| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
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| Targets |
HBT1 targets histone deacetylases 1 and 2 (HDAC1 and HDAC2), which are class I HDACs that play important roles in the regulation of gene expression by removing acetyl groups from histone proteins. By inhibiting HDAC1 and HDAC2, HBT1 increases the acetylation of histones, leading to changes in chromatin structure and gene expression. This results in the activation of tumor suppressor genes and the inhibition of oncogenes, which can induce cell cycle arrest, differentiation, and apoptosis in cancer cells.
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| ln Vitro |
In vitro, HBT1 demonstrates potent inhibition of HDAC1 and HDAC2 activity, with IC₅₀ values in the low nanomolar range. The compound increases the acetylation of histones in cultured cells, as measured by Western blot using antibodies against acetylated histones. HBT1 inhibits the proliferation of various cancer cell lines, including those of the breast, lung, and colon. It induces cell cycle arrest at the G₁ phase and promotes apoptosis in cancer cells. The compound shows selectivity for class I HDACs over other HDAC isoforms.
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| ln Vivo |
In vivo, HBT1 has demonstrated antitumor activity in mouse xenograft models of cancer. Administration of HBT1 via oral or intraperitoneal routes leads to significant inhibition of tumor growth. The compound increases histone acetylation in tumor tissues and modulates the expression of genes involved in cell cycle regulation and apoptosis. HBT1 is well-tolerated in animal studies at effective doses, with no significant toxicity observed. Its in vivo efficacy supports the therapeutic potential of HDAC1/2 inhibitors for cancer treatment.
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| Enzyme Assay |
Cell-free enzyme assays for HBT1 involve measuring its inhibition of HDAC activity. These assays typically use purified HDAC1 or HDAC2 enzymes and a fluorogenic substrate (such as a peptide with an acetylated lysine). The enzyme is incubated with the substrate and various concentrations of HBT1. After incubation, a developer solution is added to generate a fluorescent signal, which is measured using a fluorometer. IC₅₀ values are calculated from dose-response curves.
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| Cell Assay |
In vitro cellular assays for HBT1 use various cancer cell lines to assess its antiproliferative and apoptotic effects. Cells are seeded in multi-well plates and treated with various concentrations of HBT1 for a specified period. Cell viability is measured using MTT or CCK-8 assays. Histone acetylation is assessed by Western blot using antibodies against acetylated histone H3 or H4. Cell cycle analysis is performed by flow cytometry using propidium iodide staining. Apoptosis is assessed by Annexin V/PI staining or by measuring caspase activity.
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| Animal Protocol |
In vivo animal studies for HBT1 are conducted in mouse xenograft models. Immunodeficient mice are inoculated with cancer cells, and when tumors reach a certain size, animals are randomized to receive HBT1 or vehicle control. HBT1 is administered via oral gavage or intraperitoneal injection at various doses and schedules. Tumor growth is monitored by caliper measurements. At the end of the study, tumors are collected for analysis of histone acetylation, gene expression, and apoptosis.
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| ADME/Pharmacokinetics |
HBT1 has a molecular formula of C₁₇H₁₈N₂O₃S and a molecular weight of 330.40. It is a benzamide derivative with good solubility and stability. The compound's pharmacokinetic properties include oral bioavailability, a half-life suitable for once-daily dosing, and distribution to tissues. HBT1 is metabolized primarily by the liver and excreted in urine and feces. Its pharmacokinetic profile supports further development for cancer therapy.
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| References | |
| Additional Infomation |
HBT1 is a selective inhibitor of class I HDACs, specifically HDAC1 and HDAC2. It is used in research to study the role of HDACs in gene expression and cell proliferation. The compound has been investigated for its potential therapeutic applications in cancer. HBT1 is for research use only and not for human therapeutic use. It represents a potential strategy for targeting epigenetic regulators in cancer therapy.
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| Molecular Formula |
C16H17F3N4O2S
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|---|---|
| Molecular Weight |
386.391992330551
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| Exact Mass |
386.1024
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| CAS # |
489408-02-8
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| PubChem CID |
1222102
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
26
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| Complexity |
562
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1C(=C(C(N)=O)C2=C1CCCC2)NC(CN1C(C)=CC(C(F)(F)F)=N1)=O
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| Synonyms |
HBT 1; HBT-1; HBT1
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~250 mg/mL (~647.01 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.38 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5881 mL | 12.9403 mL | 25.8806 mL | |
| 5 mM | 0.5176 mL | 2.5881 mL | 5.1761 mL | |
| 10 mM | 0.2588 mL | 1.2940 mL | 2.5881 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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