MyD88 Inhibitor

TLR8 antagonist-1 (Compound 10) is a selective TLR8 antagonist. TLR8 antagonist-1 can inhibit TLR8-mediated inflammation and signaling pathways, reduce the recruitment of MyD88, and inhibit the NF-κB and IRF pathways. TLR8 antagonist-1 has anti-inflammatory activity.

Azaleatin is an orally active inhibitor of hQC, NS2B-NS3 protease and E. coli β-glucuronidase, with IC₅₀ values of 1.1 μM, 38.00 μg/mL and 0.57 μM, respectively. Azaleatin inhibits the activities of NF-κB, MyD88, JAK1, TLR4, STAT3, IL-1β, IL-6, COX-2, TNF-α and β-glucuronidase, blocks pro-inflammatory signaling pathways, reduces the levels of ROS, MDA and uric acid, elevates the levels of GPx, GSR, GST, SOD, CAT, HO-1 and GSH, scavenges free radicals and exerts reducing capacity. Azaleatin inhibits the expression of pro-apoptotic proteins Bax, Caspase-9 and Caspase-3, and upregulates the expression of anti-apoptotic protein Bcl-2. Azaleatin reduces the levels of cardiac injury markers, restores cardiac histological structure, inhibits Aβ aggregation, dengue protease activity, hepatic stellate cell proliferation and cancer cell growth, and also exhibits antibacterial activity. Azaleatin can be used in studies related to subchronic cardiotoxicity, Alzheimer's disease, dengue fever, hyperuricemia, liver fibrosis, gastric cancer and bacterial infections.

Arjunolic acid is an orally active, multifunctional bioactive compound. Arjunolic acid exhibits free radical scavenging activity, as well as fungal and bacterial activities. Arjunolic acid induces apoptosis (Apoptosis) in various cancer cells. Arjunolic acid protects hepatocytes against induced oxidative stress and apoptosis by reducing reactive oxygen species and inhibiting NF-κB activation. Arjunolic acid regulates pancreatic dysfunction in type 2 diabetic rats by blocking the activation of the TLR-4/MyD88 and canonical Wnt pathways. Arjunolic acid inhibits neuroinflammation and ameliorates depressive behaviors via the SIRT1/AMPK/Notch1 signaling pathway in microglia. Arjunolic acid improves Crohn's disease-like colitis by restoring gut microbiota composition and inhibiting TLR4 signaling. Arjunolic acid suppresses osteosarcoma progression by inhibiting Wnt3a-mediated M2 polarization of macrophages. Arjunolic acid ameliorates diabetic retinopathy via the autophagy pathway regulated by AMPK/mTOR/HO-1. Arjunolic acid is applicable to research related to type 2 diabetes, organ toxicity, depression, Crohn's disease, osteosarcoma, diabetic retinopathy, and testicular dysfunction.

Salvianolic acid D is a depside. Salvianolic acid D can be isolated from Salvia miltiorrhiza (Danshen). Salvianolic acid D promotes the expression of Bcl-2, and inhibits the expressions of Bax, Cleaved caspase-3 and -9. Salvianolic acid D reduces the expression levels of TLR4, MyD88 and TRAF6 proteins both in vitro and in vivo, and significantly inhibits the nuclear translocation of NF-κB. Salvianolic acid D inhibits the cytoplasmic translocation of HMGB1. Salvianolic acid D suppresses inflammatory responses and alleviates cerebral ischemia-reperfusion injury. Salvianolic acid D serves as a potential antiplatelet active component.

MyD88-IN-3 is an orally active, selective MyD88 Inhibitor. MyD88-IN-3 specifically targets the TIR domain of MyD88 (K_D = 28.5 μM), thereby preventing MyD88 self-polymerization and interaction with TLRs, which suppresses the activation of MAPK and NF-κB pathways. MyD88-IN-3 demonstrates significant anti-inflammatory efficacy and effectively mitigates Acute Lung Injury (ALI) symptoms in CLP (cecal ligation and puncture) and Lipopolysaccharides (HY-D1056) (LPS)-induced ALI models. MyD88-IN-3 can be used for the study of ALI.

Raffinose (Standard) is the analytical standard of Raffinose. This product is intended for research and analytical applications. Raffinose (Melitose) regulates intestinal flora, inhibits TLR4-MyD88-NF-κB signaling pathway, and activates Nrf2 signaling pathway. Raffinose exhibits anti-inflammatory, antioxidant, and immunomodulatory activities. Raffinose is orally active.

MYD88 Human Pre-designed siRNA Set A contains three designed siRNAs for MYD88 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

Grossamide is a natural product that can be isolated from fructus cannabis, the dried fruit of Cannabis sativa L.. Grossamide has anti-neuroinflammatory effects.

D228 is an orally active antiinflammatory agent. D228 reduces ConA induced T lymphocyte cell proliferation (IC₅₀: 42.85 μM) and LPS induced B lymphocyte cell proliferation (IC₅₀: 3.15 μM). D228 is effective against inflammatory bowel disease (IBD). D228 alleviates the DSS (HY-116282C)-induced inflammation response in the IBD model by downregulating the MyD88/TRAF6/p38 signaling.

