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Immunology/Inflammation

Aryl Hydrocarbon Receptor

Immunology/Inflammation related

NOD-like Receptor (NLR)

Prostaglandin Receptor

Reactive Oxygen Species

Thrombopoietin Receptor

MyD88

MyD88 (Myeloid differentiation primary response gene 88) is a protein that is encoded by the MYD88 gene in humans. Available evidence suggests that MYD88 is dispensable for human resistance to common viral infections and to all but a few pyogenic bacterial infections, demonstrating a major difference between mouse and human immune responses. MyD88 is an essential adaptor protein in the IL-1R1 signaling pathway. MyD88 may define a family of signal transduction molecules with an ancestral function in the activation of the immune system. MyD88 functions as a pure adaptor linking the IL-1R1 to downstream IRAK kinases. Mutation in MYD88 at position 265 leading to a change from leucine to proline have been identified in many human lymphomas including ABC subtype of Diffuse Large B-cell Lymphoma and Waldenstrom's Macroglobulinemia.

Filter HomeSignaling PathwaysImmunology/InflammationMyD88

Schaftoside

Shaftoside, APIGENIN-6-GLUCOSIDE-8-ARABINOSIDE

T389851938-32-0

Schaftoside (APIGENIN-6-GLUCOSIDE-8-ARABINOSIDE) has antioxidant and anticancer activity.

Antioxidant Autophagy Dynamin Mitochondrial Metabolism MyD88 TLR

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Cited

Heclin

T24136890605-54-6

Heclin is an inhibitor of HECT E3 ubiquitin ligase that acts by inhibiting Smurf2, Nedd4, and WWP1 with IC50 values of 6.8, 6.3, and 6.9 μM, respectively.

Akt E1/E2/E3 Enzyme MyD88 NEDD4-1

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EM 163

T411421206480-93-4In house

EM 163 is a TIR-TIR interaction inhibitor, which is a TIR (Toll/interleukin-1 receptor) structural domain mimic of the MyD88 protein. EM 163 targets the TIR structural domain in the IL-1 receptor and blocks the interaction with MyD88. EM 163 inhibits the production of inflammatory cytokines in vivo caused by staphylococcal enterotoxin B (SEB). EM 163 protects mice from SEB shock-induced death. In rat hippocampal neurons in vitro, EM 163 blocked the activation of p38 and the inhibitory effect of IL-1β on chemically induced long-term potentiation (LTP)-triggered protein synthesis.

IFNAR IL Receptor MyD88 p38 MAPK TNF

$123

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T6167923

T130632437475-16-4

T6167923 is a potent, selective inhibitor of MyD88-dependent signaling pathways. It achieves this by directly binding to the Toll/IL1 receptor (TIR) domain of MyD88, preventing MyD88 homodimer formation. Subsequently, T6167923 impedes NF-κB driven Staphylococcus enterotoxin AP (SEAP) activity and boasts improved anti-inflammatory effects, with IC50s values of 2.7 μM for IFN-γ, 2.9 μM for IL-1β, and 2.66 μM each for IL-6 and TNF-α, demonstrating its efficacy across multiple inflammatory mediators [1].

MyD88

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TJ-M2010-5

T97651357471-57-8

TJ-M2010-5 is a MyD88 inhibitor that binds to the TIR domain to interfere with its homodimerization and suppress MyD88 signaling. TJ-M2010-5 can be used in myocardial [ischemia/reperfusion] injury studies.

MyD88

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CL075

CL-075, 3M002

T27034256922-53-9

CL075 (3M002) is a selective TLR8 agonist with immunomodulatory activity, triggering the MyD88-dependent signaling pathway and activating NF-κB and IRF7 to elicit the production of inflammatory cytokines and type I interferon (IFN).

MyD88 NF-κB TLR

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MyD88-IN-1

T773532911609-80-6

MyD88-IN-1 is a potent MyD88 inhibitor with anti-inflammatory activity, inhibiting downstream pathways such as the NF-κB pathway of the Toll-like receptor (TLR) and interleukin-1 (IL-1) receptor family. MyD88-IN-1 may be used in the study of cancer and inflammation treatment.

IL Receptor MyD88 NF-κB TLR

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Smurf1-IN-A01

A01

T169041007647-73-5

Smurf1-IN-A01 (A01) is a ubiquitin ligase Smad ubiquitination regulatory factor-1 inhibitor (Kd: 3.664 nM) that enhances BMP-2 responsiveness by preventing Smurf1-mediated Smad1/5 degradation.

Estrogen Receptor/ERR HSP Interleukin MyD88 NF-κB Others

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Chloranil

p-Chloranil

T80673118-75-2

Chloranil (tetrachloro-p-benzoquinone) triggers inflammation and neurological dysfunction through Toll-like receptor 4 signaling and can be used to model inflammation in mice.

MyD88 TLR

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UF010

T3205537672-41-6

UF010 is a potent and selective HADC inhibitor with IC50 ~0.06 μM, 0.1 μM, 0.5 μM and 1.5 μM for HDACs 3, 2, 1 and 8, respectively.

HDAC Interleukin JAK MyD88 NF-κB TLR

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DHBP

Benzoresorcinol

T7338L131-56-6

DHBP (Benzoresorcinol) is an WalKR TCS activator. It works via targeting walk and selectively promoting the lysostaphin-induced lysis activity of the Newman wild-type strain.

IRAK MyD88 NF-κB Others Reactive Oxygen Species TLR

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TLR1

T13932566914-00-9

TLR1 is a cell-penetrating Toll/IL-1 receptor/resistance (TIR) domain/BB-Loop mimic and inhibits IL-1 receptor-mediated responses.

