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23

抑制剂 & 化合物

5

天然产物

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Cat. No. Product Name Target Signaling Pathways
T3502 C29

TLR Immunology/Inflammation
C29 是 Toll 样受体 2 抑制剂,可阻断 hTLR2/1 和 hTLR2/6 信号,IC50值分别为 19.7 和 37.6 μM。
T38361 GSK717

IL Receptor; NOD Immunology/Inflammation; NF-κB
GSK717 是 NOD2(核苷酸结合寡聚结构域 2) 的选择性抑制剂。它抑制壁酰二肽 (MDP) 诱导的 NOD2 介导的信号转导,抑制 MDP 刺激的 HEK293/hNOD2 细胞分泌 IL-8 (IC50为 400 nM)。
T6716 Valsartan

Diovan,缬沙坦,Tareg,CGP 48933

RAAS Endocrinology/Hormones
Valsartan (CGP 48933) 是一种血管紧张素 II 受体拮抗剂,有用于高血压和心力衰竭的研究潜力。
T15020 CU-CPT22

TLR Immunology/Inflammation
CU-CPT22 是 toll 样受体 1 和 2 蛋白复合物抑制剂,可阻断 Pam3CSK4诱导的 TLR1/2 激活,IC50值为 0.58 µM。 它与 TLR1/2 结合的合成三酰脂蛋白竞争,Ki 值为 0.41 µM。
T15017 CU-T12-9

TLR Immunology/Inflammation
CU-T12-9 是特异性 TLR1/2激动剂,可激活先天免疫系统和适应性免疫系统。它选择性激活 TLR1/2 异二聚体,可通过促进 TLR1 和 TLR2 二聚而激活 NF-κB 信号,引起下游 TNF-α、IL-10 和 iNOS 增加。
T76975 Tomaralimab

OPN-305

TLR Immunology/Inflammation
Tomaralimab (OPN-305) 是一种人源化的靶向 TLR2 的 IgG4 单克隆抗体。Tomaralimab 可用于研究骨髓增生异常综合征 (MDS) 。
T34249 Rabeximod

ROB-803

TLR Immunology/Inflammation
Rabeximod 是一种有效的免疫调节剂,可降低鼠模型中自身免疫性疾病疾病严重程度。Rabeximod 通过刺激TLR2TLR4下游阻断炎症细胞(可能是巨噬细胞)的激活,以时间依赖性的方式抑制关节炎。Rabeximod 能有效降低创伤性脑损伤抗炎治疗过程中小鼠的脑抗原呈递。
T26626 AN3485 Hydrochloride

AN3485 Hydrochloride inhibits TLR2-, TLR3-, TLR4- and TLR5-mediated TNF-α, IL-1β and IL-6.
T38261 Sparstolonin B

Sparstolonin B is a chemical compound that functions as a selective antagonist for TLR2 and TLR4, specifically targeting TLR2- and TLR4-mediated inflammatory signaling. This compound demonstrates additional pharmacological properties, including anti-HIV and anticancer activities[1][2].
T74890 Diprovocim-X

Diprovocim-X (compound 35) 为有效的TLR1/TLR2激动剂,其对hTLR1/TLR2和mTLR1/TLR2的EC50值分别为0.14 nM和0.75 nM。此化合物在小鼠体内作为佐剂使用时,能有效激发适应性免疫反应。
T60763 MMG-11 quarterhydrate

MMG-11 quarterhydrate 是人TLR2的选择性拮抗剂,可抑制 TLR2/1 和 TLR2/6 信号,且细胞毒性低。MMG-11 quarterhydrate 对 Pam3CSK4诱导的 hTLR2/1 和 Pam2CSK4诱导的 hTLR2/6 反应的IC50值分别为 1.7 μM 和 5.7 μM。
T16123 MMG-11

Others Others
MMG-11 inhibits both TLR2/1 and TLR2/6 signaling (IC50s: 1.7 μM for Pam3CSK4-induced hTLR2/1 and 5.7 μM for Pam2CSK4-induced hTLR2/6 responses). MMG-11 is an effective and selective human TLR2 antagonist with low cytotoxicity.
TP2282L Pam2CSK4 TFA

PUL-042 TFA,ODN-M362 TFA,Pam2CSK4 trifluoroacetate-salt,Pam2CSK4 TFA(868247-72-7 Free base)

TLR; Antifungal Immunology/Inflammation; Microbiology/Virology
Pam2CSK4 TFA (PUL-042 TFA) 是一种有效的 TLR2TLR6 双重激动剂,是一种模拟细菌脂蛋白的多肽。Pam2CSK4 TFA 可促进血小板聚集,可用来研究脂蛋白对牙周的影响。
T35701 FSL-1 TFA

