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T8496
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MAZ51
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Apoptosis;
VEGFR |
Angiogenesis;
Apoptosis;
Tyrosine Kinase/Adaptors |
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MAZ51 是一种 VEGFR-3酪氨酸激酶的选择性抑制剂。它抑制 VEGF-C 诱导的 VEGFR-3 激活，而没有阻断 VEGF-C 介导的 VEGFR2 刺激。它阻止增殖并诱导多种肿瘤细胞凋亡，具有抗肿瘤活性。 |
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T74186
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PROTAC-O4I2
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Apoptosis;
PROTACs |
Apoptosis;
PROTAC |
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PROTAC-O4I2 是一种靶向剪接因子 3B1 (SF3B1) 的 PROTAC连接体， 在 K562 细胞中促使 FLAG-SF3B1 降解，IC50 值为 0.244 μM。PROTAC-O4I2 促使 K562 WT 细胞凋亡 (apoptosis)。 |
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T8864
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Thymidylate Kinase Inhibitor, YMU1
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Others |
Others |
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YMU1 是一种选择性抑制剂，特异性作用于人胸苷酸激酶 (IC50: 610 nM) 。 |
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T23818
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BPU-11
Biphenyl Urea 11
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Others |
Others |
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BPU-11 (Biphenyl Urea 11) 是一种 HCN4 CLP 配体，通过调节通道功能和完全消除 cAMP 诱导的 V1/2 变化来发挥作用。 |
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T23444
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TCS 1105
N-(4-fluorobenzyl)-2-(1H-indol-3-yl)-2-oxoacetamide
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Others |
Others |
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TCS 1105是一种GABAA 苯并二氮卓受体（BZR）配体。TCS 1105阻断Sema3A 诱导的轴突生长锥塌陷。TCS 1105能减少小鼠的焦虑样行为，增强攻击性行为和社会支配力。 |
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T3599
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BFH772
BFH-722
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VEGFR |
Angiogenesis;
Tyrosine Kinase/Adaptors |
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BFH772 是 VEGFR2抑制剂(IC50:3 nM)，具有口服活性。 |
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T4132
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BPTU
BMS-646786
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P2Y Receptor |
GPCR/G Protein;
Neuroscience |
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BPTU (BMS-646786) 是一种非核苷酸类P2Y1受体变构拮抗剂，能够阻断位于胃肠道神经肌肉接头的 P2Y1受体，具有抗血栓活性。 |
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TP1920L1
|
Acein acetate
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RAAS |
Endocrinology/Hormones |
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Acein acetate 是高亲和力血管紧张素转换酶 (ACE) 配体 (Kd = 2.79 nM)。浓度高达 500 nM 时对 ACE 酶活性没有显着影响。增强 NMDA + D-丝氨酸诱导的多巴胺从体外纹状体切片和体内纹状体的释放。 |
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T3716
|
Rolapitant
罗拉吡坦,SCH619734,罗拉匹坦
|
Neurokinin receptor |
GPCR/G Protein;
Neuroscience |
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Rolapitant (SCH619734) 是一种高效选择性具有口服活性的神经激肽 1 受体抑制剂，Ki 值为0.66 nM。 |
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T26513
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ABD-350
ABD350,ABD 350
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ABD-350 is ligand-induced inhibitor of nuclear factor kappaB phosphorylation. |
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T24950
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VUF-10214
VUF 10214,VUF10214
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VUF-10214 is an H4 receptor-ligand. VUF-10214 has significant anti-inflammatory properties in the carrageenan-induced paw edema model in vivo studies in the rat reveal. |
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T18826
|
Thalidomide-O-PEG2-propargyl
E3 ligase Ligand-Linker Conjugates 32
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Others |
Others |
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Thalidomide-O-PEG2-propargyl (E3 Ligase Ligand-Linker Conjugates 32) is a chemical compound that has been synthesized as a conjugate of an E3 ligase ligand and a linker. It incorporates the cereblon ligand based on Thalidomide, along with a 2-unit PEG linker. This compound is specifically designed for use in PROTAC technology, which utilizes ligand-induced protein degradation [1]. |
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T29073
