TLR

Inhibitory Selectivity

Isoform-specific Inhibitors

TLR Products

All (25) TLR Inhibitors (13) TLR Antagonists (4) TLR Agonists (8)

Catalog No.	Information	Product Use Citations	Product Validations
S4157	Chloroquine diphosphate Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs).	Gut, 2021, 70(5):890-899 Dev Cell, 2021, S1534-5807(21)00518-9 Theranostics, 2021, 11(2):700-714	NCI-H929 EV and miR-137 OE cells were treated with ATM activator Chloroquine Phosphate (CQ), specific ATM inhibitor KU-55933, and ATR inhibitor AZ20 for 12 hr. Immunoblotting showed the expression of p-ATM, p-Chk2, p-BRCA1, p-ATR and p-Chk1.
S0716	E6446 E6446 is an inhibitor of Toll-like receptor (TLR) 7 and 9 signaling in a variety of human and mouse cell types and inhibits DNA-TLR9 interaction in vitro.
S6999^New	Chloroquine (NSC-187208) Chloroquine (NSC-187208, Aralen, CHQ, CQ) is an antimalarial drug and autophagy/lysosome inhibitor. Chloroquine also suppresses Toll-like receptor-9 (TLR9) protein expression. Chloroquine is highly effective agianst SARS-CoV-2 (COVID-19) infection with EC50 of 1.13 μM in Vero E6 cells. Chloroquine has anti-HIV-1 activity.	Autophagy, 2021, 10.1080/15548627.2021.1912270 Front Cell Dev Biol, 2021, 9:670145 Virulence, 2021, 12(1):509-519
S8562	IRAK4-IN-2 IRAK4-IN-2 is a reversible kinase inhibitor that modulates IRAK4 function in both the toll-like receptor (TLR) and interleukin 1 receptor (IL-1R) signaling cascades.	Cancer Lett, 2021, 503:75-90 Cancer Lett, 2021, 503:75-90
S9234	Schaftoside Schaftoside, a bioactive compound found in the Herba Desmodii Styracifolii, exhibits pancreatic lipase inhibitory activity. Schaftoside inhibits the expression of TLR4 and Myd88. Schaftoside also decreases Drp1 expression and phosphorylation, and reduces mitochondrial fission.
S6597	TLR2-IN-C29 TLR2-IN-C29 (C29) is a Toll-like receptor 2 (TLR2) inhibitor that inhibits TLR2/1 and TLR2/6 signaling.	Int J Biol Macromol, 2021, 183:145-157
S6573	MD2-IN-1 MD2-IN-1 is an inhibitor of Myeloid differentiation protein 2 (MD2) with a KD value of 189 μM.	Br J Pharmacol, 2021, 10.1111/bph.15412
S7455	Resatorvid (TAK-242) Resatorvid (TAK-242, CLI-095) is a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, blocking LPS-induced production of NO, TNF-α and IL-6 in macrophages with IC50 of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF. Resatorvid inhibits autophagy.	FASEB J, 2021, 35(4):e21485 Int J Biol Macromol, 2021, 183:145-157 Front Pharmacol, 2021, 12:626949
S0139	MD2-TLR4-IN-1 MD2-TLR4-IN-1 (Compound 22m) is a potent inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4). MD2-TLR4-IN-1 (compound 22m) inhibits lipopolysaccharide (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in macrophages with IC50 of 0.89 μM and 0.53 μM, respectively.
S4430	Hydroxychloroquine Sulfate (NSC 4375) Hydroxychloroquine Sulfate (NSC 4375, HCQ) is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of autophagy and toll-like receptor (TLR) 7/9.	Autophagy, 2021, 1-14 Cell Rep, 2021, 35(1):108940 Cell Death Dis, 2021, 12(4):347	C, SA-beta gal staining results of A549-LKB1 cells treated by trametinib (30 nmol/L), radiotherapy (2 Gy), and HCQ (50 μmol/L). Cells were treated by HCQ and/or trametinib 4 hours prior to radiotherapy. Drugs were washed out 24 hours after radiotherapy. Cells were incubated for additional 48 hours before staining. D, Clonogenic survival assay of A549-LKB1 cells treated with trametinib (30 nmol/L) and HCQ (50 μmol/L).
S6719	E6446 dihydrochloride E6446 dihydrochloride is a specific Toll-like receptor 9 inhibitor.
