ACHP Hydrochloride NEW
| Price | $61 | $147 | $239 |
| Package | 1mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: ACHP Hydrochloride | CAS No.: 406209-26-5 |
| Purity: 100% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | ACHP Hydrochloride |
| Description | ACHP Hydrochloride (IKK-2 Inhibitor VIII) is a highly potent and selective inhibitor of IKK-β with an IC50 of 8.5 nM. |
| Cell Research | HTLV-1-infected T-cell lines, ATL-35T, 81-66/45, MJ, and MT-2 cells, human ATL cell lines established from ATL patients, ATL-102, ED-40515(?) and TL-Om1 cells, and an HTLV-1-negative T-cell leukemia cell line Jurkat are used in this study. Approximately 1.5×10^4 cells are cultured in 96-well plates in triplicates at 37°C. Growth inhibitory effect of ACHP (0.01, 0.1, 1, 5, 10, 50 and 100 μM) is determined using MTT assay. Optical densities (OD) at 570 and 630?nm are measured with a multi-plate reader. Cell viability (%) is calculated [2]. |
| Animal Research | In vivo arachidonic acid-induced ear edema in mice: ear edema is induced by topical application of arachidonic acid (500 μg/ear). ACHP (0.3, 1 and 3 mg/kg, p.o.), Dexamethasone, and vehicle (10% cremophor in saline) are given po 60 min before the arachidonic acid application. Ear thickness is measured at 0, 1, 3, and 6 h after the arachidonic acid application [1]. |
| In vitro | ACHP Hydrochloride (Compound 4j) exhibits potent IKK-β inhibitory (IC50: 8.5 nM) and cellular activities (IC50: 40 nM, in A549 cells), moderately inhibits IKK-α (IC50: 250 nM), and demonstrates selectivity against other kinases such as IKK3, Syk, and MKK4 (IC50>20,000 nM). It inhibits NF-κB-dependent reporter gene activation in TNFα-activated HEK293 cells and PMA/calcium ionophore-activated Jurkat T cells but does not inhibit PMA-induced AP-1 activation in MRC-5 cells or 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 inhibiting IKK-β in living cells and inhibits their growth dose-dependently. 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 [1][2]. |
| In vivo | ACHP is orally bioavailable in mice (BA: 16%) and rats (BA: 60%), with significant in vivo activity in anti-inflammatory models (arachidonic acid-induced mouse ear edema model). It has reasonable aqueous solubility (0.12 mg/mL in pH 7.4 isotonic buffer), excellent Caco-2 permeability (Papp 62.3×10^-7 cm/s), and low clearance in rats (0.33 L/h/kg). In an acute inflammation model, ACHP demonstrates oral efficacy at 1 mg/kg in a dose-dependent manner [1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 45 mg/mL (112.25 mM), Sonication is recommended. |
| Keywords | I kappa B kinase | IκB kinase | Inhibitor | ACHP | inhibit | IKK | ACHP Hydrochloride |
| Inhibitors Related | JTP 0819958 - HOIPIN-1 | WS3 | Amlexanox | Malachite green oxalate | BAY 11-7082 | SC-514 | Resveratrol | Bardoxolone Methyl | Bay 11-7085 | GSK8612 | BX795 | Allicin |
| Related Compound Libraries | NF-κB Signaling Compound Library | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Ovarian Cancer Compound Library | Anti-Breast Cancer Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
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