IKK-2 inhibitor VIII
ACHP (Hydrochloride )
CAS: 406209-26-5
Molecular Formula: C21H25ClN4O2
IKK-2 inhibitor VIII - Names and Identifiers
IKK-2 inhibitor VIII - Physico-chemical Properties
| Molecular Formula | C21H25ClN4O2 |
| Molar Mass | 400.9018 |
| Solubility | 10 mM in DMSO |
| Storage Condition | -20℃ |
| In vitro study | ACHP Hydrochloride (Compound 4j) exhibits potent IKK-β inhibitory (IC 50 : 8.5 nM) and cellular activities (IC 50 =40 nM, in A549 cells). ACHP moderately inhibits IKK-α with an IC 50 of 250 nM but exhibits good selectivity towards other kinases, such as IKK3, Syk and MKK4 (IC 50 >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. 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 (IC 50 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. |
| In vivo study | 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 (P app 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. |
IKK-2 inhibitor VIII - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.494 ml | 12.472 ml | 24.944 ml |
| 5 mM | 0.499 ml | 2.494 ml | 4.989 ml |
| 10 mM | 0.249 ml | 1.247 ml | 2.494 ml |
| 5 mM | 0.05 ml | 0.249 ml | 0.499 ml |
Last Update：2024-01-02 23:10:35
IKK-2 inhibitor VIII - Reference Information
| biological activity | ACHP Hydrochloride (IKK-2 Inhibitor VIII) is an effective and selective IKK-β inhibitor with IC50 of 8.5 nM. |
| target | IKK-β 8.5 nM (IC 50 ) IKK-α 250 nM (IC 50 ) |
| in vitro study | ACHP Hydrochloride (Compound 4j) exhibits potent IKK-β inhibitory (IC 50 : 8.5 nM) and cellular activities (IC 50=40 nM, in A549 cells). ACHP moderately inhibits IKK-α with an IC 50 of 250 nM but exhibits good selectivity towards other kinases, such as IKK3, Syk and MKK4 (IC 50 >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 fail 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. ACHP inhibits growth of these cells in a dose-dependent banner. tax-active cell lines are more susceptible to ACHP than tax-inactive cell lines and jurkat (IC 50 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. |
| in vivo study | ACHP (Compound 4j) is orally bioavailable in ice 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 (P app 62.3 × 10 -7cm/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. |
Last Update：2024-04-09 01:59:59
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CAS: 406209-26-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 406209-26-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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