Referencia número: HY-13687

IKK 16

31 Cited Publications

Revisión del cliente

Based on 31 publication(s) in Google Scholar

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.

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Pureza: 99.88%
No. CAS: 873225-46-8
Fòrmula: C₂₈H₂₉N₅OS
Peso molecular:483.63

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

IKK 16 Chemical Structure

No. CAS: 873225-46-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (31)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Bioz

Actividad biológica

Descripciòn

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)

Ver todos los productos específicos de isoformas IKK :

Ver todos los productos específicos de isoformas PKD :

Ver todos los productos específicos de isoformas NF-κB :

Ver todos los productos específicos de isoformas TNF Receptor :

Ver todos los productos específicos de isoformas Interleukin Related :

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.

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.

Chemical Information

No. CAS 873225-46-8
Appearance Solid
Peso molecular 483.63
Fòrmula C₂₈H₂₉N₅OS
Color White to yellow
SMILES

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

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (31)

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Journal Impact Factor

Nature

A mechanism to initiate emergency type 2 myelopoiesis. [Abstract]

2026 May;653(8113):212-220. PMID: 41813898
Mol Cancer

Targeting CD30L in B-cell non-Hodgkin lymphoma: novel peptide conjugates and their therapeutic potential. [Abstract]

2025 Jul 5;24(1):189. PMID: 40615839
J Hepatol

FOSL1 promotes cholangiocarcinoma via transcriptional effectors that could be therapeutically targeted. [Abstract]

2021 Aug;75(2):363-376. PMID: 33887357
Mol Cell

Serine synthesis sustains macrophage IL-1β production via NAD+-dependent protein acetylation. [Abstract]

2024 Feb 15;84(4):744-759.e6. PMID: 38266638
Nat Commun

USP8 inhibition reshapes an inflamed tumor microenvironment that potentiates the immunotherapy. [Abstract]

2022 Mar 31;13(1):1700. PMID: 35361799
Theranostics

NIK links inflammation to hepatic steatosis by suppressing PPARα in alcoholic liver disease. [Abstract]

2020 Feb 18;10(8):3579-3593. PMID: 32206109
J Exp Clin Cancer Res

Pulmonary interleukin 1 beta/serum amyloid A3 axis promotes lung metastasis of hepatocellular carcinoma by facilitating the pre-metastatic niche formation. [Abstract]

2023 Jul 13;42(1):166. PMID: 37443052
J Exp Clin Cancer Res

Cyclin G2 reverses immunosuppressive tumor microenvironment and potentiates PD-1 blockade in glioma. [Abstract]

2021 Aug 27;40(1):273. PMID: 34452627
J Immunother Cancer

Targeted delivery of miR-99b reprograms tumor-associated macrophage phenotype leading to tumor regression. [Abstract]

2020 Sep;8(2):e000517. PMID: 32948650
Cell Death Dis

cGAS-STING/HMGB1-mediated senescence induced by LRRK2 accelerates cartilage degeneration in osteoarthritis. [Abstract]

2026 Mar 25;17(1):377. PMID: 41881967
Cell Death Dis

Cancer testis antigen 55 deficiency attenuates colitis-associated colorectal cancer by inhibiting NF-κB signaling. [Abstract]

2019 Apr 3;10(4):304. PMID: 30944312

IKK 16 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.
Phytomedicine

Celastrol disrupts the inflammatory feedback loop driven by Tenascin-C⁺ fibroblast subtype in psoriasis: Insights from single-cell RNA sequencing and experimental validation. [Abstract]

2026 Apr:153:157988. PMID: 41763138
Oncogene

PTPRZ1 dephosphorylates and stabilizes RNF26 to reduce the efficacy of TKIs and PD-1 blockade in ccRCC. [Abstract]

2024 Dec;43(50):3633-3644. PMID: 39443724
Cancer Cell Int

Construction of a prognostic model with histone modification-related genes and identification of potential drugs in pancreatic cancer. [Abstract]

2021 Jun 5;21(1):291. PMID: 34090418
J Invest Dermatol

M1 Macrophages Induce Protumor Inflammation in Melanoma Cells through TNFR-NF-κB Signaling. [Abstract]

2022 Nov;142(11):3041-3051.e10. PMID: 35580697
Inflammation

NF-κB-Inducing Kinase Provokes Insulin Resistance in Skeletal Muscle of Obese Mice. [Abstract]

2023 Aug;46(4):1445-1457. PMID: 37171694
Respir Res

IL-4-induced caveolin-1-containing lipid rafts aggregation contributes to MUC5AC synthesis in bronchial epithelial cells. [Abstract]

2017 Sep 20;18(1):174. PMID: 28931396

IKK 16 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.
Int Immunopharmacol

Extracellular matrix of early pulmonary fibrosis modifies the polarization of alveolar macrophage. [Abstract]

2022 Oct:111:109179. PMID: 36029666
FASEB J

Integrated Multi-Omics and Experimental Validation Unveil the GZMK/NF-κB Axis Driving Inflammation and Fibroblast Proliferation in Rosacea: A Novel Drug Target Selection Strategy. [Abstract]

