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Cat. No. | Product Name | Target | Signaling Pathways |
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T78053 |
PD-L1-IN-2
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PD-1/PD-L1 | Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation |
"PD-L1-IN-2是一种具有潜力的肿瘤免疫治疗剂,具有抑制PD-L1的活性。该化合物为Naamidine J的衍生物,可通过降低体内PD-L1的表达并增强肿瘤浸润性T细胞的免疫反应来发挥抗肿瘤效果。PD-L1-IN-2主要应用于结直肠癌的研究领域。" | |||
T79739 |
CYP51/PD-L1-IN-2
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CYP51/PD-L1-IN-2(compound L20)是一种具有抗真菌活性的喹唑啉化合物。它作为CYP51(IC50:0.263 μM)和PD-L1(IC50:0.017 μM)的双重抑制剂,能够在细胞周期的早期引发真菌细胞凋亡。CYP51/PD-L1-IN-2进一步显著降低IL-2、NLRP3、NF-κBp65等蛋白水平,触发线粒体损伤及ROS积累,终致真菌细胞裂解和死亡。 | |||
T76970 | Tagitanlimab | ||
Tagitanlimab (HBM-9167),一种人源化抗PD-L1抗体(IgG1κ型),通过选择性阻断PD-L1与PD-1的相互作用,展现出对研究复发性或转移性鼻咽癌(NPC)的潜力。 | |||
T76899 | Adebrelimab | ||
Adebrelimab (SHR-1316) 是一种人源化IgG4单克隆抗体,针对PD-L1(PD-1/PD-L1)具有良好的抗肿瘤活性。该药物在包括广泛期小细胞肺癌(SCLC)在内的多种实体瘤中表现出效果。 | |||
T36885 |
BMSpep-57 hydrochloride
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BMSpep-57 hydrochloride, a potent macrocyclic peptide, competitively inhibits PD-1/PD-L1 interaction, exhibiting an IC50 value of 7.68 nM. It binds to PD-L1 with dissociation constants (Kds) of 19 nM and 19.88 nM as determined by MST and SPR assays, respectively. This compound enhances T cell functionality by promoting IL-2 production in PBMCs[1]. | |||
T76897 | Acasunlimab | ||
Acasunlimab (GEN1046) 是一种双特异性抗体 (bsAb),靶向PD-L1和4-1BB。Acasunlimab 通过有条件的4-1BB 刺激增强 T 细胞和 NK 细胞功能,同时构成性地阻断PD-1/PD-L1抑制轴。Acasunlimab 可用于癌症的研究。 | |||
T78902 |
CYP51/PD-L1-IN-4
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CYP51/PD-L1-IN-4(化合物14a-2)是一种高效的双靶点抑制剂,其IC50值针对CYP51为0.17 μM,针对PD-L1为0.021 μM。该化合物在体外展现出卓越的抗真菌和抗耐药真菌能力,适用于真菌感染的研究。 | |||
T80617 |
Reozalimab
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PD-1/PD-L1 | Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation |
Reozalimab为针对PD-1/PD-L1的双特异性抗体,具有引导抗体依赖性细胞毒性(ADCC)在癌症研究中的作用。 | |||
T39106 |
BMSpep-57
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BMSpep-57, a potent macrocyclic peptide inhibitor, competitively disrupts the PD-1/PD-L1 interaction, demonstrating a significant inhibitory concentration (IC50) of 7.68 nM. It exhibits binding affinity towards PD-L1 with dissociation constants (Kd) of 19 nM and 19.88 nM in MicroScale Thermophoresis (MST) and Surface Plasmon Resonance (SPR) assays, respectively. This compound enhances T cell functionality by promoting Interleukin-2 (IL-2) production within Peripheral Blood Mononuclear Cells (PBM... | |||
T70291 |
PCC0208018