S3924	Ginsenoside Rb1 Ginsenoside Rb1 (Gypenoside Ⅲ) is a protopanaxadiol that has diverse in vitro and in vivo effects, including neuroprotective, anti-inflammatory, and anti-obesity actions. Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65. Ginsenoside Rb1 reduces the expressions of TLR3, TLR4 and TRAF-6, and down-regulates the levels of TNF-α, IFN-β and iNOS.	J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S8677	Cu-CPT22 CU-CPT22 shows dose-dependent inhibitory effects blocking Pam3CSK4-induced TLR1/2 activation with an IC50 of 0.58 ± 0.09 µM while no significant inhibition to TLR2/6. It demonstrates minimal non-specific inhibition against a panel of 10 representative kinases (PDGFRB, MET, DDR2, SRC, MAPK1, PAK1, AKT1, PKC-γ, CAMK1, and PLK4).	Int Immunopharmacol, 2020, 79:106085
S0002	IAXO-102 IAXO-102 is an antagonist of TLR4 targeting both MD-2 and CD14 co-receptors. IAXO-102 inhibits MAPK and p65 NF-κB phosphorylation and downregulates the expression of TLR4 dependent proinflammatory proteins. IAXO-102 inhibits experimental abdominal aortic aneurysm (AAA) development.
S4461^New	CU-CPT-8m CU-CPT-8m (CPD1578) is a specific antagonist of toll-like receptor 8(TLR8) with IC50 of 67 nM and Kd of 220 nM.
S9730^New	CU-CPT9a CU-CPT9a is a potent and specific antagonist of Toll-like receptor 8 (TLR8) with IC50 of 0.5 nM.
S6934^New	AMG-9810 AMG-9810 is potent, competitive and selective vanilloid receptor 1 (TRPV1) antagonist and inhibits capsaicin activation with IC50 of 24.5 nM and 85.6 nM for human TRPV1 and rat TRPV1, repectively. AMG-9810 blocks all known modes of TRPV1 activation, including protons-, heat-, and endogenous ligands, such as anandamide, N-arachidonyl dopamine, and oleoyldopamine. AMG-9810 significantly reduces the mRNA expression of TLR2 and TLR4. AMG-9810 also promotes mouse skin tumorigenesis mediated through EGFR/Akt/mTOR signaling.
S7221	GS-9620 GS-9620 is a potent and selective orally active small molecule agonist of Toll-like receptor 7.	J Pharm Biomed Anal, 2020, 179:112987 Stem Cell Res Ther, 2019, 10(1):387 Nat Biomed Eng, 2018, 2(8):578-588
S0494	SM 324405 SM 324405 (compound 9e) is a potent and selective Toll-like receptor 7 (TLR7) agonist with EC50 of 50 nM.
S2979^New	CU-T12-9 CU-T12-9 is a specific agonist of Toll-like receptor (TLR) 1/2 with EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay. CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS.
S0078	1V209 (TLR7 agonist T7) 1V209 (T7, TLR7 agonist T7) is an agonist of Toll-like receptor 7 (TLR7) with anti-tumor effects. 1V209 can be used as vaccine adjuvants, enhances antigen specific humoral and cellular immune responses.
S8133	Resiquimod (R-848) Resiquimod (R-848, S28463) is an immune response modifier that acts as a potent TLR 7/TLR 8 agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α. Resiquimod reduces hepatitis C virus (HCV) infection. Phase 2.	Pharmaceutics, 2021, 13(3)365 bioRxiv, 2021, 2021.03.31.437792 Vaccines (Basel), 2020, 15;8(2):E186
S9623	Telratolimod Telratolimod (3M-052, MEDI9197) is an agonist of toll-like receptor 7 (TLR-7) and toll-like receptor 8 (TLR-8) with antitumor activity.
S2952	SM-276001 SM-276001 is a potent and selective agonist of TLR7 that induces antitumor immune responses. SM-276001 is an orally active interferon (IFN) inducer.
S7161	Motolimod (VTX-2337) Motolimod (VTX-2337) is a selective and potent Toll-like receptor 8 (TLR8) agonist with EC50 of 100 nM, > 50-fold selectivity over TLR7. Phase 2.	Cell Rep, 2021, 35(7):109143 J Leukoc Biol, 2020, 1 J Pharm Biomed Anal, 2020, 179:112987

