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抑制剂 & 化合物

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Cat. No. Product Name Target Signaling Pathways
T6540 Ibuprofen Lysine

布洛芬赖氨酸盐,Neoprofen

COX Immunology/Inflammation; Neuroscience
Ibuprofen Lysine (Neoprofen) 是一种非甾体抗炎药。
T35343 MTI-31

MTI-31,LXI-15029

mTOR PI3K/Akt/mTOR signaling
MTI-31 (LXI-15029) 是口服有效的,高度选择性的mTORC1和mTORC2抑制剂,对 mTOR 的Kd 为 0.20 nM,IC50为 39 nM。MTI-31可用于乳腺癌的研究。
T1394 Ibuprofen

Brufen,(±)-Ibuprofe,布洛芬,Motrin,Advil

COX Immunology/Inflammation; Neuroscience
Ibuprofen (Advil) 是一种丙酸衍生物和非甾体抗炎药 (NSAID),具有抗炎、镇痛和解热作用。它是COX-1和COX-2的抑制剂,IC50值分别为 13 和 370 μM,导致前列腺素和血栓素前体的形成减少。
T12516 Polyinosinic-polycytidylic acid sodium

双链聚肌胞,Poly(I:C) sodium

Apoptosis; Others; TLR Apoptosis; Immunology/Inflammation; Others
Polyinosinic-polycytidylic acid sodium (Poly(I:C) sodium) 是双链 RNA 的合成类似物,是TLR3和视黄酸诱导型基因 I 受体激动剂。它可以用作疫苗佐剂,直接触发癌细胞发生凋亡,还增强先天性和适应性免疫反应,并改变肿瘤的微环境。
T3633 Crenigacestat

LY3039478

Gamma-secretase Neuroscience; Proteases/Proteasome; Stem Cells
Crenigacestat (LY3039478) 是一种口服具有活性的Notch 和γ-secretase 的抑制剂,其在多种肿瘤细胞中的IC50为 ∼1nM。
T82268 Gotistobart

BNT 316,ONC-392

Gotistobart (ONC-392)为一种人源化抗CTLA-4抗体,旨在通过选择性消耗肿瘤微环境中的调节性T细胞(Treg),以增强免疫疗效。
T31825 Fluoromisonidazole

Fluoromisonidazole, a Radiation-Sensitizing Agent, can be used for imaging tumor hypoxia: imaging the microenvironment for personalized cancer therapy.
T78250 Selicrelumab

Selicrelumab是一种针对CD40的抗体激动剂,能够诱导肿瘤微环境的改变,适用于胰腺癌及肿瘤新辅助治疗的研究。
T40099 ALV2

ALV2 is a potent and selective Helios degrader compound that binds to the CRBN protein, exhibiting an IC50 value of 0.57 μM. Helios, a zinc-finger transcription factor, plays a crucial role in preserving a stable T reg cell phenotype within the inflammatory tumor microenvironment.
T22725 DiMNF

Others Others
DiMNF is a selective aryl hydrocarbon receptor (AHR) modulator. It also suppresses the expression of CD55 and CD46 induced by IL-1β in an inflammatory tumor cell microenvironment.
T10713 CCR4 antagonist 2

Calcium Channel Membrane transporter/Ion channel; Metabolism
CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues. CCR4 antagonist 2 (Compound 31) exhibits IC50 values of Ca2+flux and (chemotaxis) CTX are 40 nM and 70 nM, respectively.
T69648 Inupadenant HCl

Inupadenant, also known as EOS-850, is a highly selective small molecule antagonist of the adenosine A2a receptor, in the adenosine triphosphate adenosine pathway, a key driver of immunosuppression in the tumor microenvironment across a broad range of tumors.
T74507 IDO1-IN-20

IDO1-IN-20是一种催化色氨酸氧化代谢的酶,能在肿瘤微环境中对肿瘤进行免疫抑制。
T39531 RAD16-I hydrochloride

RAD16-I hydrochloride

RAD16-I hydrochloride is a self-assembling peptide with nanofibrous morphology that provides an optimal microenvironment for the proliferation and differentiation of human mesenchymal stem cells (hMSC) into chondrocytes. This peptide, known as RAD16-I, has been extensively studied and serves as a model to assess the amyloid-like staining properties of self-assembling peptide nanofibers (SAPNFs).
T13538 AlbA-DCA

ROS Immunology/Inflammation
AlbA-DCA is a conjugate formed by the attachment of Albiziabioside A to a dichloroacetate acid subunit. It can induce a marked increase in intracellular ROS and alleviate the accumulation of lactic acid in the tumor microenvironment, and also selectively
T79199 F-CRI1