2025 Oct 31;39(20):e71164. PMID: 41139274
J Immunol

MBL regulates phagocytosis and bactericidal activity of macrophages by triggering AKT/NF-κB/Rab5A axis occurred early in vertebrate evolution. [Abstract]

2025 Apr 25:vkaf028. PMID: 40280188
J Immunol

MTOR Suppresses Environmental Particle-Induced Inflammatory Response in Macrophages. [Abstract]

2018 Apr 15;200(8):2826-2834. PMID: 29563176
mSphere

The Pseudomonas aeruginosa effector protein TesG regulates alternative activation of macrophages through NLRC5. [Abstract]

2025 Nov 25;10(11):e0068125. PMID: 41170846
Mol Immunol

Persistent IKKα phosphorylation induced apoptosis in UVB and Poly I:C co-treated HaCaT cells plausibly through pro-apoptotic p73 and abrogation of IκBα. [Abstract]

2018 Dec:104:69-78. PMID: 30445257

IKK 16 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.
Biol Pharm Bull

Ponicidin Induces Apoptosis of Murine Melanoma by Inhibiting the NF-κB Signaling Pathway. [Abstract]

2023;46(6):803-810. PMID: 37258145
bioRxiv

2026 Jun 25.
bioRxiv

Transient efferocytosis-induced activation of IKKβ reprograms macrophages to promote tissue resolution. [Abstract]

2026 Apr 30:2026.04.27.720940. PMID: 42094405
bioRxiv

2026 Feb 14.
bioRxiv

2026 Jan 24.
University of Bonn

2025.
Ribeirao Preto Medical School

2025.
SSRN

2023 Dec 13.

Solvente y solubilidad

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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μL
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (285 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Amaro-Leal Â, et al. Therapeutic effects of IkB kinase inhibitor during systemic inflammation. Int Immunopharmacol. 2020 Jul;84:106509. [Content Brief]

[2]. Johnson FL, et al. Inhibition of IκB Kinase at 24 Hours After Acute Kidney Injury Improves Recovery of Renal Function and Attenuates Fibrosis. J Am Heart Assoc. 2017 Jul 3;6(7):e005092. [Content Brief]

[3]. Waelchli R, et al. Design and preparation of 2-benzamido-pyrimidines as inhibitors of IKK. Bioorg Med Chem Lett. 2006 Jan 1;16(1):108-12. [Content Brief]

[4]. Hermanson SB, Carlson CB, Riddle SM, Zhao J, Vogel KW, Nichols RJ, Bi K. Screening for novel LRRK2 inhibitors using a high-throughput TR-FRET cellular assay for LRRK2 Ser935 phosphorylation. PLoS One. 2012;7(8):e43580. [Content Brief]

[5]. SURA AL ZOUBI, et al. Inhibition of NF-κB Pathway with IKK-16 or Linagliptin Attenuates the Cardiac Dysfunction Associated with Polymicrobial Sepsis in Mice with Preexisting Type 2 Diabetes Mellitus (T2DM). Diabetes 1 July 2018; 67 (Supplement_1): 483–P.

[6]. Tandon M, et al. New pyrazolopyrimidine inhibitors of protein kinase d as potent anticancer agents for prostate cancer cells. PLoS One. 2013 Sep 23;8(9):e75601. [Content Brief]

[7]. Ansbro MR, et al. Screening compounds with a novel high-throughput ABCB1-mediated efflux assay identifies drugs with known therapeutic targets at risk for multidrug resistance interference. PLoS One. 2013 Apr 10;8(4):e60334. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0677 mL	10.3385 mL	20.6770 mL	51.6924 mL
	5 mM	0.4135 mL	2.0677 mL	4.1354 mL	10.3385 mL
	10 mM	0.2068 mL	1.0338 mL	2.0677 mL	5.1692 mL
	15 mM	0.1378 mL	0.6892 mL	1.3785 mL	3.4462 mL
	20 mM	0.1034 mL	0.5169 mL	1.0338 mL	2.5846 mL
	25 mM	0.0827 mL	0.4135 mL	0.8271 mL	2.0677 mL
	30 mM	0.0689 mL	0.3446 mL	0.6892 mL	1.7231 mL
	40 mM	0.0517 mL	0.2585 mL	0.5169 mL	1.2923 mL
	50 mM	0.0414 mL	0.2068 mL	0.4135 mL	1.0338 mL

Keywords

IKK 16

31 Cited Publications

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IKK 16

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

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Publications Citing Use of MedChemExpress (MCE) IKK 16

Ver todos los productos específicos de isoformas IKK

Ver todos los productos específicos de isoformas PKD

Ver todos los productos específicos de isoformas NF-κB

Ver todos los productos específicos de isoformas TNF Receptor

Ver todos los productos específicos de isoformas Interleukin Related

Actividad biológica

Chemical Information

Publications (31)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

IKK 16 Related Classifications

Referencia número: HY-13687