TSI-13-57 is a pan-TLR inhibitor (IC₅₀: 2.7 μM, 6.03 μM, 7.37 μM, 6.38 μM for TLR9, TLR7, TLR2, TLR4, respectively). TSI-13-57 inhibits homodimerization of the TIR domains of MyD88. TSI-13-57 reduces systemic inflammatory responses in LPS-induced mice.

Emavusertib hydrochloride (CA-4948 tosylate) is the hydrochloride salt form of Emavusertib (HY-135317). Emavusertib hydrochloride is an orally active inhibitor for IRAK4 (IC₅₀=57 nM) and FLT3. Emavusertib hydrochloride inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib hydrochloride exhibits antitumor activity in mouse model.

Myd88 Rat Pre-designed siRNA Set A contains three designed siRNAs for Myd88 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

LYRM03 is a derivative of Ubenimex (HY-B0134) and a Aminopeptidase N inhibitor. LYRM03 is isolated from Streptomyces HCCB10043. LYRM03 inhibits TLR4, MyD88, NLRP3, ASC, NF-κB and p38 MAPK, stabilizes IκB, and suppresses LPS-induced expression of iNOS and COX-2. LYRM03 reduces the levels of inflammatory cytokines and oxidative stress markers, and alleviates pulmonary edema. LYRM03 exhibits anticancer activity against breast cancer. LYRM03 has anti-inflammatory activity. LYRM03 can be used in the research of acute lung injury and breast cancer.

Antimicrobial Peptide YD is an Antimicrobial peptide. Antimicrobial Peptide YD attenuates the TLR4/MYD88/NF-κB signaling pathway, inhibits ROS production, upregulates the expression of antioxidant enzymes, reduces the levels of inflammation-related factors, and prevents the downregulation of E-cadherin and upregulation of Vimentin. Antimicrobial Peptide YD exhibits activity against Gram-positive bacteria, Gram-negative bacteria, and multidrug-resistant bacteria. Antimicrobial Peptide YD possesses anti-inflammatory, antifibrotic, and antioxidant effects. Antimicrobial Peptide YD can be used in pulmonary fibrosis research.

Myd88 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Myd88 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

Phoenixin-14 (PNX-14) TFA is an endogenous neuropeptide with multiple biological activities, and serves as the endogenous ligand of GPR173. Phoenixin-14 TFA reduces ROS production by inhibiting the HMGB1/TLR4/MyD88/NF-κB signaling axis, thereby exerting antioxidant and mitochondrial protective effects. Phoenixin-14 TFA inhibits FOXO3 phosphorylation by upregulating SIRT3 expression, suppresses apoptosis, and improves myocardial systolic/diastolic function. Phoenixin-14 TFA resists ferroptosis by activating the ATF4/SLC7A11/GPX4 axis; it activates ERK1/2 phosphorylation via GPR173. Phoenixin-14 TFA can be used in researches on neuroprotection, diabetes, cardiomyopathy, reproductive protection and so on.

Astringin (trans-Astringin) (Standard) is the analytical standard of Astringin (HY-N4093). This product is intended for research and analytical applications. Astringin (trans-Astringin) is an orally active natural flavonoid compound. Astringin can inhibit the production of oxidative stress, inflammatory factors, etc. Astringin has multiple activities such as anti-oxidation, anti-inflammation, and anti-apoptosis. Astringin is also an inhibitor of ferroptosis. Astringin can be used in the research of diseases such as acute lung injury.

Dendrocandin U is a bibenzyl compound found in Dendrobium officinale that exhibits anti-inflammatory activity and α-glucosidase inhibitory effect (IC₅₀ = 9.46 mM). Dendrocandin U inhibits the expression of TLR4 and MyD88 in the TLR4/MyD88/NF-kB pathway, suppresses the phosphorylation of NF-kB p65 and I-kBα, and blocks the nuclear translocation of NF-kB p65. Dendrocandin U inhibits M1 polarization, NO secretion, and TNF-α release in alveolar macrophages, and reduces inflammatory morphological changes in macrophages. Dendrocandin U promotes neurite outgrowth in PC12 cells. Dendrocandin U can be used for research on inflammation-related diseases and type 2 diabetes.

LM9 is a potent, orally active MyD88 inhibitor. LM9 blocks TLR4/MyD88 binding, MyD88 homodimer formation, and TLR4/MyD88/NF-κB signaling pathway activation. LM9 prevents atherosclerosis by regulating inflammatory responses and oxidative stress in macrophages. LM9 efficiently mitigates inflammatory responses and fibrosis in obesity-induced cardiomyopathy. LM9 can be used for fibrosis and atherosclerosis research.

Myristoylated ARF6 (2-13) blocks MyD88–ARNO–ARF6–signaling axis by deactivating ARF6.