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> IKK 16 [873225-46-8]

IKK 16 [873225-46-8]

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Référence HY-13687-50mg

Conditionnement : 50mg

Marque : MedChemExpress


Description

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

Cellular Effect
Cell Line Type Value Description References
HEK293 EC50
0.003 μM
Compound: IKK-1
Inhibition of atypical PKCzeta in HEK293 cells assessed as TNF-induced NFkappaB activation incubated for 3 hrs prior to TNF induction measured after 5 hrs by bright-glo luciferase reporter gene assay
Inhibition of atypical PKCzeta in HEK293 cells assessed as TNF-induced NFkappaB activation incubated for 3 hrs prior to TNF induction measured after 5 hrs by bright-glo luciferase reporter gene assay
[PMID: 23566515]
HeLa IC50
0.07 μM
Compound: 16
Inhibitory activity against IKK complex isolated from HeLa cells
Inhibitory activity against IKK complex isolated from HeLa cells
[PMID: 16236504]
HUVEC IC50
0.3 μM
Compound: 16
Inhibition of TNF-alpha-stimulated expression of ICAM1 in HUVEC cells
Inhibition of TNF-alpha-stimulated expression of ICAM1 in HUVEC cells
[PMID: 16236504]
HUVEC IC50
0.3 μM
Compound: 16
Inhibition of TNF-alpha-stimulated expression of VCAM1 in HUVEC cells
Inhibition of TNF-alpha-stimulated expression of VCAM1 in HUVEC cells
[PMID: 16236504]
HUVEC IC50
0.5 μM
Compound: 16
Inhibition of TNF-alpha-stimulated expression of E-selectin in HUVEC cells
Inhibition of TNF-alpha-stimulated expression of E-selectin in HUVEC cells
[PMID: 16236504]
In Vitro

IKK 16 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 (20 μM) inhibits phosphorylation of Ser910, Ser935, Ser955 and Ser973 in Flp-In T-REx™ HEK293 GFP-LRRK2 G2019S cells[4].
IKK 16 (20 μM) rescues phosphorylation of Ser910, Ser935, Ser955 and Ser973 in Flp-In T-REx™ HEK293 LRRK2 A2016T/G2019S mutant[4].
IKK 16 (1 μM) inhibits PKD1 activity by 67%,is ATP-competitive inhibitors[6].
IKK 16 (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 Related Antibodies
In Vivo

IKK 16 (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 (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 (30 mg/kg, s.c., once) suppresses systemic TNFα levels in LPS-induced rats model[3].
IKK 16 (10 mg/kg, s.c., once) inhibits neutrophil extravasation in thioglycollate-induced peritonitis mice model[3].
IKK 16 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.
Masse moléculaire

483.63

Formule

C28H29N5OS
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvant et solubilité
In Vitro: 

DMSO : ≥ 27 mg/mL (55.83 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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 (5.17 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 (5.17 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.
Pureté et documentation
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Description
Cond.
Prix HT
HY-13687-10mg
IKK 16 [873225-46-8]
 10mg