MyD88

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D228

D 228

T2005512676188-98-8

D228, a natural product from Chimonanthus salicifolius, is an orally available anti-inflammatory agent with favorable inhibitory activity on B and T lymphocytes, down-regulation of MyD88/TRAF6/p38 and up-regulation of IL-10 to reduce inflammation, and can be used for the treatment of inflammatory bowel disease (IBD).

IL Receptor MyD88 p38 MAPK

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Emavusertib Tosylate

T2027602376399-41-4

Emavusertib Tosylate (also known as CA-4948) is a potent inhibitor of IRAK4/FLT3 with demonstrated antitumor activity. In cell lines such as ABC DLBCL and AML, CA-4948 exhibits strong cellular efficacy. Among 329 evaluated kinases, it shows medium to high selectivity. The compound has excellent oral bioavailability and favorable pharmacokinetic properties in ADME and PK profiles. In preclinical models involving mice, rats, and dogs, CA-4948 demonstrated good oral bioavailability and displayed over 90% tumor growth inhibition in relevant tumor models, correlating well with in vivo pharmacodynamic regulation.

Apoptosis FLT IRAK MyD88 NF-κB

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10-14 weeks

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MyD88-IN-2

T204323

MyD88-IN-2 (compound A5S) is a MyD88 inhibitor with a Kd value of 15 μM. It demonstrates protective effects in mouse models of acute lung injury induced by LPS and sepsis.

MyD88

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Pepinh-MYD TFA

T205137

Pepinh-MYD TFA is a MyD88 inhibitor that features domain sequences from MyD88TIR and a protein transduction sequence, allowing it to penetrate cell membranes. By disrupting MyD88-mediated TLR pathway signaling, it inhibits related immune responses. Pepinh-MYD TFA shows potential for investigating MyD88's role in viral infections.

MyD88

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Anti-inflammatory agent 88

T210206

Anti-inflammatory agent 88 (compound 6) is a carbazole derivative found in marine Streptomyces with anti-inflammatory properties. It exerts its effects by inhibiting pro-inflammatory factors and enhancing the expression of anti-inflammatory factors within the Myd88/Nf-κB pathway. This compound holds potential for the development of anti-inflammatory drugs.

MyD88 NF-κB

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Myristoylated ARF6 (2-13)

TP3490

Myristoylated ARF6 (2-13) inhibits the MyD88–ARNO–ARF6 signaling axis by inactivating ARF6.

GTPase MyD88

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Emavusertib Phosphate

T2028292376399-38-9

Emavusertib Phosphate (also known as CA-4948) is a potent inhibitor of IRAK4 and FLT3, exhibiting antitumor activity. In ABC DLBCL and AML cell lines, it demonstrates significant cellular efficacy. Furthermore, CA-4948 shows moderate to high selectivity across a panel of 329 kinases and possesses favorable ADME and PK profiles, including good oral bioavailability in mice, rats, and dogs. It achieves over 90% tumor growth inhibition in relevant tumor models and correlates excellently with in vivo PD modulation.

Apoptosis FLT IRAK MyD88 NF-κB

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10-14 weeks

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Pepinh-MYD

TP28361421052-89-2

Pepinh-MYD, a MyD88 inhibitor, incorporates both a domain sequence from MyD88 TIR and a protein transduction sequence to facilitate cell membrane penetration. This compound disrupts MyD88-mediated TLR signaling pathways, effectively inhibiting associated immune responses. Its design is particularly useful for investigating MyD88's function in viral infections.

MyD88

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P53/TLR2 modulator-1

T206433

P53/TLR2 modulator-1 (Compound Z9) is an agent that targets both the P53 pathway and TLR2, exhibiting radioprotective properties. It mitigates apoptosis by inhibiting radiation-induced expression of P53 and Bax. Concurrently, it enhances the TLR2 pathway by upregulating downstream proteins MyD88 and P65, which promotes secretion of cytokines like IL-6, providing radioprotective effects. P53/TLR2 modulator-1 shows significant radioprotective activity in AHH-1 and HUVECs cells, enhances survival rates in C57BL/6J mice exposed to lethal radiation doses, and alleviates radiation-induced damage to their hematopoietic system, intestinal villi, and spleen. It is applicable for research on radiation-related diseases.

Apoptosis Bcl-2 Family Interleukin MDM-2/p53 MyD88 TLR

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TLR8 antagonist-1

T2040091111460-83-3

TLR8 antagonist 1 (Compound 10) is a selective antagonist that can inhibit TLR8 mediated inflammation and signaling pathways. TLR8 antagonist 1 reduces MyD88 recruitment and inhibits NF - κ B and IRF pathways, exhibiting certain anti-inflammatory activity.

MyD88 NF-κB TLR

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7-10 days

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ST 2825

T16937894787-30-5

ST 2825 is a specific MyD88 dimerization inhibitor that blocks IL-1β-mediated activation of NF-κB transcriptional activity.

MyD88 Others

$1,970

8-10 weeks

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Emavusertib Mesylate

T2027632376399-40-3

Emavusertib Mesylate (also known as CA-4948) is a potent inhibitor of IRAK4 and FLT3, demonstrating antitumor activity. In cell lines of ABC DLBCL and AML, CA-4948 shows significant cellular activity. Moreover, it exhibits moderate to high selectivity in screening assays of 329 kinases and has impressive pharmacokinetic and pharmacodynamic profiles (ADME and PK), with good oral bioavailability in mice, rats, and dogs. In pertinent tumor models, CA-4948 achieves over 90% tumor growth inhibition and shows excellent correlation with in vivo PD modulation.

Apoptosis FLT IRAK MyD88 NF-κB

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10-14 weeks

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