1. NF-κB
    Autophagy
  2. IKK
    LRRK2

IKK 16 

Cat. No.: HY-13687 Purity: 99.78%
Handling Instructions

IKK 16 is a selective IκB kinase (IKK) inhibitor for IKK2, IKK complex and IKK1 with IC50s of 40 nM, 70 nM and 200 nM, respectively. IKK16 also inhibits leucine-rich repeat kinase-2 (LRRK2) with an IC50 of 50 nM.

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

IKK 16 Chemical Structure

IKK 16 Chemical Structure

CAS No. : 873225-46-8

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 191 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
10 mg USD 174 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 714 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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    IKK 16 purchased from MCE. Usage Cited in: Respir Res. 2017 Sep 20;18(1):174.

    BECs are pretreated with specific STAT6 inhibitor (AS1517499) or a selective IκB kinase inhibitor (IKK 16) for half an hour, then treated for 24 h in the presence or absence of 20 ng/mL IL-4. Immunofluorescence staining of MUC5AC protein is performed according to the Methods.

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    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    IKK 16 is a selective IκB kinase (IKK) inhibitor for IKK2, IKK complex and IKK1 with IC50s of 40 nM, 70 nM and 200 nM, respectively. IKK16 also inhibits leucine-rich repeat kinase-2 (LRRK2) with an IC50 of 50 nM.

    IC50 & Target[1]

    IKK2

    40 nM (IC50)

    IKK1

    200 nM (IC50)

    IKK

    70 nM (IC50)

    LRRK2

    50 nM (IC50)

    In Vitro

    IKK 16 is a potent inhibitor of IKK2 with IC50 value of 40 nM[1]. IKK 16, a leucine-rich repeat kinase-2 (LRRK2) kinase inhibitor, exhibits in vitro IC50s of 50 nM. IKK 16 exhibits sub-micromolar IC50 concentrations for LRRK2 in vitro, which is lower than what observed for cellular inhibition of Ser935 phosphorylation. IKK 16 (20 μM) can inhibit LRRK2 Ser935 phosphorylation in HEK293 GFP-LRRK2 G2019S cells (GS) or A2016T/G2019S (IRM) cells in vitro.

    In Vivo

    IKK 16 also demonstrates significant in vivo activity in an acute model of cytokine release. Both routes of administration of IKK 16 (30 mg/kg, sc) or orally (30 mg/kg, p.o) at the indicated dose results in a significant inhibition of 86% (sc) and 75% (p.o.). IKK 16(10 mg/kg, sc) is also active in the thioglycollate-induced peritonitis model in the mouse. The maximal inhibition of neutrophil extravasation in this model is about 50%[1]. Treatment of septic mice with IKK 16 (1 mg/kg body weight i.v.) results in a significantly increased degree of phosphorylation (P<0.05) of serine residues on Akt and eNOS in the liver[3].

    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 2.0677 mL 10.3385 mL 20.6770 mL
    5 mM 0.4135 mL 2.0677 mL 4.1354 mL
    10 mM 0.2068 mL 1.0338 mL 2.0677 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay
    [2]

    IKK 16 is prepared in DMSO and stored, and then diluted with appropriate medium before use[2].

    SH-SY5Y cells are transduced with 25% (v/v) BacMam LRRK2-GFP G2019S and plated (20 µL/well, 20,000 cells/well) onto eight 384-well assay plates. Then 25% BacMam LRRK2-GFP G2019S transduced SH-SY5Y cells are incubated with indicated concentrations of indicated compounds (e.g., IKK 16, 0.01, 0.1, 1, 10 and 100 μM) for 90 min prior to the TR-FRET detection with Tb-anti-LRRK2 pSer935 antibody. The % inhibition is calculated[2].
    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1][3]

    IKK 16 is prepared in DMSO and diluted with saline or PBS.

    Rats and Mice[1]
    IKK 16 is tested in two animal models. First, its efficacy to inhibit TNFα release into plasma upon LPS-challenge in the rat is determined. IKK 16 is dosed sc (30 mg/kg) or orally (30 mg/kg) 1 h prior to the LPS-challenge. Four hours after the challenge, plasma is collected and the systemic TNFα levels are analyzed using a commercially available ELISA kit. Both routes of administration of IKK 16 at the indicated dose results in a significant inhibition of 86% (sc) and 75% (p.o.). In a second experiment, IKK 16 is also active in the thioglycollate-induced peritonitis model in the mouse. The maximal inhibition of neutrophil extravasation in this model is about 50% at a dose of 10 mg/kg sc.
    Mice[3]
    Two-month-old male C57BL/6 mice receive LPS (9 mg/kg body weight) and PepG (3 mg/kg body weight) in 0.9% saline (5 mL/kg body weight) intraperitoneally. Sham mice are not subjected to LPS/PepG, but are otherwise treated the same way. At 1 hour after LPS/PepG co-administration, mice are treated either with IKK 16 (1 mg/kg body weight i.v.) or vehicle (5 mL/kg body weight 10% DMSO i.v.). At 24 hours the experiment is terminated and organ and blood samples are collected for quantification of organ dysfunction and/or injury. Mice are randomly allocated into four different groups: (1) sham+vehicle (n=10); (2) sham+IKK 16 (n=3); (3) LPS/PepG+vehicle (n=9); (4) LPS/PepG+IKK 16 (n=10).
    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    483.63

    Formula

    C₂₈H₂₉N₅OS

    CAS No.

    873225-46-8

    SMILES

    O=C(C1=CC=C(NC2=NC=CC(C3=CC4=CC=CC=C4S3)=N2)C=C1)N5CCC(N6CCCC6)CC5

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 27 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 99.78%

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    Product Name:
    IKK 16
    Cat. No.:
    HY-13687
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