IKK-2 inhibitor VIIIIKK-2 inhibitor,potent and selective CAS# 406209-26-5 |
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Quality Control & MSDS
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Chemical structure
3D structure
| Cas No. | 406209-26-5 | SDF | Download SDF |
| PubChem ID | 136216943 | Appearance | Powder |
| Formula | C21H25ClN4O2 | M.Wt | 400.9 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 50 mg/mL (124.72 mM; Need ultrasonic) | ||
| Chemical Name | 2-amino-6-[2-(cyclopropylmethoxy)-6-hydroxyphenyl]-4-piperidin-4-ylpyridine-3-carbonitrile;hydrochloride | ||
| SMILES | C1CC1COC2=CC=CC(=C2C3=NC(=C(C(=C3)C4CCNCC4)C#N)N)O.Cl | ||
| Standard InChIKey | QVYAMWAKDKEKMM-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C21H24N4O2.ClH/c22-11-16-15(14-6-8-24-9-7-14)10-17(25-21(16)23)20-18(26)2-1-3-19(20)27-12-13-4-5-13;/h1-3,10,13-14,24,26H,4-9,12H2,(H2,23,25);1H | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | ACHP Hydrochloride is a highly potent and selective IKK-β inhibitor with an IC50 of 8.5 nM.In Vitro:ACHP (Compound 4j) exhibits potent IKK-β inhibitory (IC50: 8.5 nM) and cellular activities (IC50=40 nM, in A549 cells). ACHP moderately inhibits IKK-α with an IC50 of 250 nM but exhibits good selectivity towards other kinases, such as IKK3, Syk and MKK4 (IC50>20,000 nM). Moreover, ACHP demonstrates quite potent activity in various cellular assays. ACHP inhibits NF-κB-dependent reporter gene activation in TNFα-activated HEK293 cells and PMA/calcium ionophore-activated Jurkat T cells. ACHP fails to inhibit PMA-induced AP-1 activation in MRC-5 cells and PMA/calcium ionophore induced NF-κB dependent reporter gene transcription in Jurkat cells even at concentrations exceeding 10 μM. ACHP selectively interferes with the NF-κB signaling cascade by inhibition of IKK-β in living cells[1]. ACHP inhibits the growth of these cells in a dose-dependent manner. Tax-active cell lines are more susceptible to ACHP than Tax-inactive cell lines and Jurkat (IC50 values in Tax-active cell lines, Tax-inactive cell lines or Jurkat are 3.1±1.3 μM, 10.7±1.7 μM and 23.6 μM, respectively), suggesting that the growth of Tax-active cells depends on NF-κB more than Tax-inactive cells[2].In Vivo:ACHP (Compound 4j) is orally bioavailable in mice and rats and demonstrates significant in vivo activity in anti-inflammatory models (arachidonic acid-induced mouse ear edema model). ACHP has reasonable aqueous solubility (0.12 mg/mL in pH 7.4 isotonic buffer) and excellent Caco-2 permeability (Papp 62.3×10-7 cm/s), and demonstrates orally bioavailability in mice (BA: 16%) and rats (BA: 60%). The favourable bioavailability of ACHP in rats is likely due to its low clearance (0.33 L/h/kg). In an acute inflammation model, ACHP exhibits oral efficacy at 1 mg/kg in a dose-dependent manner[1]. References: | |||||
IKK-2 inhibitor VIII Dilution Calculator
IKK-2 inhibitor VIII Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.4944 mL | 12.4719 mL | 24.9439 mL | 49.8878 mL | 62.3597 mL |
| 5 mM | 0.4989 mL | 2.4944 mL | 4.9888 mL | 9.9776 mL | 12.4719 mL |
| 10 mM | 0.2494 mL | 1.2472 mL | 2.4944 mL | 4.9888 mL | 6.236 mL |
| 50 mM | 0.0499 mL | 0.2494 mL | 0.4989 mL | 0.9978 mL | 1.2472 mL |
| 100 mM | 0.0249 mL | 0.1247 mL | 0.2494 mL | 0.4989 mL | 0.6236 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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IKK-2 inhibitor VIII is a potent and selective IKK-2 inhibitor with IC50 of 8.5 nM.
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ACHP Hydrochloride (IKK-2 Inhibitor VIII) is a highly potent and selective IKK-β inhibitor with an IC50 of 8.5 nM.
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