TNF-alpha

シグナル伝達経路

研究分野

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
S1029 Lenalidomide (CC-5013) <1 mg/mL 52 mg/mL <1 mg/mL
S1567 Pomalidomide <1 mg/mL 54 mg/mL '<1 mg/mL
S1193 Thalidomide <1 mg/mL 51 mg/mL 2 mg/mL
S8037 Necrostatin-1 <1 mg/mL 51 mg/mL ''<1 mg/mL
S2465 CPI-1189 <1 mg/mL 47 mg/mL 15 mg/mL
S7455 Resatorvid (TAK-242) <1 mg/mL 72 mg/mL '72 mg/mL
S4902 QNZ (EVP4593) <1 mg/mL 5 mg/mL <1 mg/mL
S8034 Apremilast (CC-10004) <1 mg/mL 92 mg/mL <1 mg/mL
S1623 Acetylcysteine 33 mg/mL 33 mg/mL '33 mg/mL
S4238 Cepharanthine <1 mg/mL 100 mg/mL <1 mg/mL
S8787 GSK'547 <1 mg/mL 29 mg/mL '<1 mg/mL
S8484 GSK2982772 <1 mg/mL 75 mg/mL '30 mg/mL
S8642 GSK'963 <1 mg/mL 46 mg/mL '46 mg/mL
S3785 Notoginsenoside R1 -1 mg/mL 100 mg/mL -1 mg/mL
S5913 Cambinol <1 mg/mL 21 mg/mL <1 mg/mL
S9396 Geraniin -1 mg/mL 100 mg/mL -1 mg/mL
S7609 GW4869 <1 mg/mL <1 mg/mL ''<1 mg/mL
S9090 Corilagin -1 mg/mL 100 mg/mL -1 mg/mL
S3138 Methylthiouracil <1 mg/mL 28 mg/mL <1 mg/mL
S8169 GSK481 <1 mg/mL 75 mg/mL <1 mg/mL
S7963 TIC10 <1 mg/mL 77 mg/mL '77 mg/mL
S5584 Citronellol 31 mg/mL <1 mg/mL -1 mg/mL
S3865 Taurochenodeoxycholic acid -1 mg/mL 99 mg/mL -1 mg/mL
S6643 R-7050 <1 mg/mL 18 mg/mL <1 mg/mL
S5851 4'-Methoxychalcone <1 mg/mL 48 mg/mL 2 mg/mL
S7942 Bioymifi <1 mg/mL 43 mg/mL <1 mg/mL
S1537 DMXAA (Vadimezan) <1 mg/mL 7 mg/mL ''<1 mg/mL

亜型選択性的な製品

TNF-alpha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
A2010

Adalimumab

Adalimumab is the first fully human, recombinant IgG1 monoclonal antibody that specifically targets human TNF-alpha, MW: 144.19 KD.

S1029

Lenalidomide (CC-5013)

Lenalidomide (CC-5013) is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase.

S1567

Pomalidomide

Pomalidomide inhibits LPS-induced TNF-α release with IC50 of 13 nM in PBMCs. Pomalidomide can be utilized in PROTAC as a ligand for targeting E3 ligase and inhibiting the E3 ligase protein cereblon (CRBN). Pomalidomide promotes apoptosis and cell cycle arrest.

S1193

Thalidomide

Thalidomide was introduced as a sedative drug, immunomodulatory agent and also is investigated for treating symptoms of many cancers. Thalidomide inhibits an E3 ubiquitin ligase, which is a CRBN-DDB1-Cul4A complex.

S8037

Necrostatin-1

Necrostatin-1 is a specific RIP1 (RIPK1) inhibitor and inhibits TNF-α-induced necroptosis with EC50 of 490 nM in 293T cells. Necrostatin-1 also blocks IDO and suppresses autophagy and apoptosis.

S2465

CPI-1189

CPI-1189 is the proapoptotic cytokine tumor necrosis factor (TNF) alpha inhibitor. CPI-1189 intracellularly inhibits the p38 mitogen-activated protein kinase phosphoactivation and shows neuroprotective effects.