|
UR-2922
UR 2922
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UR-2922 is an oral antagonist of platelet GPIIb/IIIa. UR-2922 possessed a high affinity for the human platelet receptor (K(d) <1 nM) and a slow dissociation rate (k(off)= 90 min) in vitro. UR-2922 induced no ligand-induced binding sites (LIBS) expression |
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T36553
|
Thrombin Receptor Peptide Ligand (trifluoroacetate salt)
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Thrombin receptor peptide ligand is antagonist of the thrombin receptor (EC50s = 16-33 μM to inhibit platelet aggregation in vitro). It inhibits α-thrombin and platelet aggregation induced by thrombin receptor activating peptide in vitro when used at a concentration of 32 μM but does not affect platelet aggregation induced by ADP or collagen. It also inhibits thrombin- and TRAP-induced proliferation of vascular smooth muscle cells (VSMCs). Thrombin receptor peptide ligand (100 μmol/kg bolus, i.v... |
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TP1920
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Acein
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Acein is a High affinity angiotensin-converting enzyme (ACE) ligand (Kd = 2.79 nM). Exhibits no significant effect on ACE enzymatic activity up to 500 nM concentration. Potentiates NMDA + D-serine-induced dopamine release from striatal slices in vitro and the striatum in vivo. |
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T38162
|
STING18
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STING18 is a competitive ligand of stimulator of interferon genes (STING; IC50 = 0.068 μM in a radioligand binding assay).1 It inhibits cGAMP-induced IFN-β production (IC50 = 11 μM) but does not stimulate IFN-β production (EC50 = >30 μM) in THP-1 cells.
|1. Siu, T., Altman, M.D., Baltus, G.A., et al. Discovery of a novel cGAMP competitive ligand of the inactive form of STING. Med. Chem. Lett. 10(1), 92-97 (2019). |
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T18697
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SNIPER(ER)-87
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Others |
Others |
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SNIPER(ER)-87 is a chemical compound composed of a derivative of the inhibitor of apoptosis protein (IAP) ligand LCL161 conjugated to the estrogen receptor α (ERα) ligand 4-hydroxytamoxifen using a PEG linker. It effectively degrades the ERα protein with an IC50 value of 0.097 μM. Within cells, SNIPER(ER)-87 selectively recruits XIAP to ERα, and XIAP functions as the primary E3 ubiquitin ligase responsible for the degradation of ERα induced by SNIPER(ER)-87[1][2]. |
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T78083
|
CB-25
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Cannabinoid Receptor |
GPCR/G Protein |
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CB-25是一种CB1大麻素受体的部分激动剂配体。它能增强Forskolin诱导的癌细胞中cAMP的形成，但在Forskolin诱导的hCB1-CHO细胞中则不显示增强作用。 |
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T81390
|
Prolactin-Releasing Peptide (1-31) (rat)
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Prolactin-Releasing Peptide (1-31) (rat) 通过减少禁食诱导的大鼠食物摄入，有效提升血浆LH、FSH及睾酮水平。 |
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TP2104
|
UFP-803
UFP 803
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Urotensin-II (UT) receptor ligand; behaves as a silent antagonist in most in vitro assays and in vivo, but does retain small residual agonist activity under certain conditions in some assays. Competitively antagonizes U-II induced contractions in the rat |
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T33631
|
Neocuproine
Neocuproin
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Neocuproine 是一种铜 （I） 螯合剂，可增强电场刺激引起的输精管收缩的嘌呤能成分，常被用作配位试剂和铜离子检测剂。Neocuproine 与铜离子形成稳定的络合物，并可在某些化学反应和分析方法中起到催化作用。Neocuproine 作为铁和钴上的氧化还原活性配体平台，对NSC34细胞氧化损伤的保护作用。 |
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T68371
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Rolapitant hydrochloride hydrate
|
|
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Rolapitant, also known as SCH-619734, is an orally bioavailable, centrally-acting, selective, neurokinin 1 receptor (NK1-receptor) antagonist with potential antiemetic activity. Upon oral administration, rolapitant competitively binds to and blocks the activity of the NK1-receptor in the central nervous system, thereby inhibiting the binding of the endogenous ligand, substance P (SP). This may prevent both SP-induced emesis and chemotherapy-induced nausea and vomiting (CINV). The interaction of ... |
