MAP3Ks (Mitogen-activated protein kinase kinase kinases), the top components of MAPK cascades, modulate many biological processes, such as growth, development and various environmental stresses. Based on the sequence of their kinase catalytic domain, MAP3Ks are classified into three groups: the MEKK-like, ZIK-like and Raf-like families. Raf-like MAP3Ks constitute largest MAP3K subfamily. Raf-like MAP3Ks play roles in response to biotic and abiotic stresses. MAP3Ks often bind to both MAP4Ks and MAP2Ks in the same pathway. For example, MEKK1 (MAP3K1) binds to both the MAP4K NIK and the MAP2K MKK4, while NSY-1 (MAP3K) binds to the MAP2K SEK-1. MAP3Ks activates MAP2Ks by phosphorylation of a serine and/or threonine, and MAP2Ks activate MAPKs by dual phosphorylation of a Thr-X-Tyr motif.


Anti-infection >
Arenavirus Bacterial CMV Enterovirus Filovirus Fungal HBV HCV HIV HSV Influenza Virus Parasite Reverse Transcriptase RSV SARS-CoV
Antibody-drug Conjugate >
ADC Cytotoxin ADC Linker Drug-Linker Conjugates for ADC PROTAC-linker Conjugate for PAC
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

TC-S 7006

Tpl2 Kinase Inhibitor 1 (Compound 1) is a potent and selective Tpl2 (COT kinase, MAP3K8) inhibitor, plays an important role in the regulation of the inflammatory response and the progression of some cancers[1].

  • CAS Number: 871307-18-5
  • MF: C21H14ClFN6
  • MW: 404.82700
  • Catalog: MAP3K
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5Z-7-Oxozeaenol

5Z-7-Oxozeaenol is a natural anti-protozoan compound from fungal origin, acting as a potent irreversible and selective inhibitor of TAK1 and VEGF-R2, with IC50s of 8 nM and 52 nM, respectively.

  • CAS Number: 253863-19-3
  • MF: C19H22O7
  • MW: 362.37400
  • Catalog: MAP3K
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3',4',7-trihydroxy isoflavone

7,3',4'-Trihydroxyisoflavone, a major metabolite of Daidzein, is an ATP-competitive inhibitor of Cot (Tpl2/MAP3K8) and MKK4. 7,3',4'-Trihydroxyisoflavone has anticancer, anti-angiogenic, chemoprotective, and free radical scavenging activities[1][2].

  • CAS Number: 485-63-2
  • MF: C15H10O5
  • MW: 270.24
  • Catalog: Apoptosis
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 572.8±50.0 °C at 760 mmHg
  • Melting Point: 280-282°C
  • Flash Point: 224.0±23.6 °C

HS220

HS220 (HS-220) is a Plasmodium-selective takinib analog that targets atypical P. falciparum protein kinase 9 (PfPK9, Kd=4.1 uM) but does not inhibit HsTAK1, decreases K63-linked ubiquitination in P. falciparum; inhibits P. berghei parasite load in HuH7 cells with EC50 of 43 uM, with no significant change on HuH7 viability; induce a unique phenotype where parasite size in hepatocytes increases.

  • CAS Number: 1570374-32-1
  • MF: C18H17N3O3
  • MW: 323.352
  • Catalog: MAP3K
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GNE-8505

GNE-8505 is an orally available inhibitor of Dual leucine zipper kinase (DLK)[1].

  • CAS Number: 1620573-48-9
  • MF: C21H24F3N5O
  • MW: 419.44
  • Catalog: MAP3K
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ASK1-IN-4

ASK1-IN-4 (Compound 17) is an ASK1 inhibitor (IC50=0.2 μM). ASK1-IN-4 interacts with ATP-binding site of ASK1[1].

  • CAS Number: 1427538-26-8
  • MF: C18H14BrNO4S2
  • MW: 452.34
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

IACS-52825

IACS-52825 is a potent and selective DLK inhibitor with Kd of 1.3 nM, useful for the study of chemotherapy-induced peripheral neuropathy[1].

