58
3
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T5345 |
V-9302
|
Others | Others |
V-9302 是一种跨膜谷氨酰胺通量的竞争性拮抗剂。它选择性的靶向氨基酸转运体 ASCT2 (SLC1A5),不影响 ASCT1。它能够阻碍 HEK-293 细胞中由 ASCT2 介导的谷氨酰胺摄取 (IC50=9.6 μM)。 | |||
T9541 |
CTB
Cholera Toxin B subunit |
Epigenetic Reader Domain | Chromatin/Epigenetic |
CTB (Cholera Toxin B subunit) 是一种 p300 组蛋白乙酰转移酶的激活剂,可诱导 MCF-7 细胞凋亡。 | |||
T7882 |
Indomethacin farnesil
吲哚美辛法呢酯,Infree |
Others; COX; Autophagy | Autophagy; Immunology/Inflammation; Neuroscience; Others |
Indomethacin farnesil (Infree) 是具有口服活性的 Indomethacin 前药,可通过干扰溶酶体的正常功能来破坏自噬流,有抗炎和抗风湿作用。它是一种可透过血脑屏障的,非选择性的 COX1和 COX2抑制剂,在 CHO 细胞中,对人 COX-1 和 COX-2 的IC50值分别为 18 nM 和 26 nM。 | |||
T41286 |
N6-Isopentenyladenosine
|
Endogenous Metabolite; Autophagy | Autophagy; Metabolism |
N6-Isopentenyladenosine 是甲羟戊酸途径的终产物,是一种具有抗黑色素瘤活性的自噬抑制剂。 N6-Isopentenyladenosine 是一种在细胞分裂素中发现的 RNA 修饰,可调节植物生长/分化,提高翻译的效率和准确性。 | |||
TQ0002 |
A-317491
ABT 202 |
P2X Receptor | Membrane transporter/Ion channel; Neuroscience |
A-317491 (ABT 202) 是选择性和非核苷酸的 P2X3和 P2X2/3受体的拮抗剂,通过阻断 P2X3和 P2X2/3受体介导的钙通量减轻炎性和神经性疼痛。它对其他 P2 受体和神经递质受体,离子通道以及酶具有高度选择性,IC50大于10 μM。 | |||
T1434 |
Clarithromycin
A-56268,克拉霉素 |
P450; ribosome; MRP; Antibacterial; Antibiotic; Autophagy | Autophagy; Immunology/Inflammation; Metabolism; Microbiology/Virology |
Clarithromycin (A-56268) 具有广谱的抗菌活性。它抑制 CYP3A4催化的三唑仑 α-羟基化,IC50(Ki) 值为 56 (43) μM。它抑制 HERG 钾电流。它可削弱连接 hERG1 和 PI3K 的信号通路影响自噬流 。 | |||
T9207 |
GW406108X
GW108X |
Kinesin; Autophagy | Autophagy; Cytoskeletal Signaling |
GW406108X (GW108X) 是一种 Kif15 抑制剂,在 ATPase 测定中的 IC50 为 0.82 uM。 它也是一种 ULK1 激酶抑制剂,pIC50 值为 6.37(427 nM),可阻断自噬通量。 | |||
T21136 |
Fluxapyroxad
|
Antifungal | Microbiology/Virology |
Fluxapyroxad 是合成的广谱杀菌剂,用于控制真菌病害。它可阻碍线粒体呼吸链复合体 II 中的琥珀酸脱氢酶的作用,进而抑制真菌目标物种内的孢子萌发、芽管和菌丝生长。 | |||
T11307 |
Fluxametamide
4-[5-(3,5-二氯苯基)-4,5-二氢-5-(三氟甲基)-3- 异恶唑基]-N-[(甲氧基氨基)亚甲基]-2-甲基苯 甲酰胺 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Fluxametamide 是广谱杀虫剂,是 GABA-和谷氨酸门控氯离子通道拮抗剂,对 M. domestica 中 GABACl 和 GluCl 的IC50值分别为 1.95 和 225 nM。 | |||
T72521 | Efflux inhibitor-1 | ||
