| Size | Price | Stock | Qty |
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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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| Targets |
Inhibitor of Krüppel-like factor 5 (KLF5) expression/activity . [1]
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| ln Vitro |
SR15006 (1 μM or 10 μM; DLD-1 CRC cells) significantly reduces the levels of tested cyclins over the course of 72 hours[1].
Treatment with SR15006 significantly reduced the activity of the human KLF5 promoter in a luciferase assay using DLD-1/pGL4.18hKLF5p cells after 24 hours, demonstrating its ability to inhibit KLF5 promoter-driven transcription. [1] SR15006 inhibited the viability of multiple colorectal cancer (CRC) cell lines (DLD-1, HCT116, HT29, SW620) in a 24-hour Cell Titer-Glo assay. [1] Treatment of DLD-1 and HCT116 CRC cells with SR15006 (1 µM or 10 µM) over 72 hours significantly reduced cell proliferation compared to vehicle control. [1] Flow cytometry analysis showed that treatment with SR15006 (10 µM) altered the cell cycle profile of DLD-1 and HCT116 cells, causing a decrease in the proportion of cells in G0/G1 phase and an increase in cells in S and G2/M phases over a 3-day period, similar to the effects of ML264. [1] Annexin V/PI staining and FACS analysis indicated that treatment with SR15006 (10 µM) increased the population of cells in early and late apoptosis in HCT116 cells over 72 hours, but its pro-apoptotic effect in DLD-1 cells was less pronounced than that of SR18662. [1] Western blot analysis demonstrated that treatment with SR15006 (1 µM or 10 µM for 72 hours) downregulated the expression of components of the MAPK signaling pathway (e.g., EGFR, ERK, KLF5, EGR1) and the WNT/β-catenin signaling pathway (e.g., AKT, p-AKT, total β-catenin, active p-S552 β-catenin) in DLD-1 and HCT116 cells. [1] Treatment with SR15006 (1 µM or 10 µM for 72 hours) also reduced the protein levels of cyclins (D1, E, A2, B1) in DLD-1 cells. [1] |
| Cell Assay |
KLF5 Promoter Activity Assay: DLD-1 cells stably transfected with a human KLF5 promoter-driven luciferase reporter (DLD-1/pGL4.18hKLF5p) were seeded in 96-well plates. Cells were treated with SR15006 dissolved in DMSO at final concentrations ranging from 0.001 to 20 µM for 24 hours. Luciferase activity was measured using a commercial luciferase assay system and a plate reader to determine the inhibitory effect on KLF5 promoter activity. [1]
Cell Viability Assay: DLD-1, HCT116, HT29, and SW620 colorectal cancer cells were seeded in 96-well plates. Cells were treated with SR15006 dissolved in DMSO at final concentrations ranging from 0.001 to 20 µM for 24 hours. Cell viability was assessed using a commercial luminescent cell viability assay kit and a plate reader. [1] Cell Proliferation, Cell Cycle, and Apoptosis Assays: DLD-1 and HCT116 cells were treated with 1 µM or 10 µM SR15006 or vehicle (DMSO). Cells were collected at 24, 48, and 72 hours post-treatment. For cell cycle analysis, cells were stained with propidium iodide and analyzed by flow cytometry. For apoptosis analysis, cells were stained with Annexin V and propidium iodide and analyzed by flow cytometry. Each experiment was performed in triplicate. [1] Western Blot Analysis: DLD-1 and HCT116 cells were treated with 1 µM or 10 µM SR15006 or vehicle for 24, 48, and 72 hours. Total protein was extracted using Laemmli buffer. Proteins were separated by SDS-PAGE, transferred to membranes, and probed with antibodies against targets of interest (e.g., MAPK pathway components, WNT pathway components, cyclins) to assess protein level changes. [1] |
| References | |
| Additional Infomation |
SR15006 is a small molecule compound related to the structure of ML264. It is a low-optimized analog developed in a structure-activity relationship (SAR) study, which ultimately led to the discovery of the improved lead compound SR18662. [1] Its chemical name is (E)-3-(3-chlorophenyl)-N-(2-(4-(methanesulfonyl)piperazin-1-yl)-2-oxoethyl)acrylamide. [1] Its synthesis is carried out in three steps, the specific steps of which are described in the supplementary materials. [1]
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| Molecular Formula |
C16H20CLN3O4S
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|---|---|
| Molecular Weight |
385.87
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| Exact Mass |
385.09
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| Elemental Analysis |
C, 49.80; H, 5.22; Cl, 9.19; N, 10.89; O, 16.59; S, 8.31
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| CAS # |
2505001-54-5
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| Related CAS # |
2505001-54-5
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| PubChem CID |
155194738
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| Appearance |
White to off-white solid powder
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| LogP |
0.8
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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
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| Heavy Atom Count |
25
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| Complexity |
609
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CS(=O)(=O)N1CCN(CC1)C(=O)CNC(=O)/C=C/C2=CC(=CC=C2)Cl
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| InChi Key |
DURMLOBZTVQDGQ-AATRIKPKSA-N
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| InChi Code |
InChI=1S/C16H20ClN3O4S/c1-25(23,24)20-9-7-19(8-10-20)16(22)12-18-15(21)6-5-13-3-2-4-14(17)11-13/h2-6,11H,7-10,12H2,1H3,(H,18,21)/b6-5+
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| Chemical Name |
(E)-3-(3-chlorophenyl)-N-[2-(4-methylsulfonylpiperazin-1-yl)-2-oxoethyl]prop-2-enamide
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| Synonyms |
SR-15006; SR15006; SR 15006
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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: ~100 mg/mL (~259.2 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.48 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 (6.48 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 (6.48 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 | 2.5915 mL | 12.9577 mL | 25.9155 mL | |
| 5 mM | 0.5183 mL | 2.5915 mL | 5.1831 mL | |
| 10 mM | 0.2592 mL | 1.2958 mL | 2.5915 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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