| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
HMBPP targets the intracellular domain of butyrophilin 3A1 (BTN3A1), a type I transmembrane protein expressed on most human cells. Upon binding to the BTN3A1 intracellular domain, HMBPP triggers a conformational change that facilitates its interaction with the BTN3A2/BTN2A1 complex. This assembly is required for the efficient activation of Vgamma9/Vdelta2 T cells, which occurs through T cell receptor (TCR)-dependent recognition of the phosphoantigen-BTN3A complex.
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| ln Vitro |
HMBPP is a potent activator of Vgamma9/Vdelta2 T cells, stimulating their proliferation, cytokine production (including IFN-gamma, TNF-alpha, and perforin), and cytotoxic activity against a broad range of cancer cells, including colon cancer and glioblastoma. At 100 nM, it induces strong upregulation of activation marker CD69 on gammadelta T cells and enhances their cytotoxicity. HMBPP also acts as a potent phagostimulant for female *Anopheles* mosquitoes, the primary vectors of malaria.
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| ln Vivo |
In murine models of colon cancer, treatment with HMBPP-activated Vgamma9/Vdelta2 T cells significantly reduced tumor burden and improved survival. In glioblastoma models, HMBPP-stimulated gammadelta T lymphocytes acquired a Th1-like profile and exhibited enhanced cytotoxicity against glioblastoma cells. HMBPP has also been used extensively as a research tool to expand and activate Vgamma9/Vdelta2 T cells *ex vivo* for adoptive cell therapy (ACT) and for vaccine adjuvant studies.
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| Enzyme Assay |
Binding of HMBPP to the BTN3A1 intracellular domain is typically measured by surface plasmon resonance (SPR) using purified recombinant BTN3A1 protein. The compound is also evaluated by its ability to stabilize the BTN3A1/BTN3A2/BTN2A1 complex in cellular lysates using co‑immunoprecipitation (co‑IP) and Western blotting. Binding affinity (KD) and kinetic parameters can be determined through SPR; however, no specific KD values are reported in the search results.
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| Cell Assay |
Human peripheral blood mononuclear cells (PBMCs) or purified Vgamma9/Vdelta2 T cells are seeded in 96‑well plates and treated with HMBPP at concentrations ranging from 0.1 nM to 10 microM for 0-72 h. Activation is assessed by flow cytometry for CD69, CD25, and CD107a expression. Cytotoxicity is measured using a standard ⁵¹Cr-release assay or a non‑radioactive alternative (e.g., lactate dehydrogenase release) against target cancer cells such as Daudi, HeLa, or colon cancer cell lines. Cytokine release (e.g., IFN-gamma, TNF-alpha, granzyme B) is quantified by ELISA.
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| Animal Protocol |
For *ex vivo* activation and expansion, human PBMCs are cultured with HMBPP (100 nM-1 microM) and IL‑2 for 10-14 days. Expanded Vgamma9/Vdelta2 T cells are then adoptively transferred into immunodeficient mice bearing established human tumor xenografts (e.g., colon cancer or glioblastoma). Tumor volume, survival, and intratumoral T cell infiltration are monitored. In *in vivo* activation studies, HMBPP can be administered directly to mice or non‑human primates, although its rapid clearance is a limitation. No detailed protocols are described in the search results.
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| ADME/Pharmacokinetics |
HMBPP (C₅H12O₇P2, MW = 246.09, CAS 396726-03-7) is typically supplied as a lithium salt (e.g., HMBPP lithium) for improved stability and solubility. For storage, the lyophilized powder should be kept at -20 degC or -80 degC, sealed and protected from light. For in vitro use, stock solutions in sterile water or PBS (1-10 mM) can be prepared and stored at -80 degC for up to 6 months; avoid repeated freeze‑thaw cycles. The compound is water‑soluble. No detailed pharmacokinetic parameters are reported.
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| Toxicity/Toxicokinetics |
HMBPP is generally well‑tolerated in cell culture at concentrations up to 10 microM. Its toxicity is primarily related to its potent immune‑stimulatory activity; high doses could potentially induce cytokine release syndrome. As a research‑grade compound, it is not intended for human or veterinary use. Standard laboratory safety precautions for handling biological reagents should be followed. No LD₅0 or formal toxicology studies are available.
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| References |
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| Additional Infomation |
HMBPP is a research‑grade phosphoantigen widely used in gammadelta T cell immunotherapy research. It is the most potent known activator of human Vgamma9/Vdelta2 T cells, discovered in 1999 by Jomaa et al. The compound has been explored for adoptive cell therapy (ACT) against a wide range of cancers, including colon cancer, glioblastoma, and bladder cancer. HMBPP is also used as a vaccine adjuvant and in studies of anti‑malarial immunity. The lithium salt form is the most common commercial preparation. HMBPP is for research use only and has not received regulatory approval.
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| Molecular Formula |
C5H12O8P2
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|---|---|
| Molecular Weight |
262.09
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| Exact Mass |
258.977
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| CAS # |
396726-03-7
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| PubChem CID |
786
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| Appearance |
White to off-white solid powder
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| Density |
1.685±0.06 g/cm3 (20 ºC 760 Torr)
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| LogP |
1.465
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
15
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| Complexity |
317
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(=CCOP(=O)(O)OP(=O)(O)O)CO
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| InChi Key |
MDSIZRKJVDMQOQ-UHFFFAOYSA-K
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| InChi Code |
InChI=1S/C5H12O8P2/c1-5(4-6)2-3-12-15(10,11)13-14(7,8)9/h2,6H,3-4H2,1H3,(H,10,11)(H2,7,8,9)/p-3
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| Chemical Name |
[(4-hydroxy-3-methylbut-2-enoxy)-oxidophosphoryl] phosphate
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| Synonyms |
(E)-4-Hydroxy-3-methyl-but-2-enyl diphosphate
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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 |
| 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 | 3.8155 mL | 19.0774 mL | 38.1548 mL | |
| 5 mM | 0.7631 mL | 3.8155 mL | 7.6310 mL | |
| 10 mM | 0.3815 mL | 1.9077 mL | 3.8155 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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