Catalog No.	Information	Product Use Citations	Product Validations
S4157	Chloroquine diphosphate Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs).	Gut, 2021, 70(5):890-899 Dev Cell, 2021, S1534-5807(21)00518-9 Theranostics, 2021, 11(2):700-714	NCI-H929 EV and miR-137 OE cells were treated with ATM activator Chloroquine Phosphate (CQ), specific ATM inhibitor KU-55933, and ATR inhibitor AZ20 for 12 hr. Immunoblotting showed the expression of p-ATM, p-Chk2, p-BRCA1, p-ATR and p-Chk1.
S0716	E6446 E6446 is an inhibitor of Toll-like receptor (TLR) 7 and 9 signaling in a variety of human and mouse cell types and inhibits DNA-TLR9 interaction in vitro.
S6999^New	Chloroquine (NSC-187208) Chloroquine (NSC-187208, Aralen, CHQ, CQ) is an antimalarial drug and autophagy/lysosome inhibitor. Chloroquine also suppresses Toll-like receptor-9 (TLR9) protein expression. Chloroquine is highly effective agianst SARS-CoV-2 (COVID-19) infection with EC50 of 1.13 μM in Vero E6 cells. Chloroquine has anti-HIV-1 activity.	Autophagy, 2021, 10.1080/15548627.2021.1912270 Front Cell Dev Biol, 2021, 9:670145 Virulence, 2021, 12(1):509-519
S8562	IRAK4-IN-2 IRAK4-IN-2 is a reversible kinase inhibitor that modulates IRAK4 function in both the toll-like receptor (TLR) and interleukin 1 receptor (IL-1R) signaling cascades.	Cancer Lett, 2021, 503:75-90 Cancer Lett, 2021, 503:75-90
S9234	Schaftoside Schaftoside, a bioactive compound found in the Herba Desmodii Styracifolii, exhibits pancreatic lipase inhibitory activity. Schaftoside inhibits the expression of TLR4 and Myd88. Schaftoside also decreases Drp1 expression and phosphorylation, and reduces mitochondrial fission.
S6597	TLR2-IN-C29 TLR2-IN-C29 (C29) is a Toll-like receptor 2 (TLR2) inhibitor that inhibits TLR2/1 and TLR2/6 signaling.	Int J Biol Macromol, 2021, 183:145-157
S6573	MD2-IN-1 MD2-IN-1 is an inhibitor of Myeloid differentiation protein 2 (MD2) with a KD value of 189 μM.	Br J Pharmacol, 2021, 10.1111/bph.15412
S7455	Resatorvid (TAK-242) Resatorvid (TAK-242, CLI-095) is a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, blocking LPS-induced production of NO, TNF-α and IL-6 in macrophages with IC50 of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF. Resatorvid inhibits autophagy.	FASEB J, 2021, 35(4):e21485 Int J Biol Macromol, 2021, 183:145-157 Front Pharmacol, 2021, 12:626949
S0139	MD2-TLR4-IN-1 MD2-TLR4-IN-1 (Compound 22m) is a potent inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4). MD2-TLR4-IN-1 (compound 22m) inhibits lipopolysaccharide (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in macrophages with IC50 of 0.89 μM and 0.53 μM, respectively.
S4430	Hydroxychloroquine Sulfate (NSC 4375) Hydroxychloroquine Sulfate (NSC 4375, HCQ) is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of autophagy and toll-like receptor (TLR) 7/9.	Autophagy, 2021, 1-14 Cell Rep, 2021, 35(1):108940 Cell Death Dis, 2021, 12(4):347	C, SA-beta gal staining results of A549-LKB1 cells treated by trametinib (30 nmol/L), radiotherapy (2 Gy), and HCQ (50 μmol/L). Cells were treated by HCQ and/or trametinib 4 hours prior to radiotherapy. Drugs were washed out 24 hours after radiotherapy. Cells were incubated for additional 48 hours before staining. D, Clonogenic survival assay of A549-LKB1 cells treated with trametinib (30 nmol/L) and HCQ (50 μmol/L).
S6719	E6446 dihydrochloride E6446 dihydrochloride is a specific Toll-like receptor 9 inhibitor.
S3924	Ginsenoside Rb1 Ginsenoside Rb1 (Gypenoside Ⅲ) is a protopanaxadiol that has diverse in vitro and in vivo effects, including neuroprotective, anti-inflammatory, and anti-obesity actions. Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65. Ginsenoside Rb1 reduces the expressions of TLR3, TLR4 and TRAF-6, and down-regulates the levels of TNF-α, IFN-β and iNOS.	J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S8677	Cu-CPT22 CU-CPT22 shows dose-dependent inhibitory effects blocking Pam3CSK4-induced TLR1/2 activation with an IC50 of 0.58 ± 0.09 µM while no significant inhibition to TLR2/6. It demonstrates minimal non-specific inhibition against a panel of 10 representative kinases (PDGFRB, MET, DDR2, SRC, MAPK1, PAK1, AKT1, PKC-γ, CAMK1, and PLK4).	Int Immunopharmacol, 2020, 79:106085

