1. NF-κB
  2. IKK
  3. ACHP Hydrochloride

ACHP Hydrochloride (Synonyms: IKK-2 Inhibitor VIII)

Cat. No.: HY-13060 Purity: 99.54%
Handling Instructions

ACHP Hydrochloride (IKK-2 Inhibitor VIII) is a highly potent and selective IKK-β inhibitor with an IC50 of 8.5 nM.

For research use only. We do not sell to patients.

ACHP Hydrochloride Chemical Structure

ACHP Hydrochloride Chemical Structure

CAS No. : 406209-26-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 243 In-stock
Estimated Time of Arrival: December 31
5 mg USD 221 In-stock
Estimated Time of Arrival: December 31
10 mg USD 356 In-stock
Estimated Time of Arrival: December 31
50 mg USD 838 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1307 In-stock
Estimated Time of Arrival: December 31
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Description

ACHP Hydrochloride (IKK-2 Inhibitor VIII) is a highly potent and selective IKK-β inhibitor with an IC50 of 8.5 nM.

IC50 & Target[1]

IKK-β

8.5 nM (IC50)

IKK-α

250 nM (IC50)

In Vitro

ACHP Hydrochloride (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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

400.90

Formula

C₂₁H₂₅ClN₄O₂

CAS No.

406209-26-5

SMILES

N#CC1=C(C=C(N=C1N)C2=C(C=CC=C2OCC3CC3)O)C4CCNCC4.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (124.72 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4944 mL 12.4719 mL 24.9439 mL
5 mM 0.4989 mL 2.4944 mL 4.9888 mL
10 mM 0.2494 mL 1.2472 mL 2.4944 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.24 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.24 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[2]

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 a HTLV-1-negative T-cell leukemia cell line Jurkat are used in this study. Approximately 1.5×104 cells are cultured in 96-well plate 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 multiplate reader. Cell viability (%) is calculated[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]
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.), 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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

ACHPIKK-2 Inhibitor VIIIIKKIκB kinaseI kappa B kinaseInhibitorinhibitorinhibit

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ACHP Hydrochloride
Cat. No.:
HY-13060
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