IKK (IκB kinase) is an enzyme complex that is involved in propagating the cellular response to inflammation. An IκB kinase is an enzyme that catalyzes the chemical reaction: ATP + IκB protein ADP + IκB phosphoprotein. The IκB kinase enzyme complex is part of the upstream NF-κB signal transduction cascade. The IκBα (inhibitor of kappa B) protein inactivates the NF-κB transcription factor by masking the nuclear localization signals of NF-κB proteins and keeping them sequestered in an inactive state in the cytoplasm. IKK specifically, phosphorylates the inhibitory IκBα protein. This phosphorylation results in the dissociation of IκBα from NF-κB. NF-κB, which is free migrates into the nucleus and activates the expression of at least 150 genes; some of which are anti-apoptotic. IKK belongs to the family of transferases, specifically those transferring a phosphate group to the sidechain oxygen atom of serine or threonine residues in proteins.


Anti-infection >
Arenavirus Bacterial CMV Enterovirus Filovirus Fungal HBV HCV HIV HSV Influenza Virus Parasite Reverse Transcriptase RSV SARS-CoV
Antibody-drug Conjugate >
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Apoptosis >
Apoptosis Bcl-2 Family c-Myc Caspase DAPK Ferroptosis IAP MDM-2/p53 PKD RIP kinase Survivin Thymidylate Synthase TNF Receptor
Autophagy >
Autophagy LRRK2 ULK Mitophagy
Cell Cycle/DNA Damage >
Antifolate APC ATM/ATR Aurora Kinase Casein Kinase CDK Checkpoint Kinase (Chk) CRISPR/Cas9 Deubiquitinase DNA Alkylator/Crosslinker DNA-PK DNA/RNA Synthesis Eukaryotic Initiation Factor (eIF) G-quadruplex Haspin Kinase HDAC HSP IRE1 Kinesin LIM Kinase (LIMK) Microtubule/Tubulin Mps1 Nucleoside Antimetabolite/Analog p97 PAK PARP PERK Polo-like Kinase (PLK) PPAR RAD51 ROCK Sirtuin SRPK Telomerase TOPK Topoisomerase Wee1
Cytoskeleton >
Arp2/3 Complex Dynamin Gap Junction Protein Integrin Kinesin Microtubule/Tubulin Mps1 Myosin PAK
Epigenetics >
AMPK Aurora Kinase DNA Methyltransferase Epigenetic Reader Domain HDAC Histone Acetyltransferase Histone Demethylase Histone Methyltransferase JAK MicroRNA PARP PKC Sirtuin Protein Arginine Deiminase
GPCR/G Protein >
5-HT Receptor Adenosine Receptor Adenylate Cyclase Adiponectin Receptor Adrenergic Receptor Angiotensin Receptor Bombesin Receptor Bradykinin Receptor Cannabinoid Receptor CaSR CCR CGRP Receptor Cholecystokinin Receptor CRFR CXCR Dopamine Receptor EBI2/GPR183 Endothelin Receptor GHSR Glucagon Receptor Glucocorticoid Receptor GNRH Receptor GPCR19 GPR109A GPR119 GPR120 GPR139 GPR40 GPR55 GPR84 Guanylate Cyclase Histamine Receptor Imidazoline Receptor Leukotriene Receptor LPL Receptor mAChR MCHR1 (GPR24) Melatonin Receptor mGluR Motilin Receptor Neurokinin Receptor Neuropeptide Y Receptor Neurotensin Receptor Opioid Receptor Orexin Receptor (OX Receptor) Oxytocin Receptor P2Y Receptor Prostaglandin Receptor Protease-Activated Receptor (PAR) Ras RGS Protein Sigma Receptor Somatostatin Receptor TSH Receptor Urotensin Receptor Vasopressin Receptor Melanocortin Receptor
Immunology/Inflammation >