  • CAS Number: 2640376-72-1
  • MF: C16H13F7N4O2
  • MW: 426.29
  • Catalog: MAP3K
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DDO3711

DDO3711, a PP5-recruiting phosphatase recruitment chimeras (PHORCs), is formed by connecting a small molecular apoptosis signal-regulated kinase 1 (ASK1) inhibitor to a PP5 activator through a chemical linker. DDO3711 specifically inhibits ASK1 (IC50 =164.1 nM) not ASK2 (IC50>20 μM). DDO3711 significantly dephosphorylates p-ASK1T838 by recruiting PP5 and shows the ASK1-dependent antiproliferative activity. DDO3711 has anti-cancer activity and has the potential for abnormally phosphorylated oncoproteins research[1].

  • CAS Number: 2673364-10-6
  • MF: C42H41N9O6
  • MW: 767.83
  • Catalog: MAP3K
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

S-99

ASK1-IN-5 (S-99) is an inhibitor of apoptosis signal-regulated kinase 1 (ASK1) and is useful in the study of autoimmune and neurodegenerative diseases[1].

  • CAS Number: 1124381-69-6
  • MF: C16H15F3N6O
  • MW: 364.33
  • Catalog: Apoptosis
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NG25 trihydrochloride

NG25 trihydrochloride is a type II kinase inhibitor that inhibits MAP4K2 and TAK1. It also inhibits the Src family kinases Src and LYN and Abl family kinases as well as CSK, FER, and p38α. NG 25 prevents TNF-α-induced IKKα/β phosphorylation and IκB-α degradation in L929 cells. It inhibits secretion of IFN-α and IFN-β induced by CpG type B and CL097, respectively. NG 25 decreases cell viability of HCT116KRASWT, and to a greater degree of HCT116KRASG13D, colorectal cancer cells in a concentration-dependent manner. It also reduces tumor growth and increases the number of TUNEL-positive tumor cells in a CT26KRASG12D mouse orthotopic model of colorectal cancer.

  • CAS Number: 2108554-00-1
  • MF: C29H33Cl3F3N5O2
  • MW: 646.96
  • Catalog: MAP3K
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GS-444217

GS-444217 is a potent and selective ATP-competitive inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of 2.87±0.85 nM[1].

  • CAS Number: 1262041-49-5
  • MF: C23H21N7O
  • MW: 411.46
  • Catalog: MAP3K
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

B-Raf inhibitor

TAK1/MAP4K2 inhibitor 1 is a potent dual TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2) inhibitor, with IC50s of 41.1 nM and 18.2 nM, respectively.

  • CAS Number: 1315330-11-0
  • MF: C29H31F3N6O2
  • MW: 552.59100
  • Catalog: MAP3K
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

torilin

Torilin is a sesquiterpene with antimicrobial, anticancer, and anti-inflammatory properties. Torilin inhibits LPS-induced NO release, as well as inhibiting iNOS, PGE2, COX-2, NF-α, IL-1β, IL-6, and GM-CSF. Torilin suppresses NF-kB and AP-1 translocation, inhibits TAK1 kinase activation. Subsequently results suppression of MAPK-mediated JNK, p38, ERK1/2, and AP-1 (ATF-2 and c-jun) activation and IKK-mediated I-κBα degradation, p65/p50 activation, and translocation[1].

  • CAS Number: 13018-10-5
  • MF: C22H32O5
  • MW: 376.49
  • Catalog: MAP3K
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 469.2±45.0 °C at 760 mmHg
  • Melting Point: 78-79℃ (methanol )
  • Flash Point: 201.0±28.8 °C

NG25

NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC50s of 149 nM and 21.7 nM, respectively.

