2. NF-κB Autophagy Membrane Transporter/Ion Channel Apoptosis Immunology/Inflammation
  3. IKK LRRK2 P-glycoprotein PKD NF-κB TNF Receptor Interleukin Related
  4. IKK 16 hydrochloride

IKK 16 hydrochloride is an orally active IKK inhibitor. IKK 16 hydrochloride shows IC50s of 40 nM, 70 nM, 200 nM, and 50 nM for IKK2, IKK complex, IKK1, and LRRK 2, respectively. IKK 16 hydrochloride is also a pan-PKD inhibitor, inhibiting PKD1, PKD2, and PKD3 with IC50s of 153.9, 115, and 99.7 nM, respectively. IKK 16 hydrochloride is also an ABCB1 inhibitor, interfering with the binding of ABCB1 to its substrates. IKK 16 hydrochloride protects against LPS (HY-D1056)-induced multiple organ dysfunction by reducing the acute inflammatory response induced by endotoxin exposure. IKK 16 hydrochloride can restore renal function and alleviate fibrosis in acute kidney injury. IKK 16 hydrochloride attenuates cardiac dysfunction associated with polymicrobial sepsis in mice with type 2 diabetes mellitus (T2DM) by inhibiting the NF-κB pathway.

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

IKK 16 hydrochloride

IKK 16 hydrochloride Chemical Structure

CAS No. : 1186195-62-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 23 publication(s) in Google Scholar

Other Forms of IKK 16 hydrochloride:

IKK 16 hydrochloride Related Antibodies

Top Publications Citing Use of Products

    IKK 16 hydrochloride purchased from MedChemExpress. 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 hydrochloride purchased from MedChemExpress. Usage Cited in: Mol Immunol. 2018 Dec:104:69-78.  [Abstract]

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

    IKK 16 hydrochloride purchased from MedChemExpress. 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

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    PKD1 PKD2 PKD3

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    NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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    TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

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    IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    IKK 16 hydrochloride is an orally active IKK inhibitor. IKK 16 hydrochloride shows IC50s of 40 nM, 70 nM, 200 nM, and 50 nM for IKK2, IKK complex, IKK1, and LRRK 2, respectively. IKK 16 hydrochloride is also a pan-PKD inhibitor, inhibiting PKD1, PKD2, and PKD3 with IC50s of 153.9, 115, and 99.7 nM, respectively. IKK 16 hydrochloride is also an ABCB1 inhibitor, interfering with the binding of ABCB1 to its substrates. IKK 16 hydrochloride protects against LPS (HY-D1056)-induced multiple organ dysfunction by reducing the acute inflammatory response induced by endotoxin exposure. IKK 16 hydrochloride can restore renal function and alleviate fibrosis in acute kidney injury. IKK 16 hydrochloride attenuates cardiac dysfunction associated with polymicrobial sepsis in mice with type 2 diabetes mellitus (T2DM) by inhibiting the NF-κB pathway[1][2][3][4][5][6][7].

    IC50 & Target[1][2][3][4][5][6][7]

    IKK2

    40 nM (IC50)

    IKK1

    200 nM (IC50)

    IKK

    70 nM (IC50)

    LRRK2

    50 nM (IC50)

    PKD1/PKCμ

    153.9 nM (IC50)

    PKD2

    115 nM (IC50)

    PKD3

    99.7 nM (IC50)

    In Vitro

    IKK 16 hydrochloride inhibits IκB degradation and inhibits TNFα-stimulated E-Sel, ICAM, VCAM, β2M, and HLA-DR expression in HUVEC cells, with IC50s of 1, 0.5, 0.3, 0.3, 2, 2 μM, respectively[3].
    IKK 16 hydrochloride (20 μM) inhibits phosphorylation of Ser910, Ser935, Ser955 and Ser973 in Flp-In T-REx™ HEK293 GFP-LRRK2 G2019S cells[4].
    IKK 16 hydrochloride (20 μM) rescues phosphorylation of Ser910, Ser935, Ser955 and Ser973 in Flp-In T-REx™ HEK293 LRRK2 A2016T/G2019S mutant[4].
    IKK 16 hydrochloride (1 μM) inhibits PKD1 activity by 67%,is ATP-competitive inhibitors[6].
    IKK 16 hydrochloride (1-100 μM) inhibits PKCα and PKCδ[6].