Aryl Hydrocarbon Receptor CCR Complement System COX CXCR FLAP Histamine Receptor IFNAR Interleukin Related IRAK MyD88 NO Synthase NOD-like Receptor (NLR) PD-1/PD-L1 PGE synthase Salt-inducible Kinase (SIK) SPHK STING Thrombopoietin Receptor Toll-like Receptor (TLR) Arginase
JAK/STAT Signaling >
EGFR JAK Pim STAT
MAPK/ERK Pathway >
ERK JNK KLF MAP3K MAP4K MAPKAPK2 (MK2) MEK Mixed Lineage Kinase MNK p38 MAPK Raf Ribosomal S6 Kinase (RSK)
Membrane Transporter/Ion Channel >
ATP Synthase BCRP Calcium Channel CFTR Chloride Channel CRAC Channel CRM1 EAAT2 GABA Receptor GlyT HCN Channel iGluR Monoamine Transporter Monocarboxylate Transporter Na+/Ca2+ Exchanger Na+/HCO3- Cotransporter Na+/K+ ATPase nAChR NKCC P-glycoprotein P2X Receptor Potassium Channel Proton Pump SGLT Sodium Channel TRP Channel URAT1
Metabolic Enzyme/Protease >
15-PGDH 5 alpha Reductase 5-Lipoxygenase Acetyl-CoA Carboxylase Acyltransferase Adenosine Deaminase Adenosine Kinase Aldehyde Dehydrogenase (ALDH) Aldose Reductase Aminopeptidase Angiotensin-converting Enzyme (ACE) ATGL ATP Citrate Lyase Carbonic Anhydrase Carboxypeptidase Cathepsin CETP COMT Cytochrome P450 Dipeptidyl Peptidase Dopamine β-hydroxylase E1/E2/E3 Enzyme Elastase Enolase FAAH FABP Factor Xa Farnesyl Transferase Fatty Acid Synthase (FAS) FXR Glucokinase GSNOR Gutathione S-transferase HCV Protease Hexokinase HIF/HIF Prolyl-Hydroxylase HIV Integrase HIV Protease HMG-CoA Reductase (HMGCR) HSP Indoleamine 2,3-Dioxygenase (IDO) Isocitrate Dehydrogenase (IDH) Lactate Dehydrogenase LXR MAGL Mineralocorticoid Receptor Mitochondrial Metabolism MMP Nampt NEDD8-activating Enzyme Neprilysin PAI-1 PDHK PGC-1α Phosphatase Phosphodiesterase (PDE) Phospholipase Procollagen C Proteinase Proteasome Pyruvate Kinase RAR/RXR Renin ROR Ser/Thr Protease SGK Stearoyl-CoA Desaturase (SCD) Thrombin Tryptophan Hydroxylase Tyrosinase Xanthine Oxidase
Neuronal Signaling >
5-HT Receptor AChE Adenosine Kinase Amyloid-β Beta-secretase CaMK CGRP Receptor COMT Dopamine Receptor Dopamine Transporter FAAH GABA Receptor GlyT iGluR Imidazoline Receptor mAChR Melatonin Receptor Monoamine Oxidase nAChR Neurokinin Receptor Opioid Receptor Serotonin Transporter γ-secretase
NF-κB >
NF-κB IKK Keap1-Nrf2 MALT1
PI3K/Akt/mTOR >
Akt AMPK ATM/ATR DNA-PK GSK-3 MELK mTOR PDK-1 PI3K PI4K PIKfyve PTEN
PROTAC >
PROTAC E3 Ligase Ligand-Linker Conjugate Ligand for E3 Ligase PROTAC Linker PROTAC-linker Conjugate for PAC
Protein Tyrosine Kinase/RTK >
Ack1 ALK Bcr-Abl BMX Kinase Btk c-Fms c-Kit c-Met/HGFR Discoidin Domain Receptor DYRK EGFR Ephrin Receptor FAK FGFR FLT3 IGF-1R Insulin Receptor IRAK Itk PDGFR PKA Pyk2 ROS Src Syk TAM Receptor Trk Receptor VEGFR
Stem Cell/Wnt >
Casein Kinase ERK Gli GSK-3 Hedgehog Hippo (MST) JAK Notch Oct3/4 PKA Porcupine ROCK sFRP-1 Smo STAT TGF-beta/Smad Wnt YAP β-catenin γ-secretase
TGF-beta/Smad >
TGF-beta/Smad PKC ROCK TGF-β Receptor
Vitamin D Related >
VD/VDR
Others >
Androgen Receptor Aromatase Estrogen Receptor/ERR Progesterone Receptor Thyroid Hormone Receptor Others

GS143

GS143 is a selec­tive IκBα ubiquitination inhibitor with an IC50 of 5.2 μM for SCFβTrCP1-mediated IκBα ubiquitylation. GS143 sup­presses NF-κB acti­va­tion and tran­scrip­tion of tar­get genes and does not inhibit proteasome activity. GS143 has anti-asthma effect[1][2].

