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
TargetMol Chemicals Inc. is headquartered in Boston, MA, and specializes in products and services that serve the research needs of chemical and biological scientists worldwide. With a client base in 40+ countries, TargetMol has evolved into one of the biggest global research suppliers for compound libraries and small molecule compounds.
170+ Compound Libraries， 10000+ Noval Small Molecucles，16000+ Nature Compounds
TargetMol diligently updates and offers over 170 types of compound libraries and a wide range of high-quality research chemicals, including inhibitors, activators, natural products, peptides, antibodies , and novel life-science kits for laboratory and scientific use. In addition, our lab allows us to conduct CADD (computer-aided drug design) and chemical synthesis to meet the customization needs of our clients.
You may like
Recommended supplier
| Product name | Price | Suppliers | Update time | |
|---|---|---|---|---|
| $48.00/1mg |
VIP5Y
|
TargetMol Chemicals Inc.
|
2024-11-19 | |
| $0.00/1kg |
VIP3Y
|
Wuhan Senwayer Century Chemical Co.,Ltd
|
2022-10-28 | |
| $61.00/1mg |
VIP5Y
|
TargetMol Chemicals Inc.
|
2024-11-19 |
United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
INQUIRY