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PCC0208018 is a novel activator of effector T cells, enhancing T cell proliferation and activation to release interferon gamma (IFN-γ) and interleukin-2 (IL-2) without blocking the programmed cell death 1 (PD-1)/programmed cell death-ligand 1 (PD-L1) binding and not directly affecting tumor cell viability in vitro. | |||
T79738 |
CYP51/PD-L1-IN-1
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CYP51/PD-L1-IN-1(compound L11)是一种具有抗真菌活性的喹唑啉化合物,作为CYP51(IC50: 0.884 μM)和PD-L1(IC50: 0.083 μM)的双重抑制剂,能够在细胞周期早期引发真菌细胞的凋亡。该化合物还能有效减少IL-2、NLRP3、NF-κBp65等蛋白的细胞内水平,诱导线粒体损伤及ROS积聚,进而导致真菌细胞的破裂和死亡。 | |||
T79740 |
CYP51/PD-L1-IN-3
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CYP51/PD-L1-IN-3(compound L21)是一种具有抗真菌活性的喹唑啉化合物。作为CYP51(IC50: 0.205 μM) 和PD-L1(IC50: 0.039 μM) 的双重抑制剂,它能够引发真菌细胞在细胞周期早期的凋亡。此外,CYP51/PD-L1-IN-3 还能显著降低IL-2、NLRP3、NF-κBp65 蛋白的细胞内水平,并诱导线粒体损害及ROS 聚集,进而导致真菌细胞的裂解与死亡。 | |||
T76945 | Cetrelimab | ||
Cetrelimab (JNJ 63723283; JNJ 3283) 为人源化IgG4κ单克隆抗体,专门针对PD-1。其与PD-1的结合Kd值为1.72 nM(在HEK293细胞中测得)。Cetrelimab有效阻断PD-1与其配体PD-L1和PD-L2的结合,其IC50值分别为111.7 ng/mL与138.6 ng/mL。此外,Cetrelimab能激活外周T细胞,提升细胞因子(IFN-γ, IL-2, TNF-α)的表达水平,进而抑制肿瘤在体内的生长。 | |||
T82414 |
Favezelimab
MK-4280 |
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Favezelimab(MK-4280)为人源化抗LAG-3单克隆抗体,能够抑制LAG-3与其配体MHC II类结合。该抗体联合PD-L1抑制剂Pembrolizumab在结直肠癌(CRC)治疗研究中展现出应用前景。 | |||
T76997 | Socazolimab | ||
Socazolimab (ZKAB001) 是一种针对PD-L1的单克隆抗体,在治疗复发或转移性宫颈癌方面展现了持久的安全性和有效性。此外,Socazolimab 也被认为在小细胞肺癌、食管鳞状细胞癌 (ESCC)、晚期尿路上皮癌及骨肉瘤治疗中具有潜在应用价值。 | |||
T37722 |
Diprovocim-1
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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... | |||
T74393 | Antitumor agent-36 | ||
Antitumor agent-36 具有有效的抗增殖和抗转移活性,能诱导严重的 DNA 损伤,并通过增加 γ-H2AX 和 p53 的表达促进肿瘤细胞通过 Bcl-2/Bax/caspase3 线粒体凋亡通路的 (apoptosis)。此外,Antitumor agent-36 还能通过抑制 PD-L1 的表达显著增加肿瘤组织中 CD3+ 和 CD8+ T 浸润细胞,从而改善免疫反应。 | |||
T79487 | MAO A/HSP90-IN-2 | Monoamine Oxidase | Neuroscience |
MAO A/HSP90-IN-2(compound 4-C)是一种针对HSP90和MAO A的双重抑制剂,显示出分别对这两种酶有0.016 μM和4.58 μM的IC50值。该化合物能够上调HSP70,降低HER2和磷酸化AKT的表达,同时能减少GL26细胞中由IFN-γ诱导的PD-L1表达增加。此外,MAO A/HSP90-IN-2能够抑制对Temozolomide敏感或耐药的胶质母细胞瘤(GBM)、结肠癌、白血病和非小细胞肺癌细胞的生长,并可能有助于阻止肿瘤逃避免疫监控。 | |||
T64022 | Antitumor agent-37 | ||
Antitumor agent-37 表现出有效的抗增殖和抗转移效果。Antitumor agent-37 能够诱导严重的 DNA 损伤,进而导致 γ-H2AX 和 p53 的高表达。Antitumor agent-37 可利用线粒体凋亡通路 Bcl-2/Bax/caspase3,诱导肿瘤细胞凋亡 (apoptosis)。Antitumor agent-37 可以抑制 PD-L1 的表达,提高肿瘤组织中 CD3+ 和 CD8+ T 浸润细胞,明显改善免疫反应。 |
Cat. No. | Product Name | Target | Signaling Pathways |
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T6S0071 |
Fraxinellone
|
HIF/HIF Prolyl-Hydroxylase; STAT; PD-1/PD-L1 | Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Immunology/Inflammation; JAK/STAT signaling; Metabolism; Stem Cells |
Fraxinellone 是从白鲜的根皮中分离出来的一种天然产物,是PD-L1抑制剂,可抑制HIF-1α蛋白质合成。它通过靶向 PD-L1,有用于癌症免疫的潜力。 |