  • CAS Number: 916232-21-8
  • MF: C28H19FN2O4
  • MW: 466.5
  • Catalog: E1/E2/E3 Enzyme
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MLN120B

MLN120B is a specific, ATP competitive IKKβ inhibitor with an IC50 of 60 nM.

  • CAS Number: 783348-36-7
  • MF: C19H15ClN4O2
  • MW: 366.801
  • Catalog: IKK
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 545.0±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 283.4±30.1 °C

TBK1/IKKε-IN-4

TBK1-IKKε inhibitor II is a potent, selective dual inhibitor of TBK1/IKKε with IC50 of 13 nM/59 nM, respectively; displays 100- to 1000-fold less activity against other tested protein kinases including PDK1, PI3K family members and mTOR; inhibits LPS-induced expression of IFNβ (IC50=62 nM), and the IFNβ target genes IP10 (IC50=78 nM) and Mx1 (IC50=20 nM); effectively blocks TLR3-dependent IRF3 nuclear translocation in cells with IC50<100 nM.

  • CAS Number: 1381930-17-1
  • MF: C28H35N7O4
  • MW: 533.622
  • Catalog: IKK
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 668.1±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 357.9±34.3 °C

BMS-345541

BMS-345541 is a selective inhibitor of the catalytic subunits of IKK (IKK-2 IC50=0.3 μM, IKK-1 IC50=4 μM). BMS-345541 binds at an allosteric site of IKK.

  • CAS Number: 547757-23-3
  • MF: C14H18ClN5
  • MW: 291.779
  • Catalog: IKK
  • Density: N/A
  • Boiling Point: 449.5ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 225.6ºC

MRT67307 hydrochloride

MRT67307 hydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively[1]. MRT67307 hydrochloride also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 hydrochloride also blocks autophagy in cells[2].

  • CAS Number: 2095432-39-4
  • MF: C26H37ClN6O2
  • MW: 501.06
  • Catalog: Autophagy
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Malachite green oxalate

Malachite green oxalate is a triphenylmethane dye which can be used to detect the release of phosphate in enzymatic reactions. Malachite green oxalate is also a potent and selective inhibitor of IKBKE, and inhibits its downstream targets such as IκBα, p65 and IRF3. Malachite green oxalate exhibits antitumor activity in vitro and in vivo[1][2][3].

  • CAS Number: 2437-29-8
  • MF: C52H54N4O12
  • MW: 454.946
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: 164°C (dec.)
  • Flash Point: N/A

Resveratrol

Resveratrol (SRT 501), a natural polyphenol that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. It has a wide spectrum of targets including mTOR, JAK, β-amyloid.

  • CAS Number: 501-36-0
  • MF: C14H12O3
  • MW: 228.243
  • Catalog: Bacterial
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 449.1±14.0 °C at 760 mmHg
  • Melting Point: 253-255°C
  • Flash Point: 222.3±14.7 °C

PHA-408

PHA 408 (PHA-408) is a potent, selective and orally active IκB kinase-2 (IKK-2) inhibitor. PHA 408 is a powerful anti-inflammatory agent against lipopolysaccharide (LPS)- and cigarette smoke (CS)-mediated lung inflammation[1].

  • CAS Number: 503555-55-3
  • MF: C29H27ClFN7O2
  • MW: 560.02
  • Catalog: IKK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

4'-Hydroxywogonin

4′-Hydroxywogonin (8-Methoxyapigenin), a flavonoid, could be isolated from a variety of plants including Scutellaria barbata and Verbena littoralis. 4′-Hydroxywogonin has anti-inflammatory activity via TAK1/IKK/NF-κB, MAPKs and PI3/AKT signaling pathways. 4′-Hydroxywogonin inhibits angiogenesis by disrupting PI3K/AKT signaling. 4′-Hydroxywogonin inhibits cell proliferation and induces apoptosis[1][2][3].