STING Immunology/Inflammation
F-CRI1为高效STING激动剂,Kd值达40.62 nM。该化合物通过18F标记成为放射性探针,适用于肿瘤微环境中STING可视化的研究。
T78521 Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE

Others Others
Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE(化合物S6)作为抗肿瘤微环境特异性活化的抗癌剂,已被证实能够抑制小鼠肿瘤生长。
T36936 Prodan

Prodan 是一种溶剂化变色荧光团,已被用作微环境敏感膜报告剂。基于Prodan 的化学原理,设计并合成了荧光核苷。荧光核苷根据溶剂的取向极化率敏感地改变斯托克斯位移值。
T12925 Sitravatinib malate

MGCD516 malate,MG-516 malate

TAM Receptor Tyrosine Kinase/Adaptors
Sitravatinib malate is an orally bioavailable receptor inhibitor of tyrosine kinase (RTK) (IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively.) , shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.
T74975 Zn-DPA-maytansinoid conjugate 1

Zn-DPA-maytansinoid conjugate 1 为一种靶向小分子免疫检查点的类美坦素偶联物。其能持续诱导肿瘤生长消退,并激活肿瘤微环境(TME),转化为“炎热肿瘤”。
T79205 PD-1/PD-L1-IN-34

PD-1/PD-L1 Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation
PD-1/PD-L1-IN-34(化合物(1S,2S)-A25)能有效地抑制PD-1/PD-L1相互作用,其IC50值为0.029 μM,表现出对PD-L1的选择性结合亲和力,KD值为0.1554 μM。该化合物通过激活免疫微环境来抑制肿瘤生长。
T76983 Tengonermin

Tengonermin (ARENEGYR) 是一种血管靶向剂,由与CNGRCG 肽结合的人肿瘤坏死因子-α (TNF-α) 组成。Tengonermin 通过改变肿瘤微环境来增加肿瘤内化疗的渗透和 T 细胞浸润。
T36900 PD-1/PD-L1-IN-NP19

PD-1/PD-L1-IN-NP19

PD-1/PD-L1 Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation
PD-1/PD-L1-IN-NP19 是 PD-1/PD-L1 的抑制剂,抑制人类 PD-1/PD-L1 相互作用的 IC50 值为 12.5 nM。PD-1/PD-L1-IN-NP19 可以激活肿瘤的免疫微环境,这可能有助于其抗肿瘤作用。
T72668 PD-1/PD-L1-IN-26

PD-1/PD-L1 Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation
PD-1/PD-L1-IN-26 (Compound II-14) 是一种高效的 PD-1/PD-L1 抑制剂,IC50 为 0.0380 μM。该化合物能够激活肿瘤免疫微环境,通过促进 CD4+ T 细胞向肿瘤组织的浸润。PD-1/PD-L1-IN-26 展示了在癌症治疗研究中的应用潜力。
T77189 Sudubrilimab

Sudubrilimab (HS636) 是一种针对 PDL1的 Ig G1-kappa 单克隆抗体。Sudubrilimab 在重链的 C 末端与 TGF-β1受体 Ⅱ 胞外域 (TGFBR2-ECD) 融合,可在免疫抑制性肿瘤微环境中隔离 PD-1/PD-L1通路和 TGF-β 生物活性。
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...
T77090 Mitazalimab

Mitazalimab(ADC-1013; JNJ-64457107)是一种FcγR依赖性CD40激动剂,以肿瘤导向活性为特征。该化合物通过激活抗原呈递细胞(如树突状细胞[DC]),启动肿瘤反应性T细胞,进而诱导肿瘤特异性T细胞浸润并杀死肿瘤,有效重塑肿瘤浸润性骨髓微环境。
T74052 Polyinosinic-polycytidylic acid potassium

Polyinosinic-polycytidylic acid potassium (Poly(I:C) potassium) 是双链 RNA 的合成类似物,是一种TLR3和视黄酸诱导型基因 I 受体 (RIG-I 和MDA5) 的激动剂。Polyinosinic-polycytidylic acid potassium 可以用作疫苗佐剂,以增强先天性和适应性免疫反应,并改变肿瘤的微环境,还可以直接触发癌细胞发生凋亡 (Apoptosis)。
T76255 Certepetide

Certepetide (CEND-1),即双功能环肽(a.k.a. iRGD),是一种具有穿透肿瘤功能的多肽。通过与α-V整联蛋白(alphav-integrins)的RGD motif相互作用,以及激活神经纤毛蛋白1(NRP-1),Certepetide能够将实体瘤微环境转化成临时的活性分子通道,从而在肿瘤中累积。该化合物在胰腺癌和其他实体瘤的研究中具有应用潜力。
T83877 2-(cyclohexylmethyl)-Plumbagin

