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24

抑制剂 & 化合物

3

天然产物

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Cat. No. Product Name Target Signaling Pathways
T8313 HCH6-1

Others Others
HCH6-1 是甲酰肽受体 1 的竞争性二肽拮抗剂。它能够抑制 fMLF (FPR1激动剂) 特异性激活的人中性粒细胞的趋化性、超氧阴离子生成和弹性酶释放。动物实验中,它对急性肺损伤具有保护作用,可用于研究 FPR1 参与的炎症性肺部疾病。
T0946 Mepivacaine hydrochloride

Mepivacaine HCl,盐酸甲哌卡因

Sodium Channel Membrane transporter/Ion channel
Mepivacaine hydrochloride (Mepivacaine HCl) 是具有局部麻醉特性的酰胺衍生物。Mepivacaine hydrochloride 与神经元细胞膜上特定的电压门控钠离子通道结合,抑制钠离子内流和膜去极化。
T2018 Apilimod

阿匹莫德,阿吡莫德,STA 5326

IL Receptor; PI3K; Interleukin Immunology/Inflammation; PI3K/Akt/mTOR signaling
Apilimod (STA 5326) 是一种有效的、高度选择性的PIKfyve 抑制剂,是一种 IL-12/IL-23 的有效抑制剂,抑制人和猴的 PBMC 细胞中的 IL-12,IC50值为 1 nM 和 2 nM。
T6831 Etretinate

Retinoid,Tegison,Etretinato,Ethyl etrinoate,Ro 10-9359,依曲替酯

Apoptosis; Others Apoptosis; Others
Etretinate (Ro 10-9359) 是一种口服芳香族维甲酸,对牛皮癣和其他皮肤病综合征有效。 它激活类视黄醇受体,引起细胞分化的诱导、细胞增殖的抑制和炎症细胞对组织浸润的抑制。
T8857 LJP-1586 HCl

LJP 1586,LJP-1586 hydrochloride,LJP-1586,LJP1586

Others Others
LJP-1586 HCl 是一种高选择性的血管粘附蛋白-1(VAP-1)抑制剂,通过减少脑出血(ICH)后粘附分子表达和免疫细胞浸润而显示出抗炎作用。
T16379 Oglemilast

GRC 3886

PDE Metabolism
Oglemilast (GRC 3886) 是一种具有口服活性磷酸二酯酶 4 (PDE4) 抑制剂,对 PDE4D3 的 IC50 为 0.5 nM。Oglemilast 在体外和体内抑制肺细胞浸润,包括嗜酸性粒细胞增多和嗜中性粒细胞减少。Oglemilast 具有应用于炎症性气道疾病的潜力。
TP1379 KKI-5 TFA(97145-43-2 free base)

KKI-5 (TFA)

KKI-5 (TFA) is a specific tissue kallikrein inhibitor.Kki-5 (TFA) can reduce breast cancer cell infiltration.
T40958 Milategrast

E6007

Milategrast is a chemical compound that functions as a potent cell adhesion inhibitor and cell infiltration inhibitor. In vitro studies have demonstrated its ability to effectively inhibit the adhesion of Jurkat cells to human fibronectin, with an IC50 value of less than 5 μM.
T82642 Cyclo(RGDfK(Mal))

Cyclo(RGDfK(Mal))为一种五肽,能促进人多能干细胞的附着与渗透,适用于三维干细胞培养及其扩增。
T61599 XT2

XT2 is a highly potent, orally active, and selective inhibitor of NF-κB-inducing kinase (NIK), exhibiting an IC50 of 9.1 nM. It effectively suppresses the upregulation of ALT, a vital biomarker for acute liver injury, induced by CCl4. Additionally, XT2 significantly decreases immune cell infiltration into the damaged liver tissue. As a result, XT2 holds immense potential in liver inflammatory disease research [1].
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。
T73520 TNG260

TNG260 是一种CoREST 选择性脱乙酰酶(CoreDAC) 抑制剂。 TNG260 抑制HDAC1的选择性是HDAC3的 10 倍。 TNG260 导致HDAC1抑制,逆转由 STK11 缺失驱动的抗 PD1 耐药性。 TNG260 减少嗜中性粒细胞的瘤内浸润。 TNG260 表现出免疫介导的细胞杀伤。
T70346 TOP1362

TOP1362 is a Narrow Spectrum Kinase Inhibitors Demonstrate Promise for the Treatment of Dry Eye Disease and Other Ocular Inflammatory Disorders. TOP1362 strongly inhibited the kinase targets p38α, Syk, Src, and Lck, blocked the rise in p38α expression in hyperosmolar Chang cells, and potently reduced inflammatory cytokine release in cellular models of innate and adaptive immunities. In the EIU model, TOP1362 dose-dependently attenuated the LPS-induced rise in inflammatory cell infiltration and o...
T79643 PD-1/PD-L1-IN-33

