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
S8562 CA-4948 <1 mg/mL 30 mg/mL <1 mg/mL
S6597 TLR2-IN-C29 <1 mg/mL 57 mg/mL 6 mg/mL
S0139 MD2-TLR4-IN-1 <1 mg/mL 84 mg/mL 5 mg/mL
S6573 MD2-IN-1 <1 mg/mL 72 mg/mL 2 mg/mL
S7455 Resatorvid (TAK-242) <1 mg/mL 72 mg/mL 72 mg/mL
S4430 Hydroxychloroquine Sulfate 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
S0002 IAXO-102 <1 mg/mL 15 mg/mL 100 mg/mL
S6934 AMG-9810 <1 mg/mL 67 mg/mL 25 mg/mL
S7221 GS-9620 <1 mg/mL 1 mg/mL <1 mg/mL
S0494 SM 324405 <1 mg/mL 77 mg/mL <1 mg/mL
S9623 Telratolimod <1 mg/mL <1 mg/mL 13 mg/mL
S0078 1V209 (TLR7 agonist T7) <1 mg/mL 72 mg/mL <1 mg/mL
S8133 Resiquimod <1 mg/mL 63 mg/mL 21 mg/mL
S7161 Motolimod (VTX-2337) <1 mg/mL 55 mg/mL 15 mg/mL

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).

S8562

CA-4948

CA-4948 is a reversible kinase inhibitor that modulates IRAK4 function in both the toll-like receptor (TLR) and interleukin 1 receptor (IL-1R) signaling cascades, and demonstrates pharmacodynamic and antitumor activity in in vitro and in vivo nonclinical models. CA-4948 also inhibits FLT3.

S6597

TLR2-IN-C29

TLR2-IN-C29 (C29) is a Toll-like receptor 2 (TLR2) inhibitor that inhibits TLR2/1 and TLR2/6 signaling.

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.

S6573

MD2-IN-1

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

S7455

Resatorvid (TAK-242)

Resatorvid (TAK-242) is a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, blocking LPS-induced production of NO, TNF-α, IL-6, and IL-1β in macrophages with IC50 values of 1-11 nM. Resatorvid inhibits autophagy.

S4430

Hydroxychloroquine Sulfate

Hydroxychloroquine Sulfate (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).

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.

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.

S7221

GS-9620

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.

S9623

Telratolimod

Telratolimod is an agonist of toll-like receptor 7 (TLR-7) and toll-like receptor 8 (TLR-8) with antitumor activity.

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

Resiquimod 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.

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.

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).

S8562

CA-4948

CA-4948 is a reversible kinase inhibitor that modulates IRAK4 function in both the toll-like receptor (TLR) and interleukin 1 receptor (IL-1R) signaling cascades, and demonstrates pharmacodynamic and antitumor activity in in vitro and in vivo nonclinical models. CA-4948 also inhibits FLT3.

S6597

TLR2-IN-C29

TLR2-IN-C29 (C29) is a Toll-like receptor 2 (TLR2) inhibitor that inhibits TLR2/1 and TLR2/6 signaling.

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.

S6573

MD2-IN-1

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

S7455

Resatorvid (TAK-242)

Resatorvid (TAK-242) is a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, blocking LPS-induced production of NO, TNF-α, IL-6, and IL-1β in macrophages with IC50 values of 1-11 nM. Resatorvid inhibits autophagy.

S4430

Hydroxychloroquine Sulfate

Hydroxychloroquine Sulfate (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
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.

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.

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

GS-9620

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

2020, 179:112987

2019, 10(1):387

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.

S9623

Telratolimod

Telratolimod is an agonist of toll-like receptor 7 (TLR-7) and toll-like receptor 8 (TLR-8) with antitumor activity.

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

Resiquimod 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.

2020, 15;8(2):E186

2020, 11(1):3521

2020, 469:173-185

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.

2020, 1

2020, 179:112987

2020, 4(2):93-107