  • CAS Number: 57096-02-3
  • MF: C16H12O6
  • MW: 300.263
  • Catalog: Apoptosis
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 578.1±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 220.9±23.6 °C

Isophysalin A

Isophysalin A is a physalin with alpha and beta unsaturated ketone components. Isophysalin A binds to GSH and targets multiple cysteine residues on IKKβ. Isophysalin A also inhibits inducible NO synthase (iNOS) and nitric oxide (NO) production, showing anti-inflammatory activity[1].

  • CAS Number: 1363398-67-7
  • MF: C28H30O10
  • MW: 526.53
  • Catalog: NO Synthase
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 846.6±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 286.6±27.8 °C

IKK-IN-4

IKK-IN-4 is a potent and selective IkappaB kinase 2 (IKKβ orIKK2) inhibitor, with IC50s of 45 and 650 nM for IKKβ and IKKα, respectively[1].

  • CAS Number: 615529-94-7
  • MF: C18H19N5S
  • MW: 337.44
  • Catalog: IKK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BMS 345541

BMS-345541 free base is a selective inhibitor of the catalytic subunits of IKK (IKK-2 IC50=0.3 μM, IKK-1 IC50=4 μM). BMS-345541 binds at an allosteric site of IKK.

  • CAS Number: 445430-58-0
  • MF: C14H17N5
  • MW: 255.318
  • Catalog: IKK
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 449.5±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 225.6±28.7 °C

ACHP (Hydrochloride)

ACHP Hydrochloride is a highly potent and selective IKK-β inhibitor with an IC50 of 8.5 nM.

  • CAS Number: 406209-26-5
  • MF: C21H25ClN4O2
  • MW: 400.90200
  • Catalog: IKK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MRT67307

MRT67307 is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively. MRT67307 also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively.

  • CAS Number: 1190378-57-4
  • MF: C26H36N6O2
  • MW: 464.603
  • Catalog: Autophagy
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BMS-066

BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor, with IC50s of 9 nM and 72 nM, respectively.

  • CAS Number: 914946-88-6
  • MF: C19H21N7O2
  • MW: 379.41600
  • Catalog: IKK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Amlexanox

AmLexanox is a specific inhibitor of IKKε and TBK1, and inhibits the IKKε and TBK1 activity determined by MBP phosphorylation with an IC50 of approximately 1-2 μM.

  • CAS Number: 68302-57-8
  • MF: C16H14N2O4
  • MW: 298.293
  • Catalog: IKK
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 570.0±50.0 °C at 760 mmHg
  • Melting Point: >3000C
  • Flash Point: 298.5±30.1 °C

IMD 0354

IMD-0354 is a selective IKKβ inhibitor which inhibits NF-κB activity. IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC 50 of 1.2±0.3 uM.

  • CAS Number: 978-62-1
  • MF: C15H8ClF6NO2
  • MW: 383.67300
  • Catalog: IKK
  • Density: 1.561g/cm3
  • Boiling Point: 323.1ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 149.2ºC

CAY10575

IKK2-IN-3 (Compound 8) is an IKK2 inhibitor with an IC50 of 0.075 μM[1].

  • CAS Number: 916985-21-2
  • MF: C22H21N3O6S2
  • MW: 487.549
  • Catalog: IKK
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 735.4±70.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 398.5±35.7 °C

MRT67307 dihydrochloride

MRT67307 dihydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively[1]. MRT67307 dihydrochloride also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 dihydrochloride also blocks autophagy in cells[2].

  • CAS Number: 1781882-89-0
  • MF: C26H38Cl2N6O2
  • MW: 537.52
  • Catalog: Autophagy
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

IKK-16

IKK 16 hydrochloride is a selective IκB kinase (IKK) inhibitor for IKK2, IKK complex and IKK1 with IC50s of 40 nM, 70 nM and 200 nM, respectively[1]. IKK16 also inhibits leucine-rich repeat kinase-2 (LRRK2) with an IC50 of 50 nM[2].