2-(cyclohexylmethyl)-Plumbagin是naphthoquinone plumbagin的衍生物。在模拟胰腺癌肿瘤微环境的营养匮乏条件下,与营养丰富条件下的PANC-1细胞相比,对PANC-1人类胰腺癌细胞表现出选择性的细胞毒性,50%优选细胞毒性值(PC50s)分别为0.11和47.2 µM。1 µM浓度下,还可诱导PANC-1细胞发生凋亡。此外,2-(cyclohexylmethyl)-Plumbagin在营养匮乏条件下,而非营养丰富条件下,选择性降低PANC-1细胞中Akt和哺乳动物雷帕霉素靶蛋白(mTOR)的磷酸化。在以每周五次、每次50和250 µg/动物剂量给药的MiaPaCa-2胰腺癌小鼠异种移植模型中,能减少肿瘤体积和重量。

化合物

Ibuprofen Lysine
Cat.No: T6540
Synonym: 布洛芬赖氨酸盐,Neoprofen
Target: COX
MTI-31
Cat.No: T35343
Synonym: MTI-31,LXI-15029
Target: mTOR
Ibuprofen
Cat.No: T1394
Synonym: Brufen,(±)-Ibuprofe,布洛芬,Motrin,Advil
Target: COX
Polyinosinic-polycytidylic acid sodium
Cat.No: T12516
Synonym: 双链聚肌胞,Poly(I:C) sodium
Target: Apoptosis, Others, TLR
Crenigacestat
Cat.No: T3633
Synonym: LY3039478
Target: Gamma-secretase
Gotistobart
Cat.No: T82268
Synonym: BNT 316,ONC-392
Target:
Fluoromisonidazole
Cat.No: T31825
Synonym:
Target:
Selicrelumab
Cat.No: T78250
Synonym:
Target:
ALV2
Cat.No: T40099
Synonym:
Target:
DiMNF
Cat.No: T22725
Synonym:
Target: Others
CCR4 antagonist 2
Cat.No: T10713
Synonym:
Target: Calcium Channel
Inupadenant HCl
Cat.No: T69648
Synonym:
Target:
IDO1-IN-20
Cat.No: T74507
Synonym:
Target:
RAD16-I hydrochloride
Cat.No: T39531
Synonym: RAD16-I hydrochloride
Target:
AlbA-DCA
Cat.No: T13538
Synonym:
Target: ROS
F-CRI1
Cat.No: T79199
Synonym:
Target: STING
Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE
Cat.No: T78521
Synonym:
Target: Others
Prodan
Cat.No: T36936
Synonym:
Target:
Sitravatinib malate
Cat.No: T12925
Synonym: MGCD516 malate,MG-516 malate
Target: TAM Receptor
Zn-DPA-maytansinoid conjugate 1
Cat.No: T74975
Synonym:
Target:
PD-1/PD-L1-IN-34
Cat.No: T79205
Synonym:
Target: PD-1/PD-L1
Tengonermin
Cat.No: T76983
Synonym:
Target:
PD-1/PD-L1-IN-NP19
Cat.No: T36900
Synonym: PD-1/PD-L1-IN-NP19
Target: PD-1/PD-L1
PD-1/PD-L1-IN-26
Cat.No: T72668
Synonym:
Target: PD-1/PD-L1
Sudubrilimab
Cat.No: T77189
Synonym:
Target:
Ganglioside GD1a mixture (sodium salt)
Cat.No: T35587
Synonym: Ganglioside B1
Target:
Mitazalimab
Cat.No: T77090
Synonym:
Target:
Polyinosinic-polycytidylic acid potassium
Cat.No: T74052
Synonym:
Target:
Certepetide
Cat.No: T76255
Synonym:
Target:
2-(cyclohexylmethyl)-Plumbagin
Cat.No: T83877
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
TN6967 (R)-Isomucronulatol

(-)-Isomucronulatol,2H-1-Benzopyran-7-ol

Apoptosis Apoptosis
(R)-Isomucronulatol (2H-1-Benzopyran-7-ol) 是一种可从黄芪、刺槐、虎杖和甘草叶片中提取得到的类黄酮,抑制BMSCs 在TNF-α微环境中的增殖和凋亡。(R)-Isomucronulatol 具有潜在的抗炎活性。

天然产物

(R)-Isomucronulatol
Cat.No: TN6967
Synonym: (-)-Isomucronulatol,2H-1-Benzopyran-7-ol
Target: Apoptosis
TargetMol Loading
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