  • CAS Number: 1315355-93-1
  • MF: C29H30F3N5O2
  • MW: 537.57600
  • Catalog: MAP3K
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DLK-IN-1

DLK-IN-1 is a selective inhibitor of dual leucine zipper kinase (DLK, MAP3K12), with a Ki of 3 nM. DLK-IN-1 retains excellent CNS penetration and is well tolerated following multiple days of dosing at concentrations that exceed those required for DLK inhibition in the brain. DLK-IN-1 has activity in a model of Alzheimer’s Disease.

  • CAS Number: 1620574-24-4
  • MF: C20H24F3N5O2
  • MW: 423.43
  • Catalog: MAP3K
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TC ASK 10

TC ASK 10 (Compound 10) is a potent, selective and orally active apoptosis signal-regulating kinase 1 (ASK1) inhibitor with an IC50 of 14 nM. The inhibitory activities of TC ASK 10 towards other representative panel of kinases are less than 50%, except for ASK2 (IC50 of 0.51 μM)[1].

  • CAS Number: 1005775-56-3
  • MF: C21H23Cl2N5O
  • MW: 432.346
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Selonsertib(GS-4997)

Selonsertib is an apoptosis signal-regulating kinase 1 (ASK1) inhibitor with a pIC50 of 8.3±0.07.

  • CAS Number: 1448428-04-3
  • MF: C24H24FN7O
  • MW: 445.492
  • Catalog: MAP3K
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PF-05381941

PF-05381941 (PF 05381941, PF05381941) is a potent, dual TAK1/p38a inhibitor with IC50 of 156/186 nM respectively, with good kinome selectivity against 50 representative kinases; inhibits LPS-stimulated release of TNF-α from human peripheral mononuclear cells with IC50 of 8 nM.

  • CAS Number: 1474022-02-0
  • MF: C27H26N6O2
  • MW: 466.545
  • Catalog: MAP3K
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ASK1-IN-3

ASK1-IN-3 is a potent and selective ASK1 kinase inhibitor with IC50 of 33.8 nM, as well as inhibits several cell cycle regulating kinases. ASK1-IN-3 has strong HepG2 cancer cells apoptosis induction and potent cell cycle arrest activities[1].

  • CAS Number: 2426705-19-1
  • MF: C18H18N8O2
  • MW: 378.39
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Takinib

Takinib is a potent and selective TAK1 inhibitor with an IC50 of 9.5 nM.

  • CAS Number: 1111556-37-6
  • MF: C18H18N4O2
  • MW: 322.36
  • Catalog: MAP3K
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SW-083688

SW-083688 (SW083688) is a potent, highly selective TAOK2 (Thousand-And-One Kinase 2, MAP3K17) inhibitor with IC50 of 1.3 uM; increases the abundance of p62 and inhibits autophagy; TAOK2 is an activator of p38 MAP kinase cascade that is up-regulated in response to environmental stresses, and a potential cancer therapeutic target.

  • CAS Number: 422281-45-6
  • MF: C23H25N3O5S
  • MW: 455.529
  • Catalog: MAP3K
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NQDI 1

NQDI-1 inhibits apoptosis signal-regulating kinase 1 (ASK1) with a Ki of 500 nM and an IC50 of 3 μM.

  • CAS Number: 175026-96-7
  • MF: C19H13NO4
  • MW: 319.311
  • Catalog: MAP3K
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 581.4±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 305.4±30.1 °C

TAK1-IN-3

TAK1-IN-3 is a potent ATP-competitive TAK1 inhibitor.

  • CAS Number: 494772-87-1
  • MF: C16H19N3O2S
  • MW: 317.40600
  • Catalog: MAP3K
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GNE-3511

GNE-3511 is a dual leucine zipper kinase (DLK) inhibitor with a Ki of 0.5 nM.

  • CAS Number: 1496581-76-0
  • MF: C23H26F2N6O
  • MW: 440.489
  • Catalog: MAP3K
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 579.0±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 304.0±30.1 °C