| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| Targets |
Activates transcription factor 4, ATF4[1]
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|---|---|
| ln Vitro |
In HT1080 cells, E235 (1 µM; 2, 4, 8, 16 or 24 h) time-dependently reduces the levels of XBP-1 mRNA [1]. E235 exhibits antiproliferative action on HT1080, RPMI-8226, B16F10, 4T1, HT1080 shNT, and HT1080 shATF4 cells at concentrations of 0.1–10 µM over 4 or 5 days [1]. In AG1522 cells, E235 (0, 1, 5, and 10 µM; 4 h) boosted p53 expression in a dose-dependent way. In AG1522 cells, E235 (1 µM; 2 h) enhances p-Chk2 expression [1]. In AG1522 and HT1080 cells, E235 (0, 1, 5, and 10 µM; 2 h) enhances p-p53 expression [1]. HT1080 cells express more γ-H2AX when exposed to E235 (0, 0.5, 1, 5, and 10 µM; 0.5 h) in a dose-dependent manner [1].
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: HT1080, B16F10 and AG1522 cells. Tested Concentrations: 0, 1, 5 and 10 µM. Incubation Duration: 4 h. Experimental Results: Increased the expression of ATF4 with dose-dependent manner. Western Blot Analysis[1] Cell Types: HT1080 cells. Tested Concentrations: 0, 0.5, 1, 5 or 10 µM. Incubation Duration: 2, 4 or 8 h. Experimental Results: Increased the expression of p-elF2α with time and dose dependent manner. Cell Proliferation Assay [1] Cell Types: HT1080 or RPMI-8226 cells. Tested Concentrations: 1 µM. Incubation Duration: 0, 8, 16 and 24 h. Experimental Results: demonstrated anti-proliferative activity. Cell Viability Assay[1] Cell Types: AG1522 cells. Tested Concentrations: 0, 0.1, 0.5, 1 and 10 µM. Incubation Duration: 4 d. Experimental Results: Inhibited cell viability with dose-dependent manner. Cell Cycle Analysis[1] Cell Types: HT1080 cells and B16F10 cells. Tested Concentrations: 1 µM. Incubation Duration: 8, 16 and 24 h. Experimental Results: Caused cell arrest during G2/M phase. |
| References |
| Molecular Formula |
C28H25FN4OS
|
|---|---|
| Molecular Weight |
484.587708234787
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| Exact Mass |
484.173
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| CAS # |
891894-69-2
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| PubChem CID |
22523776
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
6.4
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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 |
5
|
| Heavy Atom Count |
35
|
| Complexity |
720
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
SNVVZJBHCSPRGY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H25FN4OS/c29-22-9-6-20(7-10-22)24-18-33-25-11-8-21(16-26(25)35-28(33)31-24)27(34)30-23-12-14-32(15-13-23)17-19-4-2-1-3-5-19/h1-11,16,18,23H,12-15,17H2,(H,30,34)
|
| Chemical Name |
N-(1-benzylpiperidin-4-yl)-2-(4-fluorophenyl)imidazo[2,1-b][1,3]benzothiazole-6-carboxamide
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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)
|
| Solubility (In Vitro) |
DMSO: 10 mg/mL (20.64 mM)
H2O: < 0.1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 1 mg/mL (2.06 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 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 | 2.0636 mL | 10.3180 mL | 20.6360 mL | |
| 5 mM | 0.4127 mL | 2.0636 mL | 4.1272 mL | |
| 10 mM | 0.2064 mL | 1.0318 mL | 2.0636 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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