| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
INH1 (also called IBT-13131; INH-1; IBT13131) is a potent and cell-permeable Hec1 (High expression in cancer 1) inhibitor with potential anticancer activity. It acts by specifically disrupting the Hec1/Nek2 protein-protein interaction.
| ln Vitro |
When Hec1 was treated with INH1 (25 μM) for 24 hours, the global level of Nek2 protein decreased and Hec1's association with the kinetochore was lessened[1]. In MDA-MB-468 cells, 15 μM in SKBR3 cells, 10.5 μM in T47D cells, 20.5 μM in MDA-MB-361 cells, 15 μM in ZR-75-1 cells, 15 μM in HBL 100 cells, 15.5 μM in MDA-MB-435 cells, 11 μM in HS578T cells, and 41 μM in MCF10A cells, respectively, are the GI50 values for INH1[1]. In the dose-dependent transwell migration assays using MDA-MB-231 cells, INH1 (5k) has an IC50 value of 176 nM. INH1 (5k) significantly lowers cellular f-actin and inhibits fascin from localizing to membrane protrusions that are rich in actin[2]. INH1 causes aberrant cell apoptosis and mitotic processes[3].
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| ln Vivo |
In nude mice using a xenografted breast cancer model, INH1 (50 or 100 mg/kg, ip, every other day/25 cycles) suppresses the formation of tumors[1].
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| Cell Assay |
Cell Cytotoxicity Assay[1]
Cell Types: MCF10A cells. Tested Concentrations: 10 μM. Incubation Duration: 12 days. Experimental Results: Effectively inhibits the proliferation of human breast cancer lines. Western Blot Analysis[1] Cell Types: MCF10A cells. Tested Concentrations: 25 μM. Incubation Duration: 24 h. Experimental Results: Nek2 reduction in INH1-treated cells may be independent of Hec1. |
| Animal Protocol |
Animal/Disease Models: Xenografted nude mice breast cancer model[1].
Doses: 50 or 100 mg/kg. Route of Administration: IP, every other day/25 cycles. Experimental Results: Inhibited tumor growth. |
| References |
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| Molecular Formula |
C18H16N2OS
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|---|---|---|
| Molecular Weight |
308.40
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| Exact Mass |
308.098
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| CAS # |
313553-47-8
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| Related CAS # |
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| PubChem CID |
959043
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Index of Refraction |
1.657
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| LogP |
5.24
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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 |
3
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| Heavy Atom Count |
22
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| Complexity |
383
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JPMOKRWIYQGMJL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H16N2OS/c1-12-8-9-15(13(2)10-12)16-11-22-18(19-16)20-17(21)14-6-4-3-5-7-14/h3-11H,1-2H3,(H,19,20,21)
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| Chemical Name |
N-[4-(2,4-dimethylphenyl)-1,3-thiazol-2-yl]benzamide
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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 (8.11 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 (8.11 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 25.0 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 | 3.2425 mL | 16.2127 mL | 32.4254 mL | |
| 5 mM | 0.6485 mL | 3.2425 mL | 6.4851 mL | |
| 10 mM | 0.3243 mL | 1.6213 mL | 3.2425 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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