PD-1/PD-L1 Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation
PD-1/PD-L1-IN-33 (Compound N11) 是抑制PD-1与PD-L1相互作用的抑制剂,IC50 值为 6.3 nM。该化合物能够促进T细胞的增殖、激活以及浸润肿瘤球,显示出免疫调节和抗肿瘤的活性。
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。
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。
T76786 Cabiralizumab

Cabiralizumab (FPA 008) 是一种抗 CSF1R 单克隆抗体 (MAb)。Cabiralizumab 可增强 T 细胞浸润和抗肿瘤 T 细胞免疫反应。Cabiralizumab 抑制破骨细胞的活化并阻止骨质破坏,可用于类风湿性关节炎 (RA) 的研究。Cabiralizumab 可与 Nivolumab 结合用于肺癌研究。
T62284 Anti-inflammatory agent 21

Anti-inflammatory agent 21 (compound 9o) 是一种低细胞毒性的、口服具有活力的抗炎剂,能够作用于 NO (IC50: 0.76 μM)。Anti-inflammatory agent 21 能够积累 ROS、阻断 NF-κB/MAPK 信号通路来发挥抗炎作用。 Anti-inflammatory agent 21 对关节炎大鼠模型的软骨破坏和炎症细胞浸润有一定的改善作用。
T61133 SSAO/VAP-1 inhibitor 1

SSAO/VAP-1 inhibitor 1 是一种有效的SSAO/VAP-1抑制剂。SSAO/VAP-1 促进葡萄糖转运 4 (GLUT 4) 从脂肪细胞转移到细胞膜,从而调节葡萄糖转运。在内皮细胞中,SSAO/VAP-1 可以介导白细胞和内皮细胞的粘附和渗出,并参与炎症反应。SSAO/VAP-1 inhibitor 1 具有研究炎症和/或炎症相关疾病或糖尿病和/或糖尿病相关疾病的潜力。
T35573 Adenosine 5’-methylenediphosphate (hydrate)

Adenosine 5’-methylenediphosphate is an inhibitor of ecto-5’-nucleotidase, also known as CD73, with a Kivalue of 37 nM.1It inhibits cAMP accumulation induced by adenosine 5’-monophosphate , adenosine 5’-diphosphate , or adenosine 5’-triphosphate but not adenosine in VA-13 human fibroblasts when used at a concentration of 100 μM. Adenosine 5’-methylenediphosphate reduces proliferation of U138MG glioma cells, as well as inhibits the invasion and migration of MHCC97H hepatocellular carcinoma (HCC) ...
T83700 IRBP (651-670) (human) TFA

IRBP651-670,Interphotoreceptor Retinoid-Binding Protein (651-670)

IRBP651-670(Interphotoreceptor retinoid-binding protein (651-670))是IRBP(亦称为retinoid-binding protein 3)的肽段,参与色素再生,通过将视黄醇和视黄醛从光感受细胞传输到视网膜色素上皮。在C57BL/6小鼠中,利用IRBP651-670诱导自身免疫性葡萄膜炎,这些小鼠携带H-2b单体型。用IRBP651-670(300 µg/动物)免疫增加了小鼠眼部IL-1β、IL-6、IL-17、TNF-α和IFN-γ水平,免疫细胞浸润及光感受器损伤。
T83763 EPI-X4 TFA

Endogenous Peptide Inhibitor of CXCR4

EPI-X4是一种源于人血清白蛋白408-423氨基酸的内源性肽段,是趋化因子(C-X-C基序)受体4 (CXCR4)的拮抗剂。在0.8至1,000µM的浓度范围内,EPI-X4能抑制表达CXCR4的HEK293细胞中由趋化因子(C-X-C基序)配体12 (CXCL12)诱发的钙离子动员和受体内化。EPI-X4还能抑制CXCL12诱导的Jurkat T细胞和人类CD34+造血干细胞的迁移。体内实验中,EPI-X4(16µmol/kg)在急性过敏性气道高嗜酸性粒细胞疾病的小鼠模型中减少了Cxcr4依赖的炎症细胞气道浸润。慢性肾脏病患者尿液中EPI-X4的水平增高,并与肾小球滤过率(GFR)成反比。
T38100 Betamethasone 21-phosphate (sodium salt hydrate)

Betamethasone 21-phosphate is a synthetic glucocorticoid.1It prevents increases in macrophage and eosinophil numbers in bronchoalveolar lavage fluid (BALF) and decreases in blood leukocyte numbers in a guinea pig model of parainfluenza-3 viral infection when administered at a dose of 8 mg/kg but does not prevent airway hyperresponsiveness after infection.2Betamethasone 21-phosphate inhibits cell infiltration into the aqueous humor in a rat model of endotoxin-induced uveitis when administered top...
T83779 EP4 Antagonist 14