  • CAS Number: 1186195-62-9
  • MF: C28H30ClN5OS
  • MW: 520.09
  • Catalog: LRRK2
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PS 1145 dihydrochloride

PS-1145 (dihydrochloride) is a potent IκB kinase-2 inhibitor with an IC50 value of 88 nM. PS-1145 (dihydrochloride) inhibits activity of NF-κB by blocking IκB kinase phosphorylation in tumor-bearing rats[1].

  • CAS Number: 1049743-58-9
  • MF: C17H13Cl3N4O
  • MW: 395.670
  • Catalog: IKK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

LY2409881

LY2409881 is a selective IκB kinase β (IKK2) inhibitor with an IC50 of 30 nM.

  • CAS Number: 946518-61-2
  • MF: C24H29ClN6OS
  • MW: 485.045
  • Catalog: IKK
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

HPN-01

HPN-01 is a potent and selective IKK inhibitor, with pIC50 values of 6.4, 7.0 and <4.8 for IKK-α, IKK-β and IKK-ε, respectively. HPN-01 displays greater 50-fold selectivity over a panel of more than 50 other kinases, including ALK5, CDK-2, EGFR, ErbB2, GSK3β, PLK1, Src, and VEGFR-2[1].

  • CAS Number: 928655-63-4
  • MF: C19H16ClN3O3S
  • MW: 401.87
  • Catalog: IKK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bay 65-1942 (hydrochloride)

Bay 65-1942 hydrochloride is an ATP-competitive and selective IKKβ inhibitor.

  • CAS Number: 600734-06-3
  • MF: C22H26ClN3O4
  • MW: 431.91300
  • Catalog: IKK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PS-1145

PS-1145 is an IκB kinase (IKK) inhibitor with an IC50 of 88 nM.

  • CAS Number: 431898-65-6
  • MF: C17H11ClN4O
  • MW: 322.748
  • Catalog: IKK
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 511.0±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 262.9±30.1 °C

IKK-16

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.

  • CAS Number: 873225-46-8
  • MF: C28H29N5OS
  • MW: 483.628
  • Catalog: LRRK2
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 721.6±70.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 390.2±35.7 °C

(5-PHENYL-2-UREIDO)THIOPHENE-3-CARBOXAMIDE

IKK2-IN-4 (compound 4) is a potent IKK-2 inhibitor, with an IC50 of 25 nM. IKK2-IN-4 can inhibit the LPS-induced production of TNFα in PBMCs[1].

  • CAS Number: 354811-10-2
  • MF: C12H11N3O2S
  • MW: 261.30
  • Catalog: IKK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PF 184

PF-184 is a potent inhibitory factor-κB kinase 2 (IKK-2) inhibitor with an IC50 of 37 nM. PF-184 has anti-inflammatory effects[1].

  • CAS Number: 1187460-81-6
  • MF: C32H32ClFN6O4
  • MW: 619.09
  • Catalog: IKK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BI 605906

BI605906 is a novel IKKβ inhibitor with an IC50 value of 380 nM when assayed at 0.1 mM ATP.

  • CAS Number: 960293-88-3
  • MF: C17H22F2N4O3S2
  • MW: 432.50800
  • Catalog: IKK
  • Density: 1.48±0.1 g/cm3 (20 °C, 760 mmHg)
  • Boiling Point: 713.7±60.0 °C (760 mmHg)
  • Melting Point: N/A
  • Flash Point: N/A

BOT-64

BOT-64 is an inhibitory κB (IκB) kinase β (IKKβ) inhibitor with an IC50 of 1 µM. BOT-64 blocks lipopolysaccharide-induced nuclear factor-κB activation and nuclear factor-κB-regulated inflammatory gene transcription[1].

  • CAS Number: 113760-29-5
  • MF: C15H15NO2S
  • MW: 273.35
  • Catalog: IKK
  • Density: 1.27±0.1 g/cm3
  • Boiling Point: 402.1±48.0 °C
  • Melting Point: N/A
  • Flash Point: N/A