TLR

阻害剤の選択性比較

カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S4157 Chloroquine diphosphate 100 mg/mL <1 mg/mL <1 mg/mL
S0716 E6446 <1 mg/mL <1 mg/mL '''90 mg/mL
S8562 IRAK4-IN-2 <1 mg/mL 30 mg/mL '''''<1 mg/mL
S9234 Schaftoside -1 mg/mL 100 mg/mL -1 mg/mL
S6597 TLR2-IN-C29 <1 mg/mL 57 mg/mL 6 mg/mL
S6573 MD2-IN-1 <1 mg/mL 72 mg/mL 2 mg/mL
S6999 Chloroquine (NSC-187208) <1 mg/mL 64 mg/mL ''''64 mg/mL
S6934 AMG-9810 <1 mg/mL 67 mg/mL 25 mg/mL
S7455 Resatorvid (TAK-242) <1 mg/mL 72 mg/mL ''''72 mg/mL
S0139 MD2-TLR4-IN-1 <1 mg/mL 84 mg/mL '5 mg/mL
S4430 Hydroxychloroquine Sulfate (NSC 4375) 67 mg/mL <1 mg/mL ''<1 mg/mL
S6719 E6446 dihydrochloride 100 mg/mL 3 mg/mL '2 mg/mL
S3924 Ginsenoside Rb1 -1 mg/mL 100 mg/mL -1 mg/mL
S8677 Cu-CPT22 <1 mg/mL 72 mg/mL 9 mg/mL
S9937 CU-CPD107 <1 mg/mL 80 mg/mL 80 mg/mL
S0002 IAXO-102 <1 mg/mL 15 mg/mL 100 mg/mL
S0822 TLR4-IN-C34 78 mg/mL 78 mg/mL ''78 mg/mL
S4461 CU-CPT-8m <1 mg/mL 6 mg/mL '''<1 mg/mL
S9730 CU-CPT9a <1 mg/mL 53 mg/mL '''''''10 mg/mL
S7221 Vesatolimod (GS-9620) <1 mg/mL 1 mg/mL '<1 mg/mL
S0494 SM 324405 <1 mg/mL 77 mg/mL <1 mg/mL
S0078 1V209 (TLR7 agonist T7) <1 mg/mL 72 mg/mL <1 mg/mL
S8133 Resiquimod (R-848) <1 mg/mL 63 mg/mL '''''21 mg/mL
S9623 Telratolimod <1 mg/mL <1 mg/mL '13 mg/mL
S2952 SM-276001 ' mg/mL
S7161 Motolimod (VTX-2337) <1 mg/mL 55 mg/mL 15 mg/mL
S2979 CU-T12-9 <1 mg/mL 72 mg/mL '''5 mg/mL

亜型選択性的な製品

TLR製品

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
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).

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.

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.

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.

S6573

MD2-IN-1

MD2-IN-1 is an inhibitor of Myeloid differentiation protein 2 (MD2) with a KD value of 189 μM.

S6999

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.

S6934

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.

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.

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.

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.

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).

S9937

CU-CPD107

CU-CPD107 is a selective, dual-activity small-molecule which demonstrated differential activity against the TLR8 agonists and ssRNA ligands. In the presence of R848, CU-CPD107 acts as a TLR8 signaling inhibitor (IC50=13.7 μM). In the presence of ssRNA, CU-CPD107 shows synergistic agonist activities, while CU-CPD107 alone is unable to influence TLR8 signaling.

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.

S0822

TLR4-IN-C34

TLR4-IN-C34 (TLR4-C34, C34, TLR4-C34-IN) is a potent and selective antagonist of Toll-like receptor 4 (TLR4). TLR4-IN-C34 reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis.

S4461

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

CU-CPT9a

CU-CPT9a is a potent and specific antagonist of Toll-like receptor 8 (TLR8) with IC50 of 0.5 nM.

S7221

Vesatolimod (GS-9620)

Vesatolimod (GS-9620) is a potent and selective orally active small molecule agonist of Toll-like receptor 7.

S0494

SM 324405

SM 324405 (compound 9e) is a potent and selective Toll-like receptor 7 (TLR7) agonist with EC50 of 50 nM.

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.

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.

S2979

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.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
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).

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.

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.

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.

S6573

MD2-IN-1

MD2-IN-1 is an inhibitor of Myeloid differentiation protein 2 (MD2) with a KD value of 189 μM.

S6999

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.

S6934

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.

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.

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.

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.

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).

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S9937

CU-CPD107

CU-CPD107 is a selective, dual-activity small-molecule which demonstrated differential activity against the TLR8 agonists and ssRNA ligands. In the presence of R848, CU-CPD107 acts as a TLR8 signaling inhibitor (IC50=13.7 μM). In the presence of ssRNA, CU-CPD107 shows synergistic agonist activities, while CU-CPD107 alone is unable to influence TLR8 signaling.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
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.

S0822

TLR4-IN-C34

TLR4-IN-C34 (TLR4-C34, C34, TLR4-C34-IN) is a potent and selective antagonist of Toll-like receptor 4 (TLR4). TLR4-IN-C34 reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis.

2022, 838(Pt 2):155825

S4461

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

CU-CPT9a

CU-CPT9a is a potent and specific antagonist of Toll-like receptor 8 (TLR8) with IC50 of 0.5 nM.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S7221

Vesatolimod (GS-9620)

Vesatolimod (GS-9620) is a potent and selective orally active small molecule agonist of Toll-like receptor 7.

2022, 18(3):e1010354

2020, 179:112987

2019, 10(1):387

S0494

SM 324405

SM 324405 (compound 9e) is a potent and selective Toll-like receptor 7 (TLR7) agonist with EC50 of 50 nM.

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.

2022, 18(4):e2103552

2021, 33(51):e2104362

2021, 13(3)365

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.

2021, 35(7):109143

2020, 1

2020, 179:112987

S2979

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.

Tags: TLR inhibitor|TLR agonist|TLR activator|TLR inducer|TLR antagonist|TLR signaling pathway|TLR assay kit