Prostaglandin E2 Receptor 4 Antagonist 14,PGE2 Receptor 4 Antagonist 14

EP4 antagonist 14是一种前列腺素E2(PGE2)受体亚型EP4的拮抗剂,其在使用表达人源受体的HEK293细胞的报告基因测定中的IC50值为1.1 nM。它还能抑制PGE2诱导的同种细胞中的β-阿雷斯汀招募(IC50 = 0.9 nM)。EP4 antagonist 14(10 µM)能减少RAW 264.7巨噬细胞中PGE2诱导的mRNA表达,这些mRNA编码Il-4、巨噬细胞甘露糖受体1(Mrc1)、几丁质酶样蛋白3(Chil3)、趋化因子(C-X-C)基序配体1(Cxcl1)、表达在髓样细胞上的触发受体2(Trem2)和精氨酸酶-1(Arg1)。在体内,EP4 antagonist 14(每天30 mg/kg),结合抗PD-1抗体,能够在CT26小鼠结肠癌模型中抑制肿瘤生长并增加CD8+ T细胞对肿瘤的浸润。

化合物

HCH6-1
Cat.No: T8313
Synonym:
Target: Others
Mepivacaine hydrochloride
Cat.No: T0946
Synonym: Mepivacaine HCl,盐酸甲哌卡因
Target: Sodium Channel
Apilimod
Cat.No: T2018
Synonym: 阿匹莫德,阿吡莫德,STA 5326
Target: IL Receptor, PI3K, Interleukin
Etretinate
Cat.No: T6831
Synonym: Retinoid,Tegison,Etretinato,Ethyl etrinoate,Ro 10-9359,依曲替酯
Target: Apoptosis, Others
LJP-1586 HCl
Cat.No: T8857
Synonym: LJP 1586,LJP-1586 hydrochloride,LJP-1586,LJP1586
Target: Others
Oglemilast
Cat.No: T16379
Synonym: GRC 3886
Target: PDE
KKI-5 TFA(97145-43-2 free base)
Cat.No: TP1379
Synonym: KKI-5 (TFA)
Target:
Milategrast
Cat.No: T40958
Synonym: E6007
Target:
Cyclo(RGDfK(Mal))
Cat.No: T82642
Synonym:
Target:
XT2
Cat.No: T61599
Synonym:
Target:
Tengonermin
Cat.No: T76983
Synonym:
Target:
TNG260
Cat.No: T73520
Synonym:
Target:
TOP1362
Cat.No: T70346
Synonym:
Target:
PD-1/PD-L1-IN-33
Cat.No: T79643
Synonym:
Target: PD-1/PD-L1
PD-1/PD-L1-IN-26
Cat.No: T72668
Synonym:
Target: PD-1/PD-L1
Antitumor agent-36
Cat.No: T74393
Synonym:
Target:
Cabiralizumab
Cat.No: T76786
Synonym:
Target:
Anti-inflammatory agent 21
Cat.No: T62284
Synonym:
Target:
SSAO/VAP-1 inhibitor 1
Cat.No: T61133
Synonym:
Target:
Adenosine 5’-methylenediphosphate (hydrate)
Cat.No: T35573
Synonym:
Target:
IRBP (651-670) (human) TFA
Cat.No: T83700
Synonym: IRBP651-670,Interphotoreceptor Retinoid-Binding Protein (651-670)
Target:
EPI-X4 TFA
Cat.No: T83763
Synonym: Endogenous Peptide Inhibitor of CXCR4
Target:
Betamethasone 21-phosphate (sodium salt hydrate)
Cat.No: T38100
Synonym:
Target:
EP4 Antagonist 14
Cat.No: T83779
Synonym: Prostaglandin E2 Receptor 4 Antagonist 14,PGE2 Receptor 4 Antagonist 14
Target:
Cat. No. Product Name Target Signaling Pathways
T3662 Eleutheroside E

NF-κB NF-κB
Eleutheroside E 是刺五加的重要成分,具有抗炎,保护缺血心脏的功能。
T16733 Resolvin E1

RvE1

Others Others
Resolvin E1 is an effective endogenous pro-resolving mediator of inflammation. Resolvin E1 has unique counterregulatory actions that inhibit PMN transendothelial migration. Resolvin E1 also acts as an effective inhibitor of leukocyte infiltration, dendrit
TN4582 Moracin T

c-Myc; COX Cell Cycle/Checkpoint; Immunology/Inflammation; Neuroscience
Moracin treatment can inhibit the double 12-O-tetradecanoylphorbol 13-acetate (TPA) treatment-induced morphological changes reflecting inflammatory response, including leucocyte infiltration, hyperplasia and cell proliferation; moracin treatment furthermo

天然产物

Eleutheroside E
Cat.No: T3662
Synonym:
Target: NF-κB
Resolvin E1
Cat.No: T16733
Synonym: RvE1
Target: Others
Moracin T
Cat.No: TN4582
Synonym:
Target: c-Myc, COX
TargetMol Loading
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