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T13847
|
PROTAC SGK3 degrader-1
SGK3-PROTAC1
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SGK |
Metabolism |
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PROTAC SGK3 degrader-1 (SGK3-PROTAC1) 是一种靶向 SGK3 且与 VH032 VHL 结合配体的 PROTAC 偶联物，可诱导内源性 SGK3 降解。PROTAC SGK3 degrader-1 可抑制GDC0941诱导的癌细胞增殖。 |
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T76195
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Stresscopin-related peptide (human)
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Stresscopin-related peptide (human) 是 2 型 CRH 受体的特异性配体。Stresscopin-related peptide (human) 抑制食物摄入，延迟胃排空，并减少热引起的水肿。Stresscopin-related peptide (human) 在应激后维持体内平衡，可用于应激相关疾病的研究。 |
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T75839
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Kisspeptin-10, rat TFA
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|
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Kisspeptin-10, rat TFA 作为有效的血管收缩剂及血管生成抑制剂，为GPR54 (亦称KISS1) 亲吻蛋白受体的配体。此外，Kisspeptin-10, rat TFA 能降低Methotrexate引起的生殖毒性并显示出抗氧化潜力。 |
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T36982
|
CXCR3 Antagonist 6c
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CXCR3 antagonist 6c is an antagonist of chemokine (C-X-C motif) receptor 3 (CXCR3).1It inhibits calcium mobilization induced by chemokine (C-X-C motif) ligand 11 (CXCL11) in HEK293 cells expressing the human receptor (IC50= 0.06 μM). It is selective for CXCR3 over a panel of 14 human G protein-coupled receptors at 10 μM. CXCR3 antagonist 6c inhibits CXCR3-mediated migration of isolated human T cells (IC50= ~100 nM).
1.Cole, A.G., Stroke, I.L., Brescia, M.-R., et al.Identification and initial eva... |
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T61846
|
CM398
|
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CM398 is an orally active chemical compound that acts as a highly selective ligand for the sigma-2 receptor (K i =0.43 nM), demonstrating a significant ratio of selectivity between sigma-1 and sigma-2 receptors (1000-fold). Moreover, CM398 exhibits notable affinity towards dopamine (K i =32.90 nM) and serotonin transporters (K i =244.2 nM). In addition, CM398 has shown promising efficacy as an anti-inflammatory analgesic in a mouse model of inflammatory pain induced by formalin [1]. |
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T75776
|
R18 TFA
|
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R18 TFA 是14-3-3的肽拮抗剂，其KD 值为 70-90 nM。R18 可有效阻断14-3-3 与其配体Raf-1激酶的结合，可有效地消除14-3-3对磷酸酶诱导的Raf-1失活的保护作用。 |
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T70352
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PH11
|
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PH11 is a novel Focal Adhesion Kinase (FAK) inhibitor. PH11 restores TRAIL apoptotic pathway in PANC-1 cells through down-regulation of c-FLIP via inhibition of FAK and the phosphatidylinositol-3 kinase (PI3K)/AKT pathways. Tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) emerges as one of the most-promising experimental cancer therapeutic drugs and is currently being tested in clinical trials. However, both intrinsic and acquired resistance of human cancer cells to TRAIL... |
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T70377
|
BAY 61-3606 HCl
|
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BAY 61-3606 HCl is a cell-permeable, reversible inhibitor of spleen tyrosine kinase. BAY 61-3606 HCl can inhibit degranulation and block cytokine release from mast cells. Oral administration of BAY 61-3606 to rats was shown to suppress antigen-induced passive cutaneous anaphylactic reaction, bronchoconstriction, and bronchial edema. It can also sensitize MCF-7 breast cancer cells to TNF-related apoptosis-inducing ligand (TRAIL)-mediated apoptosis by inhibiting Cdk9. This compound has been used i... |
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T37013
|
(+/-)-PPCC oxalate
|
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Selective sigma (σ) receptor ligand. Displays high affinity for σ1; also binds at σ2 sites (Ki = 1.5 nM and 50.8 nM respectively). Selective over a range of receptor types including dopaminergic and muscarinic receptors, DAT and SERT.
