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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
HSF1A is a cell-permeable and small-molecule activator of heat shock transcription factor 1 (HSF1). HSF1A inhibits TRiC activity without interfering with ATP hydrolysis, binds TRiC subunits both in vivo and in vitro, and shields cells from stress-induced apoptosis. Human HSF1 is activated upon genetic inactivation or depletion of the TRiC complex, and the in vitro direct interaction between purified TRiC and HSF1 is inhibited by HSF1A. Heat shock transcription factor 1 (HSF1) is a transcription factor that has been conserved throughout evolution and shields cells from stress and apoptosis caused by misfolded proteins.
| Targets |
HSF1
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
Using biotin-binding buffer (20 mM HEPES, 5 mM MgCl2, 1 mM EDTA, 100 mM KCl, 0.03% NP-40), in addition to protease inhibitors and 1% Trition-X100, protein extracts are produced from mammalian, yeast, and E. Coli cultures. After 4 hours at 4°C incubation with 100 μM HSF1A-Biotin, about 0.5 mg of protein extract is captured with NeutrAvidin Agarose Resin, corresponding with HSF1A-Biotin'sassociatedproteins. Once the proteins have been cleaned in the biotin binding buffer, they are resolved on a 4–20% SDS-PAGE and immunoblotted using 50 μL of biotin elution buffer (100 mM Tris, 150 mM NaCl, 0.1 mM EDTA, and 2 mM D-biotin). In order to analyze purified TRiC and Hsp70, 5 nM protein is incubated for 4 hours at 4°C in biotin-binding buffer+0.5% Triton X-100 with 100 μM biotin or 100 μM HSF1A-Biotin. The protein is then captured using NeutrAvidin Rinse. Different concentrations of Tcp1 (0.5 μM, 1 mM, 2 mM, 3 mM, and 4 mM) in 25 mM Hepes pH 7.5, 150 mM NaCl are incubated with 0.5 μM Biotin or HSF1A-Biotin for 4 hours at 4°C and then captured using NeutrAvidin Resin for NiNTA purified yeast Tcp1[1].
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| Cell Assay |
PC12 cells seeded into a 96-well plate (5 ×104 cells/well) are treated with increasing concentrations of HSF1A (2, 4, 8, and 12 μM) for 15 hours. Following this, httQ74-GFP expression is stimulated by incubating the cells for 5 days in the presence of 1 µg/mL Doxycycline. The XTT viability assay is used to evaluate cell viability[2].
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| Animal Protocol |
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| References |
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| Molecular Formula |
C21H19N3O2S2
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| Molecular Weight |
409.52
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| Exact Mass |
409.092
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| Elemental Analysis |
C, 61.59; H, 4.68; N, 10.26; O, 7.81; S, 15.66
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| CAS # |
1196723-93-9
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| Related CAS # |
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| PubChem CID |
44472508
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| Appearance |
White to off-white solid powder
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| LogP |
6.117
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
28
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| Complexity |
595
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1(S(NC2N(C3=CC=CC=C3)N=C(C3SC=CC=3)C=2)(=O)=O)=CC=C(CC)C=C1
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| InChi Key |
KJTITGSAONQVPY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H19N3O2S2/c1-2-16-10-12-18(13-11-16)28(25,26)23-21-15-19(20-9-6-14-27-20)22-24(21)17-7-4-3-5-8-17/h3-15,23H,2H2,1H3
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| Chemical Name |
4-ethyl-N-(2-phenyl-5-thiophen-2-ylpyrazol-3-yl)benzenesulfonamide
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.10 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 (6.10 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 (6.10 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 | 2.4419 mL | 12.2094 mL | 24.4188 mL | |
| 5 mM | 0.4884 mL | 2.4419 mL | 4.8838 mL | |
| 10 mM | 0.2442 mL | 1.2209 mL | 2.4419 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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