Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T3146 |
BMS-202
PD1-PDL1 inhibitor 2,PD-1/PD-L1 inhibitor 2 |
Apoptosis; PD-1/PD-L1 | Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation |
BMS-202 (PD1-PDL1 inhibitor 2) 是一种非肽类 PD-1/PD-L 复合物抑制剂,其 IC50为 18 nM,KD 为 8 μM。它与 PD-L1 直接结合并阻断人类 PD-1/PD-L 的相互作用,具有抗肿瘤活性。 | |||
T4696 |
BMS202 hydrochloride (1675203-84-5(free base))
PD-1/PD-L1 inhibitor 2 hydrochloride |
PD-1/PD-L1 | Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation |
BMS202 hydrochloride (1675203-84-5(free base)) (PD-1/PD-L1 inhibitor 2 hydrochloride) 是一种小分子 PD-1/PD-L1 相互作用抑制剂 (IC50: 18 nM)。生物物理研究表明 BMS202 直接与 PD-L1 结合。 BMS202 的结合促进 PD-L1 二聚化并阻断 PD-L1/PD1 相互作用。 | |||
T3468 |
Tomivosertib
eFT508 |
MNK; PD-1/PD-L1 | Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation; MAPK |
Tomivosertib (eFT508) 是一种具有口服活性的MNK1和MNK2高选择性抑制剂,IC50值均为 1-2 nM。它可降低肿瘤细胞中eIF4E 的磷酸化水平 (位点为 Ser209,IC50=2-16 nM),下调PD-L1蛋白的平均含量。 | |||
T71032 |
Melafolone
|
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Melafolone is a natural dual inhibitor of cox-2 and egfr, improving program death 1 (pd-1) checkpoint blockade therapy through normalizing tumor vasculature and pd-l1 downregulation | |||
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。 | |||
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... | |||
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。 | |||
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。 | |||
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。 | |||
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。 |