FSL-1 TFA, a bacterial-derived toll-like receptor 2/6 (TLR2/6) agonist, enhances resistance to experimental HSV-2 infection[1]. FSL-1 TFA induces MMP-9 production through TLR2 and NF-κB/AP-1 signaling pathways in monocytic THP-1 cells[2]. FSL-1 significantly reduces HSV-2 replication in human vaginal epithelial cells (EC)[1].FSL-1 induces significant resistance to experimental genital HSV-2 infection through elaboration of a specific cytokine response profile[1].FSL-1 (50 ng/mL, 24 hours) induce...
T74230 Dioleoylphosphatidylglycerol

Dioleoylphosphatidylglycerol (DOPG) 是由水通道蛋白3 (AQP3) 和磷脂酶 D2 (PLD2) 作用而产生的天然磷脂。此化合物能抑制巨噬细胞产生炎症介质,此作用是通过热休克蛋白 B4 (HSPB4) 激活的 toll 样受体 2 (TLR2)来实现的。
TP2035 FSL-1

FSL 1

TLR2/6 agonist (also a putative TLR10 ligand). Activates NF-κB. Induces pro-inflammatory cytokines including IL-8, IL-1β, CCL20 and TNF-α in vitro. Synergizes with IFNγ to induce CXCL10 release from melanoma cells.
TP1962 Pam2CSK4

Toll-like receptor 2/6 (TLR2/6) agonist. Induces TNF-α production in human mononuclear cells. Also induces proliferation and activation of mouse splenic B cells.
T78101 Zymosan A

Zymosan A from Saccharomyces cerevisiae

Zymosan A(来自酿酒酵母的Zymosan A)是一种针对TLR2的激动剂,能够预防及抑制由IR引起的肠道伤害。该化合物显著增强了对辐射的防护能力,并能够保护小鼠免受辐射引起的肠损伤。此外,Zymosan A还能促进受IR损伤的肠干细胞(ISCs)的再生。
T35587 Ganglioside GD1a mixture (sodium salt)

Ganglioside B1

Ganglioside GD1a is a sialic acid-containing glycosphingolipid found in brain, erythrocytes, bone marrow, testis, spleen, and liver. [1] It can be shed from the surface of tumor cells into the microenvironment where it influences tumor-host cell interactions to promote tumor cell proliferation, invasion, and metastasis. Ganglioside GD1a (20 μM) also increases endothelial cell proliferation. Furthermore, ganglioside GD1a has been shown to act as a functional coreceptor for toll-like receptor 2 (T...
T81360 PSMα3 TFA

PSMα3 TFA 作为一种肽类化合物,主要用于诱导生成耐受性的树突细胞(DC),以应用于DC疫苗接种。该化合物能对TLR2TLR4诱导的DC成熟过程进行调节,抑制促炎和消炎细胞因子的产生,降低抗原摄取,并影响人单核细胞来源DC的渗透和调节能力。此外,PSMα3 TFA 是耐甲氧西林金黄色葡萄球菌(MRSA)中最有毒株释放的关键毒素之一。
T37722 Diprovocim-1

Diprovocim-1 is an agonist of the toll-like receptor 1/2 heterodimer.1It induces TNF-α release in THP-1 cells (EC50= 110 pM), an effect that can be inhibited by anti-TLR1 or anti-TLR2 antibodies. Diprovocim-1 (10 mg/kg) increases the production of ovalbumin-specific IgG1 in wild-type, but notTLR2-/-, mice sensitized to ovalbumin.2It also enhances anti-PD-L1 antibody-induced activation of cytotoxic T lymphocytes, reduction of tumor growth, and increases in survival in a B16/F10 murine melanoma mo...
T35672 SMU127

SMU127 is an agonist of the toll-like receptor 1/2 (TLR1/2) heterodimer.1It induces NF-κB signaling in cells expressing human TLR2 (EC50= 0.55 μM) but not cells expressing human TLR3, -4, -5, -7, or -8 when used at concentrations ranging from 0.1 to 100 μM. SMU127 induces the production of TNF-α in isolated human peripheral blood mononuclear cells (PBMCs) when used at concentrations ranging from 0.01 to 1 μM.In vivo, SMU127 (0.1 mg/animal) reduces tumor volume in a 4T1 murine mammary carcinoma m...
T83895 NCI 126224

NSC 126224

NCI 126224 是一种 toll-like receptor 4 (TLR4) 的拮抗剂。它在 RAW 264.7 巨噬细胞中,选择性抑制由 TLR4 激动剂 LPS 引起的一氧化氮 (NO) 产生(IC50 = 0.31 µM),而对 TLR7/8 激动剂 R-848、TLR1/2 激动剂 Pam3CSK4 以及 TLR3 激动剂 poly(I:C) 的影响较小;但对于相同细胞中由 TLR2/6 激动剂 FSL-1 引起的 NO 产生,其抑制作用在 0.6 µM 时亦显现。此外,NCI 126224 在 BV-2 微胶质细胞的报告实验中抑制了 LPS 引起的 NF-κB 活性,并在 RAW 264.7 巨噬细胞中降低了 LPS 引起的 IL-1β 和 TNF-α 水平(IC50s = 5.92, 0.42, 和 1.54 µM,分别)。

