| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
The primary target of HyT36 is not a specific protein but rather any HaloTag-fused protein or fusion protein of interest. The compound serves as a hydrophobic tag that selectively destabilizes and promotes the degradation of fusion proteins. By attaching a hydrophobic tag, HyT36 induces ubiquitination and proteasomal degradation of target proteins, enabling selective protein knockdown. It also promotes the degradation of pseudokinase Her3.
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| ln Vitro |
In HEK293 cells expressing GFP-HaloTag2/Fz4-HaloTag2/GFP-HaloTag7 fusion protein, HyT36 (10 µM; 24 h) decreases the expression of GFP-HaloTag2/Fz4-HaloTag2 [1]. In HEK293 Flp-In cells expressing HA-EGFP-HaloTag2, HyT36 (10 µM; 2 h or 48 h) decreased EGFP expression and increased Hsp70 binding to the HA-EGFP-HaloTag2 fusion protein [3]. In HEK293 Flp-In cells expressing HA-EGFP-HaloTag2, HyT36 (50 nM; 24 h) lowers the amount of EGFP-HaloTag2 [3]. In NIH-3T3 cells expressing HA−HaloTag2−HRasG12V, HyT36 (1 µM; 4 d) decreases the expression of HA−HaloTag2−HRasG12V [
In vitro studies demonstrate that HyT36 promotes the degradation of fusion proteins and pseudokinase Her3 in cell culture systems. As a small-molecule hydrophobic tagging degrader, it induces ubiquitination and proteasomal degradation of target proteins. The compound's activity is dependent on its covalent binding to HaloTag-fused proteins, which triggers misfolding and degradation. |
| ln Vivo |
In vivo activity data for HyT36 are limited, as the compound is primarily used as a research tool in cell-based studies. The compound's ability to promote targeted protein degradation in vivo would depend on the expression of HaloTag-fused proteins in target tissues. Further in vivo studies are needed to characterize its pharmacokinetic and pharmacodynamic properties.
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| Enzyme Assay |
Non-cellular assays for HyT36 typically involve characterizing its chemical properties and its ability to bind to HaloTag protein. Binding affinity can be measured using surface plasmon resonance or isothermal titration calorimetry. The compound's stability and reactivity with HaloTag are assessed using biochemical methods. These cell-free systems allow for characterization of the compound's interactions with its target.
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| Cell Assay |
Western Blot Analysis[1][3]
Cell Types: HEK293 cells expressing GFP-HaloTag2/Fz4-HaloTag2/HA-EGFP-HaloTag2 or NIH-3T3 cells expressing HA−HaloTag2−HRasG12V. Tested Concentrations: 1 µM or 10 µM. Incubation Duration: 2 h, 24 h or 4 days. Experimental Results: diminished the expression of fusion proteins and increased the binding of Hsp70 and HA-EGFP-HaloTag2 fusion protein. Cellular assays for HyT36 are conducted using cells expressing HaloTag-fused proteins or fusion proteins of interest. Cells are treated with the compound, and the degradation of the target protein is assessed by Western blotting. Proteasome inhibitors such as MG132 are used to confirm that degradation occurs via the ubiquitin-proteasome pathway. Cell viability is assessed to determine cytotoxicity. |
| Animal Protocol |
In vivo animal experiments for HyT36 are limited. The compound may be studied in mouse models expressing HaloTag-fused proteins to assess its ability to induce targeted protein degradation in vivo. The compound is administered via injection, and target protein levels in various tissues are assessed by Western blotting or immunohistochemistry. These studies evaluate the compound's efficacy in a physiological context.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of HyT36 are not well-characterized. The compound has a molecular weight of 442.08 g/mol and is soluble in DMSO. It is typically stored at -20°C for long-term stability. The compound's absorption, distribution, metabolism, and excretion have not been extensively studied. As a small, lipophilic molecule, it may have reasonable membrane permeability and bioavailability.
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| Toxicity/Toxicokinetics |
Toxicological data for HyT36 are limited, as the compound is a research reagent not intended for human use. Standard laboratory safety precautions should be followed when handling the compound. No significant toxicity has been reported at the concentrations used in cell-based studies. The compound is for research use only and should not be administered to humans.
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| References |
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| Additional Infomation |
Other information includes HyT36's role as a low-molecular-weight hydrophobic tag that promotes the degradation of fusion proteins and pseudokinase Her3. It is also known as hydrophobic tag-36. The compound is used in targeted protein degradation research using the HaloTag system. It induces ubiquitination and proteasomal degradation of target proteins by attaching a hydrophobic tag, enabling selective protein knockdown. The compound is available as a research reagent with ≥98% purity.
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| Molecular Formula |
C25H44CLNO3
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|---|---|
| Molecular Weight |
442.0748
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| Exact Mass |
441.3
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| CAS # |
1323151-45-6
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| PubChem CID |
52953469
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| Appearance |
Light yellow to brown ointment
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| LogP |
6.1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
16
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| Heavy Atom Count |
30
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| Complexity |
471
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C[C@H](CCC12CC3CC(C1)CC(C3)C2)C(=O)NCCOCCOCCCCCCCl
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| InChi Key |
FRQCQVUXVOJKTG-AXYUOHRYSA-N
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| InChi Code |
InChI=1S/C25H44ClNO3/c1-20(6-7-25-17-21-14-22(18-25)16-23(15-21)19-25)24(28)27-9-11-30-13-12-29-10-5-3-2-4-8-26/h20-23H,2-19H2,1H3,(H,27,28)/t20-,21?,22?,23?,25?/m1/s1
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| Chemical Name |
(2R)-4-(1-adamantyl)-N-[2-[2-(6-chlorohexoxy)ethoxy]ethyl]-2-methylbutanamide
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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: 100 mg/mL (226.21 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.66 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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: ≥ 2.5 mg/mL (5.66 mM) (saturation unknown) 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. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.66 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2621 mL | 11.3104 mL | 22.6209 mL | |
| 5 mM | 0.4524 mL | 2.2621 mL | 4.5242 mL | |
| 10 mM | 0.2262 mL | 1.1310 mL | 2.2621 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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