Catalog No.	Information	Product Use Citations	Product Validations
S0002	IAXO-102 IAXO-102 is an antagonist of TLR4 targeting both MD-2 and CD14 co-receptors. IAXO-102 inhibits MAPK and p65 NF-κB phosphorylation and downregulates the expression of TLR4 dependent proinflammatory proteins. IAXO-102 inhibits experimental abdominal aortic aneurysm (AAA) development.
S4461^New	CU-CPT-8m CU-CPT-8m (CPD1578) is a specific antagonist of toll-like receptor 8(TLR8) with IC50 of 67 nM and Kd of 220 nM.
S9730^New	CU-CPT9a CU-CPT9a is a potent and specific antagonist of Toll-like receptor 8 (TLR8) with IC50 of 0.5 nM.
S6934^New	AMG-9810 AMG-9810 is potent, competitive and selective vanilloid receptor 1 (TRPV1) antagonist and inhibits capsaicin activation with IC50 of 24.5 nM and 85.6 nM for human TRPV1 and rat TRPV1, repectively. AMG-9810 blocks all known modes of TRPV1 activation, including protons-, heat-, and endogenous ligands, such as anandamide, N-arachidonyl dopamine, and oleoyldopamine. AMG-9810 significantly reduces the mRNA expression of TLR2 and TLR4. AMG-9810 also promotes mouse skin tumorigenesis mediated through EGFR/Akt/mTOR signaling.

Catalog No.	Information	Product Use Citations
S7221	GS-9620 GS-9620 is a potent and selective orally active small molecule agonist of Toll-like receptor 7.	J Pharm Biomed Anal, 2020, 179:112987 Stem Cell Res Ther, 2019, 10(1):387 Nat Biomed Eng, 2018, 2(8):578-588
S0494	SM 324405 SM 324405 (compound 9e) is a potent and selective Toll-like receptor 7 (TLR7) agonist with EC50 of 50 nM.
S2979^New	CU-T12-9 CU-T12-9 is a specific agonist of Toll-like receptor (TLR) 1/2 with EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay. CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS.
S0078	1V209 (TLR7 agonist T7) 1V209 (T7, TLR7 agonist T7) is an agonist of Toll-like receptor 7 (TLR7) with anti-tumor effects. 1V209 can be used as vaccine adjuvants, enhances antigen specific humoral and cellular immune responses.
S8133	Resiquimod (R-848) Resiquimod (R-848, S28463) is an immune response modifier that acts as a potent TLR 7/TLR 8 agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α. Resiquimod reduces hepatitis C virus (HCV) infection. Phase 2.	Pharmaceutics, 2021, 13(3)365 bioRxiv, 2021, 2021.03.31.437792 Vaccines (Basel), 2020, 15;8(2):E186
S9623	Telratolimod Telratolimod (3M-052, MEDI9197) is an agonist of toll-like receptor 7 (TLR-7) and toll-like receptor 8 (TLR-8) with antitumor activity.
S2952	SM-276001 SM-276001 is a potent and selective agonist of TLR7 that induces antitumor immune responses. SM-276001 is an orally active interferon (IFN) inducer.
S7161	Motolimod (VTX-2337) Motolimod (VTX-2337) is a selective and potent Toll-like receptor 8 (TLR8) agonist with EC50 of 100 nM, > 50-fold selectivity over TLR7. Phase 2.	Cell Rep, 2021, 35(7):109143 J Leukoc Biol, 2020, 1 J Pharm Biomed Anal, 2020, 179:112987

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