2. NF-κB Autophagy
  3. IKK LRRK2
  4. IKK 16

IKK 16 

Cat. No.: HY-13687 Purity: 98.57%
COA 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
Solution
10 mM * 1 mL in DMSO USD 110 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 110 In-stock
Solid
5 mg USD 100 In-stock
10 mg USD 174 In-stock
50 mg USD 520 In-stock
100 mg USD 780 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 17 publication(s) in Google Scholar

Other Forms of IKK 16:

IKK 16 Related Antibodies

Top Publications Citing Use of Products

    IKK 16 purchased from MCE. Usage Cited in: Cell Death Dis. 2019 Apr 3;10(4):304.   [Abstract]

    IKK 16 treatment overwhelms the function of CT55 to promote the activation of p65 and IκBα degradation. HCT116 cells transfected with Flag-CT55 were treated with IKK 16 (20 mM) or DMSO for 2 h before TNF-α treatment. Western blotting is performed to detect the protein levels of IκBα, p-p65, and p65.

    IKK 16 purchased from MCE. Usage Cited in: Mol Immunol. 2018 Nov 13;104:69-78.  [Abstract]

    Western analysis of proteins expression with treatment of IKK-16 or MG-132.

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

    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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    IKK-α IKK-β IKK IKKε TBK1

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    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[1].

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

    IKK 16 Related Antibodies
    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].

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

    483.63

    Appearance

    Solid

    Formula

    C28H29N5OS
    CAS No.
    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 27 mg/mL (55.83 mM)

    H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent 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.
    In Vivo:
    • 1.

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

      Solubility: ≥ 2.5 mg/mL (5.17 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.5 mg/mL (5.17 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.17 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 98.57%

    COA (248 KB) LCMS (270 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [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]

    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
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    IKK 16 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Keywords:

    IKK 16873225-46-8IKK16IKK-16IKKLRRK2IκB kinaseI kappa B kinase Leucine-rich repeat kinase 2Inhibitorinhibitorinhibit

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