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.

S4902

QNZ (EVP4593)

QNZ (EVP4593) shows potent inhibitory activity toward both NF-κB activation and TNF-α production with IC50 of 11 nM and 7 nM in Jurkat T cells, respectively.

S8034

Apremilast (CC-10004)

Apremilast (CC-10004) is a potent and orally active PDE4 and TNF-α inhibitor with IC50 of 74 nM and 77 nM, respectively.

S1623

Acetylcysteine

Acetylcysteine(N-acetyl-l-cysteine) is a ROS(reactive oxygen species) inhibitor that antagonizes the activity of proteasome inhibitors. It is also a tumor necrosis factor production inhibitor. Acetylcysteine(N-acetyl-l-cysteine) suppresses TNF-induced NF-κB activation through inhibition of IκB kinases. Acetylcysteine(N-acetyl-l-cysteine) induces apoptosis via the mitochondria-dependent pathway. Acetylcysteine(N-acetyl-l-cysteine) inhibits ferroptosis and virus replication.Solutions of Acetylcysteine are best fresh-prepared.

S4238

Cepharanthine

Cepharanthine is a biscoclaurine alkaloid inhibiting tumor necrosis factor (TNF)-α-mediated NFκB stimulation, plasma membrane lipid peroxidation and platelet aggregation and suppressing cytokine production.

S8787

GSK'547

GSK'547 is a highly selective and potent inhibitor of RIP1 exhibiting a 400-fold improvement in mouse pharmacokinetic oral exposure compared with GSK'963

S8484

GSK2982772

GSK2982772 is an ATP competitive receptor-interacting protein-1 (RIP1) kinase inhibitor with the IC50 value of 1 nM. It has exquisite kinase specificity and excellent activity in blocking many TNF-dependent cellular responses.

S8642

GSK'963

GSK'963 is a chiral small-molecule inhibitor of RIP1 kinase with an IC50 of 29 nM in FP binding assays. It is >10 000-fold selective for RIP1 over 339 other kinases.

S3785

Notoginsenoside R1

Notoginsenoside R1 is the main ingredient with cardiovascular activity in Panax notoginseng. It inhibits TNF-α-induced PAI-1 overexpression via extracellular signal-related kinases (ERK1/2) and phosphatidylinositol 3-kinase (PI3K)/protein kinase B (PKB) signaling pathways.

S5913

Cambinol

Cambinol is a novel uncompetitive nSMase2 inhibitor with a K i value of 7 μM (IC50 = 5 ± 1 μM).

S9396

Geraniin

Geraniin, a hydrolysable polyphenol derived from Nephelium lappaceum L. fruit rind, has been shown to possess significant antioxidant activity in vitro.

S7609

GW4869

GW4869 is a neutral, noncompetitive inhibitor of sphingomyelinase (SMase) with an IC50 of 1 μM. It is selective for N-SMase, and does not inhibit acid SMase at up to at least 150 μM.

S9090

Corilagin

Corilagin, discovered in many medicinal plants such as Phyllanthus speices etc., has multiple activities including anti-oxidative, anti-inflammatory, anti-apoptotic, hepatoprotective and others. It is an inhibitor of TNF-α.

S3138

Methylthiouracil

Methylthiouracil is an antithyroid preparation.

S8169

GSK481

GSK481 is a RIP1(Receptor Interacting Protein Kinase1) inhibitor. Inhibition of RIP1 has been shown to hinder cell necrotic death.

S7963

TIC10

TIC10 inactivates Akt and ERK to induce TNF-related apoptosis-inducing ligand (TRAIL) through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics. Phase 1/2.

S5584

Citronellol

Citronellol, a constituent of rose and geranium oils, is used in perfumes and insect repellents.

S3865

Taurochenodeoxycholic acid

Taurochenodeoxycholic acid, a bile acid formed in the liver of most species, is used as a cholagogue and choleretic.