Prezzavento et al (2007) Novel sigma receptor ligands: synthesis and biological profile. J.Med.Chem. 50 951 PMID:17328523 |Prezzavento et al (2008) A new sigma ligand, (±)-PPCC, antagonizes kappa opioid receptor-mediated antinociceptive effect. Life Sci. 82 549 PMI... |
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T37619
|
Leukotriene B4 Ethanolamide
|
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The effects of Leukotriene B4 (LTB4) are mediated by two known receptors, BLT1 and BLT2. LTB4 is a high affinity ligand for BLT1, and many of its pro-inflammatory effects are believed to be transduced through this receptor. The BLT2 is more enigmatic, in that LTB4 is not a high-affinity ligand, nor is it clear that BLT2 activation promotes inflammation. LTB4 ethanolamide (LTB4-EA) is a theoretical 5-LO metabolite of arachidonoyl ethanolamide (AEA). In CHO cells transfected with human BLTR1, LTB4... |
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T71306
|
Gemfibrozil-d6
|
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Gemfibrozil-d6 is intended for use as an internal standard for the quantification of gemfibrozil by GC- or LC-MS. Gemfibrozil is a peroxisome proliferator-activated reporter α and PPARγ agonist. In vivo, gemfibrozil reduces serum total cholesterol, triglyceride, and LDL levels in a rat model of high-cholesterol diet-induced hyperlipidemia. Gemfibrozil reduces atherosclerotic plaque area, superoxide production, and expression of the genes encoding the NF-κB subunit p65 and chemokine (C-C) motif l... |
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T38087
|
20-hydroxy Leukotriene B4
20-hydroxy Leukotriene B4
|
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20-hydroxy LTB4 is a metabolite of LTB4 in human neutrophils. In human leukocytes, LTB4 is inactivated by the enzyme LTB4 20-hydroxylase. 20-hydroxy LTB4 is not only much less active (~5%) compared to LTB4 in causing degranulation of PMNL, but actually inhibits LTB4-induced degranulation of human neutrophils (Ki = 13.3 nM). However, 20-hydroxy LTB4 is as active as LTB4 in contracting parenchymal strips from guinea pig lung. 20-hydroxy LTB4 retains considerable ligand binding affinity at the BLT2... |
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T76420
|
Nocistatin
|
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Nocistatin 是一种神经肽，是孤儿类阿片受体的内源性配体。 Nocistatin 还是神经肽伤害感受肽或孤啡肽 FQ (Noc/OFQ) 的功能性拮抗剂。Nocistatin 通过 Gi/o 蛋白介导途径抑制 5-HT 释放。Nocistatin 阻断 Nociceptin 诱导的异常性疼痛和痛觉过敏。 |
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T83926
|
S-Geranylgeranyl-L-glutathione
GGG
|
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S-Geranylgeranyl-L-glutathione是孤儿G蛋白偶联受体（GPCR）P2RY8的配体。该化合物在100 nM浓度下，选择性地诱导P2RY8而非鞘氨醇-1-磷酸受体2（S1P2）、GPR55、半胱氨酸白三烯受体1（CysLT1 receptor）以及CysLT2 receptor的内吞作用。在10 nM浓度下，S-Geranylgeranyl-L-glutathione抑制了表达P2RY8的WEHI-231 B细胞淋巴瘤细胞和分离的人扁桃体生发中心B细胞由趋化因子（C-X-C motif）配体12（CXCL12）诱导的迁移。 |
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T35463
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(±)14(15)-EET
(±)14,15-EET,(±)14,15-EpETrE,(±)14(15)-EET
|
