| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| Other Sizes |
| Targets |
IC50: 14 nM (PTEN)[1]
BpV(HOpic) targets PTEN, a critical negative regulator of the PI3K/AKT signaling pathway. By inhibiting PTEN, the compound prevents the dephosphorylation of phosphatidylinositol (3,4,5)-trisphosphate (PIP3), allowing for sustained PI3K/AKT signaling. This activation of the PI3K/AKT pathway has various downstream effects, including enhanced cell survival and proliferation. It also inhibits other PTPs, but its selectivity for PTEN is a key feature. |
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| ln Vitro |
BpV(HOpic) (1 μM) therapy boosted cell division and decreased the rate of apoptosis in MG63 cells treated with cisplatin [3]. Bpv(HOpic) (1 μM) stimulated C2C12 myoblast migration, interacted with PI3K/AKT, and was linked to the MAPK/ERK signaling pathway activation [4]. Like in humans and rodents, BpV(HOpic (1 μM; 48 hours) stimulates the start of follicle growth and development in pigs [5]. Neural axonal development is enhanced by nanocarrier-BpV(HOpic) [2].
In vitro, BpV(HOpic) is a potent inhibitor of PTEN with an IC50 of 14 nM. It exhibits significant selectivity for PTEN over other phosphatases, with IC50s for PTP-β and PTP-1B being about 350- and 1800-fold higher, respectively. This high potency and selectivity make it a valuable tool for studying PTEN function and PI3K/AKT signaling in various cell types. It is often used to mimic the effects of PTEN loss. |
| ln Vivo |
After reperfusion, BpV(HOpic (0.05 mg/kg; ip) ameliorates liver ischemia/reperfusion (I/R) injury in vivo[6]. Mice exposed to BpV (HOpic (200 μg/kg; ip) Injury (IRI) experience worsening renal dysfunction and increased tubular damage[7].
In vivo, BpV(HOpic) has been shown to have insulin-mimetic effects and may protect the myocardium from ischemia-reperfusion injury by enhancing PI3K/Akt signaling. Nanocarrier formulations of BpV(HOpic) have demonstrated neuroprotective activity. However, PTEN inhibition with this compound has also been associated with enhanced tubular cell apoptosis in kidneys with ischemia-reperfusion injury, linked to excessive caspase-3 activation and increased neutrophil and macrophage infiltration. |
| Enzyme Assay |
Cell-free assays for BpV(HOpic) typically involve measuring its inhibitory activity against PTEN using biochemical phosphatase assays. The IC50 value of 14 nM is determined by measuring the dephosphorylation of a synthetic substrate, such as 3-O-methylfluorescein phosphate (OMFP), in the presence of varying concentrations of the inhibitor. Selectivity is assessed by comparing the compound's potency against a panel of other phosphatases, such as PTP-β and PTP-1B.
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| Cell Assay |
In vitro cellular assays are conducted to evaluate the functional activity of BpV(HOpic) in cells. Cells are treated with the compound, and the activation of the PI3K/AKT pathway is measured by assessing the phosphorylation of AKT (pAKT) and its downstream effectors. PTEN inhibition is confirmed by measuring the levels of PIP3 or by assessing the activity of PTEN in cell lysates. These assays are used to study the role of PTEN in various cellular processes.
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| Animal Protocol |
Animal/Disease Models: Male Wistar rats are subjected to partial hepatic ischemia[6]
Doses: 0.05 mg/kg Route of Administration: Ip injections at the start of reperfusion Experimental Results: Ameliorated reoxygenation injury and reproduced the hepatoprotective effects obtained by adenosine A2A receptor stimulation. Animal/Disease Models: Male C57BL/6 mice (8-12 weeks old; 20-30 g ) are subjected to renal ischemia[7] Doses: 200 μg/ kg Route of Administration: Ip injections 1 h before ischemia and then administers every 6 h after ischemia for 24 hr Experimental Results: Raised the level of serum creatinine and blood serum urea nitrogen. In vivo animal experiments typically involve models of ischemia-reperfusion injury, diabetes, or neurodegeneration. Animals are administered BpV(HOpic), and the effects on PI3K/AKT signaling are assessed in target tissues. Markers of apoptosis, inflammation, and tissue damage are measured to evaluate the compound's therapeutic potential and toxicity. The compound's neuroprotective effects have been studied using nanocarrier formulations. |
| ADME/Pharmacokinetics |
The pharmacokinetic properties of BpV(HOpic) are characteristic of a small molecule inhibitor. Its molecular weight is 347.24. It is soluble in water at 69 mg/mL but is insoluble in DMSO and ethanol. Its bioavailability and half-life are not widely published, but its use in various in vivo models suggests adequate systemic exposure. The compound is stable and can be stored at -20°C for long-term use.
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| Toxicity/Toxicokinetics |
The toxicity profile of BpV(HOpic) is context-dependent. While it has shown neuroprotective and cardioprotective effects, PTEN inhibition has also been associated with enhanced tubular cell apoptosis in kidneys with ischemia-reperfusion injury, accompanied by increased inflammation. The compound is intended for research use only and is not for human consumption. Its safety profile in vivo requires careful evaluation in specific disease models.
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| References | |
| Additional Infomation |
BpV(HOpic) is a widely used research tool for studying the PTEN/PI3K/AKT signaling pathway. Its high potency and selectivity for PTEN make it a valuable compound for investigating the role of this tumor suppressor in cancer, metabolism, and neurodegeneration. It has been cited in numerous publications across various fields, including immunology, stem cell research, and cancer biology. It is not a therapeutic agent.
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| Molecular Formula |
C6H4K2NO8V
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|---|---|
| Molecular Weight |
347.24
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| Exact Mass |
346.865
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| CAS # |
722494-26-0
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| Appearance |
Light yellow to yellow solid powder
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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: (1). This product is not stable in solution, please use freshly prepared working solution for optimal results. (2). Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
H2O: 50 mg/mL (143.99 mM)
DMSO: 2.89 mg/mL (8.32 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 | 2.8799 mL | 14.3993 mL | 28.7985 mL | |
| 5 mM | 0.5760 mL | 2.8799 mL | 5.7597 mL | |
| 10 mM | 0.2880 mL | 1.4399 mL | 2.8799 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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