficacy.[1]
- Chemical Structure: The chemical name of OB-24 is 2-[2-(4-bromophenyl)ethyl]-2-[(1H-imidazol-1-yl)methyl]-1,3-dioxolane hydrochloride, with a molecular weight of 373.67.[1]
|
| Molecular Formula |
C15H17BRN2O2
|
|---|---|
| Molecular Weight |
337.211683034897
|
| Exact Mass |
336.0473
|
| Elemental Analysis |
C, 53.43; H, 5.08; Br, 23.70; N, 8.31; O, 9.49
|
| CAS # |
940061-39-2
|
| Related CAS # |
OB-24 HCl;939825-12-4
|
| PubChem CID |
44178077
|
| Appearance |
Typically exists as solids at room temperature
|
| LogP |
2.4
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
20
|
| Complexity |
302
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
BrC1C=CC(=CC=1)CCC1(CN2C=NC=C2)OCCO1
|
| InChi Key |
AKRPSFVFWQTUDK-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C15H17BrN2O2/c16-14-3-1-13(2-4-14)5-6-15(19-9-10-20-15)11-18-8-7-17-12-18/h1-4,7-8,12H,5-6,9-11H2
|
| Chemical Name |
1-[[2-[2-(4-bromophenyl)ethyl]-1,3-dioxolan-2-yl]methyl]imidazole
|
| Synonyms |
OB-24 free base; OB-24; OB24; BPC2VWH3XM; 1-((2-(2-(4-bromophenyl)ethyl)-1,3-dioxolan-2-yl)methyl)-1H-imidazole; 1-((2-(4-Bromophenethyl)-1,3-dioxolan-2-yl)methyl)-1H-imidazole;
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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 | 2.9655 mL | 14.8276 mL | 29.6551 mL | |
| 5 mM | 0.5931 mL | 2.9655 mL | 5.9310 mL | |
| 10 mM | 0.2966 mL | 1.4828 mL | 2.9655 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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