化合物

C29
Cat.No: T3502
Synonym:
Target: TLR
GSK717
Cat.No: T38361
Synonym:
Target: IL Receptor, NOD
Valsartan
Cat.No: T6716
Synonym: Diovan,缬沙坦,Tareg,CGP 48933
Target: RAAS
CU-CPT22
Cat.No: T15020
Synonym:
Target: TLR
CU-T12-9
Cat.No: T15017
Synonym:
Target: TLR
Tomaralimab
Cat.No: T76975
Synonym: OPN-305
Target: TLR
Rabeximod
Cat.No: T34249
Synonym: ROB-803
Target: TLR
AN3485 Hydrochloride
Cat.No: T26626
Synonym:
Target:
Sparstolonin B
Cat.No: T38261
Synonym:
Target:
Diprovocim-X
Cat.No: T74890
Synonym:
Target:
MMG-11 quarterhydrate
Cat.No: T60763
Synonym:
Target:
MMG-11
Cat.No: T16123
Synonym:
Target: Others
Pam2CSK4 TFA
Cat.No: TP2282L
Synonym: PUL-042 TFA,ODN-M362 TFA,Pam2CSK4 trifluoroacetate-salt,Pam2CSK4 TFA(868247-72-7 Free base)
Target: TLR, Antifungal
FSL-1 TFA
Cat.No: T35701
Synonym:
Target:
Dioleoylphosphatidylglycerol
Cat.No: T74230
Synonym:
Target:
FSL-1
Cat.No: TP2035
Synonym: FSL 1
Target:
Pam2CSK4
Cat.No: TP1962
Synonym:
Target:
Zymosan A
Cat.No: T78101
Synonym: Zymosan A from Saccharomyces cerevisiae
Target:
Ganglioside GD1a mixture (sodium salt)
Cat.No: T35587
Synonym: Ganglioside B1
Target:
PSMα3 TFA
Cat.No: T81360
Synonym:
Target:
Diprovocim-1
Cat.No: T37722
Synonym:
Target:
SMU127
Cat.No: T35672
Synonym:
Target:
NCI 126224
Cat.No: T83895
Synonym: NSC 126224
Target:
Cat. No. Product Name Target Signaling Pathways
T2897 (Rac)-Shikonin

(±)-Shikonin,Alkanet extract,Anchusin,紫草素,Anchusa acid

Others Others
(Rac)-Shikonin (Anchusin) 具有抗肿瘤作用。它能够诱导坏死死亡来绕过癌症耐药性。
T4958 (-)-Alkannin

Alkannin,左旋紫草素,紫草素,Shikonin

Apoptosis; PI3K Apoptosis; PI3K/Akt/mTOR signaling
(-)-Alkannin (Shikonin) 是从紫朱草中发现的一种天然产物,具有抗癌活性,可抑制细胞周期,诱导细胞凋亡,用作食品着色剂,在 Rho 激酶途径中可改善肝脏炎症。
T3795 Corilagin

Apoptosis; TLR; Reverse Transcriptase; Antibacterial; Autophagy Apoptosis; Autophagy; Immunology/Inflammation; Microbiology/Virology
Corilagin 是一种鞣酸,有抑制 RNA 肿瘤病毒逆转录酶的活性。它抑制金黄色葡萄球菌的生长,MIC 为 25 μg/mL。它有抗肿瘤活性,可用于肝癌和卵巢癌。
T27191 D-Mannuronic Acid

D-Mannuronic Acid is a blocker of the TLR2 and TLR4 downstream signaling pathway. D-Mannuronic Acid effectively inhibits mRNA expression of MyD88 and p65, major subunit of nuclear factor-kappaB.
T38394 PSMα3

PSMα3 is a peptide compound that can be utilized to induce tolerance in dendritic cells (DCs) for DC vaccination strategies. It effectively penetrates and modulates human monocyte-derived DCs by modifying the maturation process induced by TLR2 or TLR4. Additionally, PSMα3 inhibits the production of both pro- and anti-inflammatory cytokines and decreases antigen uptake. Notably, PSMα3 is a significant virulence factor released by the most pathogenic strains of methicillin-resistant Staphylococcus...

天然产物

(Rac)-Shikonin
Cat.No: T2897
Synonym: (±)-Shikonin,Alkanet extract,Anchusin,紫草素,Anchusa acid
Target: Others
(-)-Alkannin
Cat.No: T4958
Synonym: Alkannin,左旋紫草素,紫草素,Shikonin
Target: Apoptosis, PI3K
Corilagin
Cat.No: T3795
Synonym:
Target: Apoptosis, TLR, Reverse Transcriptase, Antibacterial, Autophagy
D-Mannuronic Acid
Cat.No: T27191
Synonym:
Target:
PSMα3
Cat.No: T38394
Synonym:
Target:
TargetMol Loading
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