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(±)14(15)-EET is a metabolite of arachidonic acid that is formed via epoxidation of arachidonic acid by cytochrome P450.[1],[2] It prevents increases in leukotriene B4, ICAM-1, and chemokine (C-C motif) ligand 1 (CCL2) induced by oxidized LDL in primary rat pulmonary artery endothelial cells (RPAECs) when used at a concentration of 1 μM.[3] (±)14(15)-EET induces dilation of preconstricted isolated canine coronary arterioles (EC50 = 0.2 pM).[4] It reduces myocardial infarct size as a percentage o... |
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T36531
|
PAR2 (1-6) (mouse, rat)
PAR2 (1-6) (mouse, rat)
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PAR2 (1-6) is a synthetic peptide agonist of proteinase-activated receptor 2 (PAR2) that corresponds to residues 1-6 of the amino terminal tethered ligand sequence of mouse and rat PAR2. It also corresponds to residues 39-44 and 37-42 of the mouse and rat full-length sequences, respectively. PAR2 (1-6) induces relaxation in precontracted rat arteries in a concentration-dependent manner, an effect that can be reduced by the nitric oxide synthase inhibitor L-NNA . It inhibits keratinocyte growth i... |
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T63307
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AChE-IN-6
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AChE-IN-6 是一种多功能配体，可显着抑制 AChE 的活性，对 EeAChE 和 HuAChE 的 IC50 值分别为 0.20 μM 和 37.02 nM，并具有抗 Aβ 活性 (IC50= 1.92 μM，用于自诱导 Aβ1-42 聚集；IC50= 1.80 μM，用于分解 Aβ1-42 原纤维；IC50= 2.18 μM，用于 Cu2+ 诱导的 Aβ1- 42 聚集；IC50= 1.17 μM，用于解聚 Cu2+ 诱导的 Aβ1-42 原纤维)。AChE-IN-6 对阿尔茨海默病表现出研究潜力。 |
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T79666
|
WLB-89462
|
Sigma receptor |
GPCR/G Protein |
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WLB-89462（Compound 20c）是一种高选择性σ2受体配体（Ki：13 nM），展示出神经保护活性，并能有效改善由Aβ肽引发的大鼠短期记忆障碍。该化合物拥有出色的ADMET特性，包含良好的溶解度、无CYP抑制作用、优异的代谢稳定性、高渗透性、脑部可渗透性以及在啮齿类动物中经口服途径高暴露量。 |
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T68497
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FI-700
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FI-700 is a novel and potent FLT3 inhibitor with promising antileukemia activity. FI-700 showed a potent IC(50) value against FLT3 kinase at 20 nmol/L in an in vitro kinase assay. FI-700 showed selective growth inhibition against mutant FLT3-expressing leukemia cell lines and primary acute myeloid leukemia cells, whereas it did not affect the FLT3 ligand (FL)-driven growth of Wt-FLT3-expressing cells. Oral administration of FI-700 induced the regression of tumors in a s.c. tumor xenograft model ... |
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T37289
|
Resolvin D2 n-3 DPA
Resolvin D2 n-3 DPA
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Resolvin D2 n-3 DPA (RvD2 n-3 DPA) is a specialized pro-resolving mediator (SPM).1It is formed from docosapentaenoic acid , an intermediate in the conversion of eicosapentaenoic acid to docosahexaenoic acid , in human leukocytes. RvD2 n-3 DPA (1 nM) reduces TNF-α-induced chemotaxis and adhesion of isolated human neutrophils.In vivo, RvD2 n-3 DPA (100 ng/animal; i.v.) reduces peritoneal neutrophil infiltration and exudate levels of IL-6 and chemokine (C-C motif) ligand 2 (CCL2) in a mouse model o... |
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T36800
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EN219
