| Size | Price | |
|---|---|---|
| Other Sizes |
| Targets |
STAT5
HODHBt targets the interaction between STAT5 and SUMO (small ubiquitin-like modifier). STAT5 is a transcription factor that plays a critical role in cytokine signaling, cell proliferation, and survival. By inhibiting the SUMOylation of phosphorylated STAT5, HODHBt modulates STAT5 activity and downstream signaling. This leads to enhanced IL-15 signal intensity and increased NK cell function. HODHBt is a valuable tool for studying STAT5 signaling, NK cell biology, and immunotherapy. |
|---|---|
| ln Vitro |
HODHBt (100 μM; 24 and 48 hours, respectively) phosphorylates STAT in NK cells through IL-15 and improves the cytotoxic profile of NK cells[1]. HODHBt (100 μM; 24 h) increases NK cells' cytotoxicity (100 ng/mL) mediated by IL-15 against HIV-positive cells (K562 cells)[1]. The cytotoxicity of NK cells against cancer cell lines (A2780 and U877; OCILy1 and OCILy10) is enhanced by HODHBt (100 μM; 24 h) when combined with IL-15 (100 ng/mL, 6 h)[1]. Human CIML NK cells generated in vitro exhibit an improved memory response upon recall when exposed to HODHBt (100 μM; 7 d)[1].
In vitro, HODHBt inhibits STAT5-SUMO interaction and suppresses SUMOylation of phosphorylated STAT5. It enhances IL-15 signal intensity, significantly increases the cytotoxic phenotype and function of natural killer (NK) cells, and increases the generation of cytokine-induced memory-like natural killer cells (CIML NK). These in vitro activities support its potential for enhancing NK cell-based immunotherapies. |
| ln Vivo |
In vivo data for HODHBt is limited in publicly available sources. As a STAT5-SUMO interaction inhibitor that enhances NK cell function, the compound has potential applications in animal models of HIV infection and cancer. By enhancing IL-15 signaling and NK cell activity, HODHBt could improve immune responses against tumors and viral infections. However, specific published in vivo efficacy studies are not widely reported. HODHBt is primarily used as a research tool.
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| Enzyme Assay |
The in vitro STAT5-SUMO interaction assay for HODHBt uses purified STAT5 and SUMO proteins. The interaction is measured using co-immunoprecipitation, pull-down assays, or fluorescence-based methods. SUMOylation of phosphorylated STAT5 is assessed by Western blotting using anti-SUMO antibodies. NK cell function assays are performed using primary NK cells or NK cell lines, with cytotoxicity measured against target cells.
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| Cell Assay |
Cellular assays for HODHBt are conducted in NK cells and other immune cells. Cells are treated with varying concentrations of HODHBt. STAT5 SUMOylation is assessed by Western blotting. IL-15 signaling is evaluated by measuring STAT5 phosphorylation and downstream gene expression. NK cell cytotoxicity is measured using standard chromium release or flow cytometry-based assays. Generation of CIML NK cells is assessed by flow cytometry for memory-like markers.
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| Animal Protocol |
In vivo studies for HODHBt would typically involve mouse models of HIV infection or cancer. The compound would be administered via intraperitoneal or intravenous routes at doses determined by pharmacokinetic studies. Efficacy would be assessed by measuring tumor growth inhibition, viral loads, and NK cell function. However, specific published in vivo protocols for HODHBt are not available in the current literature. The compound is currently used as a research tool for studying NK cell biology and immunotherapy.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for HODHBt is not extensively reported in publicly available sources. The compound has a molecular weight of 163.13 g/mol and a molecular formula of C7H5N3O2. It is soluble in DMSO at ≥200 mg/mL. Storage conditions: powder at -20°C for 3 years or 4°C for 2 years. As a small molecule STAT5 inhibitor, it is expected to have moderate bioavailability. Detailed PK parameters such as half-life are not available in the current literature.
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| Toxicity/Toxicokinetics |
Toxicity data for HODHBt is limited in publicly available sources. As with all research compounds, HODHBt is intended for research use only and not for human therapeutic applications. Standard in vitro cytotoxicity assays and in vivo tolerability studies would be required for a complete toxicity assessment. The compound's mechanism of enhancing NK cell function suggests potential immune-related effects that would need to be evaluated.
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| References | |
| Additional Infomation |
HODHBt (HOOBt) is a STAT5-SUMO protein-protein interaction inhibitor that suppresses SUMOylation of phosphorylated STAT5. It enhances IL-15 signal intensity, increases NK cell cytotoxicity, and increases generation of CIML NK cells. HODHBt can be used for research on HIV infection and cancer. It has a molecular formula of C7H5N3O2 and a molecular weight of 163.13 g/mol. HODHBt is a valuable tool for studying STAT5 signaling, NK cell biology, and immunotherapy.
|
| Molecular Formula |
C7H5N3O2
|
|---|---|
| Molecular Weight |
163.13
|
| Exact Mass |
163.038
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| CAS # |
28230-32-2
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| PubChem CID |
73026
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| Appearance |
White to off-white solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
348.7±25.0 °C at 760 mmHg
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| Melting Point |
184-189°C
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| Flash Point |
164.7±23.2 °C
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| Vapour Pressure |
0.0±0.8 mmHg at 25°C
|
| Index of Refraction |
1.739
|
| LogP |
0.43
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| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
0
|
| Heavy Atom Count |
12
|
| Complexity |
229
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C1N(O)N=NC2=CC=CC=C12
|
| InChi Key |
HJBLUNHMOKFZQX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C7H5N3O2/c11-7-5-3-1-2-4-6(5)8-9-10(7)12/h1-4,12H
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| Chemical Name |
3-hydroxy-1,2,3-benzotriazin-4-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 |
| 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 : 500 mg/mL (3065.04 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 4.17 mg/mL (25.56 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (41.7 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 4.17 mg/mL (25.56 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (41.7 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 6.1301 mL | 30.6504 mL | 61.3008 mL | |
| 5 mM | 1.2260 mL | 6.1301 mL | 12.2602 mL | |
| 10 mM | 0.6130 mL | 3.0650 mL | 6.1301 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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