S6643

R-7050

R-7050 is a cell permeable TNF-α receptor antagonist and is 2.3-fold more selective for TNF-α-mediated signaling than for that driven by IL-1β.

S5851

4'-Methoxychalcone

4'-Methoxychalcone, found in citrus, is chalcone derivative that has shown diverse pharmacological properties, including anti-tumor and anti-inflammatory activities.

S7942

Bioymifi

Bioymifi, a small-molecule death receptor 5 (DR5) agonist, binds to the extracellular domain(ECD) of DR5 with a Kd of 1.2 μM but showed little binding affinity to the DR4 ECD. It induces DR5 clustering and aggregation, leading to apoptosis.

S1537

DMXAA (Vadimezan)

DMXAA (Vadimezan) is a vascular disrupting agents (VDA) and competitive inhibitor of DT-diaphorase with Ki of 20 μM and IC50 of 62.5 μM in cell-free assays, respectively. DMXAA (Vadimezan) is also a STING agonist with potential antineoplastic activity. DMXAA (Vadimezan) potently induces IFN-β but relatively low TNF-α expression in vitro. DMXAA (Vadimezan) has antiviral activity. Phase 3.

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
A2010

Adalimumab

Adalimumab is the first fully human, recombinant IgG1 monoclonal antibody that specifically targets human TNF-alpha, MW: 144.19 KD.

S1029

Lenalidomide (CC-5013)

Lenalidomide (CC-5013) is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase.

S1567

Pomalidomide

Pomalidomide inhibits LPS-induced TNF-α release with IC50 of 13 nM in PBMCs. Pomalidomide can be utilized in PROTAC as a ligand for targeting E3 ligase and inhibiting the E3 ligase protein cereblon (CRBN). Pomalidomide promotes apoptosis and cell cycle arrest.

S1193

Thalidomide

Thalidomide was introduced as a sedative drug, immunomodulatory agent and also is investigated for treating symptoms of many cancers. Thalidomide inhibits an E3 ubiquitin ligase, which is a CRBN-DDB1-Cul4A complex.

S8037

Necrostatin-1

Necrostatin-1 is a specific RIP1 (RIPK1) inhibitor and inhibits TNF-α-induced necroptosis with EC50 of 490 nM in 293T cells. Necrostatin-1 also blocks IDO and suppresses autophagy and apoptosis.

S2465

CPI-1189

CPI-1189 is the proapoptotic cytokine tumor necrosis factor (TNF) alpha inhibitor. CPI-1189 intracellularly inhibits the p38 mitogen-activated protein kinase phosphoactivation and shows neuroprotective effects.

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.

S4902

QNZ (EVP4593)

QNZ (EVP4593) shows potent inhibitory activity toward both NF-κB activation and TNF-α production with IC50 of 11 nM and 7 nM in Jurkat T cells, respectively.

S8034

Apremilast (CC-10004)

Apremilast (CC-10004) is a potent and orally active PDE4 and TNF-α inhibitor with IC50 of 74 nM and 77 nM, respectively.

S1623

Acetylcysteine

Acetylcysteine(N-acetyl-l-cysteine) is a ROS(reactive oxygen species) inhibitor that antagonizes the activity of proteasome inhibitors. It is also a tumor necrosis factor production inhibitor. Acetylcysteine(N-acetyl-l-cysteine) suppresses TNF-induced NF-κB activation through inhibition of IκB kinases. Acetylcysteine(N-acetyl-l-cysteine) induces apoptosis via the mitochondria-dependent pathway. Acetylcysteine(N-acetyl-l-cysteine) inhibits ferroptosis and virus replication.Solutions of Acetylcysteine are best fresh-prepared.

S4238

Cepharanthine

Cepharanthine is a biscoclaurine alkaloid inhibiting tumor necrosis factor (TNF)-α-mediated NFκB stimulation, plasma membrane lipid peroxidation and platelet aggregation and suppressing cytokine production.