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

    IKK 16 hydrochloride Related Antibodies
    In Vivo

    IKK 16 hydrochloride (1 mg/kg, i.v., once) protects against LPS-induced multiple organ dysfunction by reducing the acute inflammatory response induced by endotoxin exposure in male Wistar rats model[1].
    IKK 16 hydrochloride (1 mg/kg, i.v., once) improves recovery of renal glomerular and tubular function, prevents fibrosis at 28 days after the AKI insult in male Wistar rats model[2].
    IKK 16 hydrochloride (30 mg/kg, s.c., once) suppresses systemic TNFα levels in LPS-induced rats model[3].
    IKK 16 hydrochloride (10 mg/kg, s.c., once) inhibits neutrophil extravasation in thioglycollate-induced peritonitis mice model[3].
    IKK 16 hydrochloride reduces CLP-induced cardiac dysfunction, NF-κB pathway activation and iNOS expression in high fat (HFD)-caecal ligation and puncture (CLP) mice model[5].

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

    Animal Model: Male Wistar rats (240-450 g) model[1]
    Dosage: 1 mg/kg
    Administration: i.v., once
    Result: Increased the serum concentration amylase and lipase, decreased serum concentration creatine kinase.
    Prevented the elevation of urea, creatinine, AST, ALT and CK serum levels, had no significant alterations in serum pancreatic enzymes (amylase and lipase) levels induced by LPS treatment.
    Decreased the mRNA gene expression of TNF-α and IL-1β, increased the gene expression of IL-6 in the heart, overexpressed the mRNA gene expression of TNF-α, IL-6 and IL-1β in kidney and liver.
    Animal Model: Male Wistar rats (240-290 g) model[2]
    Dosage: 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg
    Administration: i.v., once
    Result: Attenuated serum urea, SCr, and eCCL, reduced signs of histological injury with 1 mg/kg at 24 h into reperfusion. Attenuated the increase in the phosphorylation of IκBα on Ser32/36, phosphorylation (Ser176/180 of IKKα/β) and activation of IKK, and the subsequent nuclear translocation of the p65 NF‐κB subunit. Attenuated the increase in Sirius red staining for collagen I and III and, therefore, fibrosis. Attenuated myofibroblast formation and macrophage infiltration, and decreased TGF-β and Smad2/3 phosphorylation. prevented the expression of fibronectin caused by unilateral IRI and 28 days of reperfusion. Reduced Sirius red, α-smooth muscle actin and CD68 staining, reduced macrophage accumulation in the renal tissue.
    Animal Model: LPS-induced rats model[3]
    Dosage: 30 mg/kg
    Administration: s.c., once
    Result: Suppressed systemic TNFα levels.
    Animal Model: Thioglycollate-induced peritonitis mice model[3]
    Dosage: 10 mg/kg
    Administration: s.c., once
    Result: Inhibited neutrophil extravasation.
    Molecular Weight

    520.09

    Formula

    C28H30ClN5OS
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(C1=CC=C(NC2=NC=CC(C3=CC4=CC=CC=C4S3)=N2)C=C1)N5CCC(N6CCCC6)CC5.[H]Cl
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (192.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9227 mL 9.6137 mL 19.2274 mL
    5 mM 0.3845 mL 1.9227 mL 3.8455 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

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

      Solubility: ≥ 2.5 mg/mL (4.81 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

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

      Solubility: ≥ 2.5 mg/mL (4.81 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    % 
    +
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9227 mL 9.6137 mL 19.2274 mL 48.0686 mL
    5 mM 0.3845 mL 1.9227 mL 3.8455 mL 9.6137 mL
    10 mM 0.1923 mL 0.9614 mL 1.9227 mL 4.8069 mL
    15 mM 0.1282 mL 0.6409 mL 1.2818 mL 3.2046 mL
    20 mM 0.0961 mL 0.4807 mL 0.9614 mL 2.4034 mL
    25 mM 0.0769 mL 0.3845 mL 0.7691 mL 1.9227 mL
    30 mM 0.0641 mL 0.3205 mL 0.6409 mL 1.6023 mL
    40 mM 0.0481 mL 0.2403 mL 0.4807 mL 1.2017 mL
    50 mM 0.0385 mL 0.1923 mL 0.3845 mL 0.9614 mL
    60 mM 0.0320 mL 0.1602 mL 0.3205 mL 0.8011 mL
    80 mM 0.0240 mL 0.1202 mL 0.2403 mL 0.6009 mL
    100 mM 0.0192 mL 0.0961 mL 0.1923 mL 0.4807 mL
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    IKK 16 hydrochloride 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.

    Keywords:

    IKK 161186195-62-9IKK16IKK-16IKKLRRK2P-glycoproteinPKDNF-κBTNF ReceptorInterleukin RelatedIκB kinaseI kappa B kinase Leucine-rich repeat kinase 2P-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Protein kinase DNuclear factor-κBNuclear factor-kappaBTumor Necrosis Factor ReceptorTNFRILHUVEC cellsWistar ratsLPS-inducedHFD-CLP miceInhibitorinhibitorinhibit

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