| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
IC50: 7.68 nM (PD-1/PD-L1 interaction)[1]
BMSpep-57 hydrochloride specifically targets PD-L1, a surface protein expressed on many cancer cells. By binding to PD-L1 with high affinity (Kd of 19 nM as measured by MST), it prevents PD-L1 from engaging with its receptor PD-1 on T cells. This blockade releases the "brakes" on the immune system, allowing for enhanced T cell proliferation, cytokine production, and cytotoxic activity against tumor cells. This makes it a valuable tool for studying PD-1/PD-L1 blockade. |
|---|---|
| ln Vitro |
BMSpep-57 suppresses PD-1/PD-L1 binding up to 98.1% at 300 nM in an ELISA competition experiment. Additionally, it exhibits an IC50 of 7.68 nM for concentration-dependent inhibition of PD-1/PD-L1 binding[1]. When BMSpep-57 is added to SEB-stimulated peripheral blood mononuclear cells at doses of 1 µM and 500 nM, it causes elevated levels of IL-2[1]. At the several tested concentrations, BMSpep-57 (0.2-10 μM; 24 hours) does not have any effect on the viability of Jurkat, CHO, and HepG2 cells[1].
In vitro, BMSpep-57 hydrochloride binds to PD-L1 with Kds of 19 nM and 19.88 nM in MST and SPR assays, respectively. It potently inhibits the PD-1/PD-L1 interaction with an IC50 of 7.68 nM. This is a macrocyclic peptide inhibitor that facilitates T cell function, as demonstrated by an increase in interleukin-2 (IL-2) production in peripheral blood mononuclear cells (PBMCs) in co-culture assays. |
| ln Vivo |
Detailed in vivo efficacy data for BMSpep-57 hydrochloride are not extensively reported in standard product literature, as the compound is primarily used as a research tool for in vitro immune checkpoint studies. As a macrocyclic peptide, its in vivo activity would be influenced by factors such as proteolytic stability and bioavailability. In vivo studies using mouse tumor models would be required to evaluate its therapeutic potential and in vivo efficacy.
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| Enzyme Assay |
Non-cellular binding affinity of BMSpep-57 to PD-L1 is typically measured using Surface Plasmon Resonance (SPR) and Microscale Thermophoresis (MST). In an SPR assay, recombinant PD-L1 protein is immobilized on a sensor chip, and varying concentrations of the peptide are flowed over the surface to calculate the kinetic rate constants (ka, kd) and the equilibrium dissociation constant (KD). MST measures the directed movement of molecules in a temperature gradient to quantify binding affinity.
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| Cell Assay |
A functional cellular assay involves co-culturing human PBMCs or purified T cells with PD-L1 expressing cancer cells. Cells are treated with varying concentrations of BMSpep-57 hydrochloride. After incubation, T cell activation is assessed by measuring IL-2 and IFN-gamma cytokine levels in the supernatant using ELISA. Cancer cell death can be assessed by flow cytometry or by measuring released lactate dehydrogenase (LDH) as a marker of cytotoxicity.
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| Animal Protocol |
Detailed in vivo animal experimental protocols for BMSpep-57 hydrochloride are not standardly described in the literature. Its application is primarily as a research tool for in vitro and ex vivo studies. For a hypothetical in vivo experiment, a xenograft mouse model of human cancer could be used, and BMSpep-57 hydrochloride administered intravenously or intratumorally to assess tumor growth inhibition.
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| ADME/Pharmacokinetics |
Dedicated pharmacokinetic studies for BMSpep-57 hydrochloride are not available in standard literature. As a macrocyclic peptide, its bioavailability is likely low due to poor membrane permeability and susceptibility to proteases. Optimized for research use, its drug-like properties such as oral bioavailability, half-life, and clearance would need to be characterized for therapeutic development.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for BMSpep-57 hydrochloride are not provided in standard product literature. As a research-use compound, standard safety assessments for acute toxicity, genotoxicity, and organ-specific toxicity are not typically described. For laboratory use, standard chemical safety precautions for handling peptides should be followed. No adverse events or toxicities have been reported for the compound in in vitro studies.
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| References | |
| Additional Infomation |
BMSpep-57 hydrochloride is a macrocyclic peptide with the sequence {mercaptoacetic acid}-FANPHLSWSW-{norleucine}-{norleucine}-RCG, containing a sulfide bridge between mercaptoacetic acid and Cys15. It has a molecular weight of 1904.63 Da. The compound is stored at -20degC or -80degC and should be handled to avoid freeze/thaw cycles. This product is intended for research purposes only and is not for human use.
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| Molecular Formula |
C89H127CLN24O19S
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|---|---|
| Molecular Weight |
1904.63
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| Related CAS # |
BMSpep-57;1629655-80-6
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| Appearance |
White to off-white 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: 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) |
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
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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 | 0.5250 mL | 2.6252 mL | 5.2504 mL | |
| 5 mM | 0.1050 mL | 0.5250 mL | 1.0501 mL | |
| 10 mM | 0.0525 mL | 0.2625 mL | 0.5250 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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