S8787

GSK'547

GSK'547 is a highly selective and potent inhibitor of RIP1 exhibiting a 400-fold improvement in mouse pharmacokinetic oral exposure compared with GSK'963

S8484

GSK2982772

GSK2982772 is an ATP competitive receptor-interacting protein-1 (RIP1) kinase inhibitor with the IC50 value of 1 nM. It has exquisite kinase specificity and excellent activity in blocking many TNF-dependent cellular responses.

S8642

GSK'963

GSK'963 is a chiral small-molecule inhibitor of RIP1 kinase with an IC50 of 29 nM in FP binding assays. It is >10 000-fold selective for RIP1 over 339 other kinases.

S3785

Notoginsenoside R1

Notoginsenoside R1 is the main ingredient with cardiovascular activity in Panax notoginseng. It inhibits TNF-α-induced PAI-1 overexpression via extracellular signal-related kinases (ERK1/2) and phosphatidylinositol 3-kinase (PI3K)/protein kinase B (PKB) signaling pathways.

S5913

Cambinol

Cambinol is a novel uncompetitive nSMase2 inhibitor with a K i value of 7 μM (IC50 = 5 ± 1 μM).

S9396

Geraniin

Geraniin, a hydrolysable polyphenol derived from Nephelium lappaceum L. fruit rind, has been shown to possess significant antioxidant activity in vitro.

S7609

GW4869

GW4869 is a neutral, noncompetitive inhibitor of sphingomyelinase (SMase) with an IC50 of 1 μM. It is selective for N-SMase, and does not inhibit acid SMase at up to at least 150 μM.

S9090

Corilagin

Corilagin, discovered in many medicinal plants such as Phyllanthus speices etc., has multiple activities including anti-oxidative, anti-inflammatory, anti-apoptotic, hepatoprotective and others. It is an inhibitor of TNF-α.

S3138

Methylthiouracil

Methylthiouracil is an antithyroid preparation.

S8169

GSK481

GSK481 is a RIP1(Receptor Interacting Protein Kinase1) inhibitor. Inhibition of RIP1 has been shown to hinder cell necrotic death.

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
S7963

TIC10

TIC10 inactivates Akt and ERK to induce TNF-related apoptosis-inducing ligand (TRAIL) through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics. Phase 1/2.

2019, 14(5):1020-1029

2019, 857:172423

2018, 9(8):1486-1499

S5584

Citronellol

Citronellol, a constituent of rose and geranium oils, is used in perfumes and insect repellents.

S3865

Taurochenodeoxycholic acid

Taurochenodeoxycholic acid, a bile acid formed in the liver of most species, is used as a cholagogue and choleretic.

2019, 7(1):145

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
S6643

R-7050

R-7050 is a cell permeable TNF-α receptor antagonist and is 2.3-fold more selective for TNF-α-mediated signaling than for that driven by IL-1β.

S5851

4'-Methoxychalcone

4'-Methoxychalcone, found in citrus, is chalcone derivative that has shown diverse pharmacological properties, including anti-tumor and anti-inflammatory activities.

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
S7942

Bioymifi

Bioymifi, a small-molecule death receptor 5 (DR5) agonist, binds to the extracellular domain(ECD) of DR5 with a Kd of 1.2 μM but showed little binding affinity to the DR4 ECD. It induces DR5 clustering and aggregation, leading to apoptosis.

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
S1537

DMXAA (Vadimezan)

DMXAA (Vadimezan) is a vascular disrupting agents (VDA) and competitive inhibitor of DT-diaphorase with Ki of 20 μM and IC50 of 62.5 μM in cell-free assays, respectively. DMXAA (Vadimezan) is also a STING agonist with potential antineoplastic activity. DMXAA (Vadimezan) potently induces IFN-β but relatively low TNF-α expression in vitro. DMXAA (Vadimezan) has antiviral activity. Phase 3.

2020, 7 pii: S1074-7613(20)30129-1

2019, 9(6):722-737

2018, 13(19):2057-2064