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EN219 is a synthetic recruiter of the E3 ubiquitin ligase RNF114.1It binds to cysteine 8 (C8) in the intrinsically disordered region of RNF114 (RNF114-C8; IC50= 470 nM) and inhibits RNF114-induced autoubiquitination and p21 ubiquitination in a cell-free assay when used at a concentration of 50 μM. EN219 (1 μM) also interacts with cysteine residues in the tubulin β1 chain (TUBB1), heat shock protein 60 (Hsp60), also known as Hsp family D member 1 (HspD1), and histone H3.1 (HIST1H3A) in 231MFP hum... |
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T83769
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TC 14012 hydrochloride
H-Arg-Arg-Nal-Cys-Tyr-Cit-Lys-D-Cit-Pro-Tyr-Arg-Cit-Cys-Arg-NH2
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TC 14012是一种化学肽模拟的拮抗剂，针对趋化因子(C-X-C motif)受体4（CXCR4；IC50 = 2.9 nM）和CXCR7激动剂。它能在表达CXCR7的HEK293T细胞中诱导β-arrestin招募（EC50 = 350 nM）。TC 14012可减少HIV在MT-4细胞中的细胞病理效应（EC50 = 0.4 nM），并以CXCR4依赖的方式抑制HIV在体外进入（IC50 = 19.3 nM）。它还能抑制由趋化因子(C-X-C motif)配体12（CXCL12）在MDA-MB-231乳腺癌细胞和人脐静脉内皮细胞（HUVECs）中诱导的迁移，当使用浓度范围从10到1,000 nM时。在通过左前降（LAD）冠状动脉结扎诱导的急性心肌梗死小鼠模型中，TC 14012（10 mg/kg）能减少梗死面积。 |
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T83857
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Soluble Epoxide Hydrolase PROTAC 1a
sEH Proteolysis-targeting Chimera 1a,Soluble Epoxide Hydrolase Proteolysis-targeting Chimera 1a,sEH PROTAC 1a
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Soluble epoxide hydrolase (sEH) PROTAC 1a是一种利用蛋白质降解靶向嵌合体(PROTAC)技术，通过连接区域将cereblon配体1与sEH抑制剂t-TUCB结合。该化合物通过促进sEH的降解，特异性抑制sEH的水解酶活性(IC50 = 0.8 nM)，相较于其磷酸酶活性(IC50 = >10,000 nM)具有较高选择性。sEH PROTAC 1a还特定促进细胞质中而非过氧体中的sEH降解，并通过溶酶体而非蛋白酶体实现其降解。它能够降低thapsigargin诱导的HepG2与293T细胞中磷酸化的inositol-requiring enzyme 1α (IRE1α)水平和X-box结合蛋白1 (XBP1)剪接，表明能减少ER应激。 |
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T41156
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MS 39
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MS 39是突变型表皮生长因子受体(EGFR)的高效、高亲和力和选择性降解剂，具有的高效、高亲和力和选择性。MS 39 由吉非替尼通过连接物偶联至 VHL 配体，能有效地诱导突变型 EGFR 的降解（在 HCC827(外显子19 del)和 H3255 (L858R 突变)肺癌细胞系中的 DC50值分别为5 nM 和3.3 nM)，但在浓度高达10 μM 的野生型 EGFR 细胞系中无显著作用。MS 39在体外抑制 H3255肺癌细胞的增殖，并且在给药后在小鼠中具有生物利用性。 |
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T36717
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RWJ-56110 dihydrochloride
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RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 . RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell ap... |
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T83724
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TPP-1 hydrochloride
Targeting PD-L1 Peptide
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TPP-1是一种针对程序化细胞死亡蛋白1(PD-1)及其配体PD-1配体(PD-L1)之间蛋白-蛋白相互作用的肽抑制剂。它在无细胞实验中结合到PD-L1(Kd = 94.67 nM)。TPP-1 (20 µM)能逆转PD-L1在抗CD3激活的人类CD4+ T细胞中所引起的干扰素γ(IFN-γ)水平的下降。在使用HL-60白血病细胞与抗CD3激活的人类CD4+ T细胞共培养并在植入前预处理时，以4 mg/kg的剂量给药，可减少小鼠异种移植模型中的肿瘤体积。 |
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T83894
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4A7C-301-Nurr1 Agonist
4A7C-301-Nuclear Receptor-Related 1
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4A7C-301-Nurr1激动剂是一种核受体相关1（Nurr1）的激动剂。它通过与Nurr1配体结合域（LBD；IC50 = 48.22 nM）结合，增加了在使用SK-N-BE(2)C人神经母细胞瘤细胞进行的报告基因测定中Nurr1-LBD和全长Nurr1的转录活性（EC50s = 6.53 和 50-70 µM，分别）。每天5 mg/kg的4A7C-301-Nurr1激动剂能减少在经MPTP神经毒素或α-突触核蛋白过表达诱导的帕金森病鼠模型中纹状体和黑质compacta部分多巴胺能细胞的死亡，并减少运动和嗅觉缺陷，而不诱发类似运动障碍的行为。 |
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