Efflux inhibitor-1为一种吡唑啉[1,5-a]嘧啶类外排抑制剂,具有对ABCG2/BCRP和ABCB1的选择性靶向性,优先靶向ABCG2,其IC50值分别为0.45 μM与2.17 μM。 | |||
T60036 |
ML-SA5
|
Autophagy | Autophagy |
ML-SA5 是一种 MCOLN1 激动剂,通过扰乱自噬体和溶酶体之间的融合来阻止自噬通量。 | |||
T27060 |
CP-226269
CP 226269,CP226269 |
Dopamine Receptor | GPCR/G Protein; Neuroscience |
CP-226269 是一种高效的多巴胺 D4 受体 (dopamine D4 receptor) 激动剂,可以调节钙通量,其 EC50 值为32.0 nM。CP 226269 可用于研究精神分裂症等神经系统疾病。 | |||
T24859 | TC-AQP1-1 | Aquaporin | Membrane transporter/Ion channel |
TC-AQP1-1 是一种通过虚拟筛选鉴定的水通道蛋白 1 通道的阻断剂,并在低微摩尔浓度下抑制非洲爪蟾卵母细胞肿胀试验中通过 hAQP1 的水通量。 | |||
T11142 |
EACC
|
Autophagy | Autophagy |
EACC 是自噬的可逆抑制剂,可阻断自噬通量。它对自噬体特异性的 SNARE Stx17 易位具有选择性抑制作用,从而阻止自噬体与溶酶体的融合。 | |||
T68122 |
Oxmetidine
SKF 92994,Oxmetidina,Oxmetidinum |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Oxmetidine (SKF 92994) 是一种新型 H2 受体拮抗剂,具有细胞毒性。 Oxmetidine 抑制心脏和血管组织中跨膜钙通量,可用于治疗活动性十二指肠溃疡。 | |||
T14688 |
BMS CCR2 22
|
CCR | Immunology/Inflammation; Microbiology/Virology |
BMS CCR2 22 是一种有效的选择性 CC 型趋化因子受体2拮抗剂,钙通量 IC50为 18 nM,趋化性 IC50为1 nM,结合 IC50为5.1 nM。 | |||
T41008 |
BODIPY-Cholesterol
BCh2 |
||
BODIPY-Cholesterol (TF-Chol)是一种带有荧光 BODIPY 基团和细胞通透性的胆固醇类似物,是一种新型 BODIPY 胆固醇探针。BODIPY-Cholesterol 可用于研究细胞内固醇摄取和细胞器间固醇通量。 | |||
T3528 |
Senicapoc
塞尼卡泊,ICA-17043 |
Potassium Channel | Membrane transporter/Ion channel |
Senicapoc (ICA-17043) 是有效的,选择性的Gardos 通道 (Ca2+激活的 K+通道;KCa3.1) 阻断剂,IC50为 11 nM。Senicapoc 阻断人红细胞的 Ca2+诱导的铷通量,IC50为 11 nM, 抑制红细胞脱水的IC50为 30 nM。 | |||
T13041 |
Surfactin
|
HSV | Microbiology/Virology |
Surfactin 是一种有效的环状脂肽生物表面活性剂,可介导单价和二价阳离子(如钙)穿过脂质双层膜的通量,具有抗菌、抗真菌、抗支原体和溶血作用。 | |||
T0802 |
Procaine hydrochloride
Novocaine HCl,Procaine HCl,盐酸普鲁卡因 |
Histone Demethylase; 5-HT Receptor; DNA/RNA Synthesis; Sodium Channel; NMDAR; AChR | Cell Cycle/Checkpoint; Chromatin/Epigenetic; DNA Damage/DNA Repair; GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience |
Procaine hydrochloride (Novocaine HCl) 是DNA 脱甲基剂,是一种苯甲酸衍生物,具有局部麻醉和抗心律失常特性。 | |||
T3465L |
Vesnarinone HCl
Synonym 2,OPC-8212 HCl,Vesnarinone HCl(81840-15-5 Free base) |
Potassium Channel; Calcium Channel; PDE | Membrane transporter/Ion channel; Metabolism |
Vesnarinone HCl (OPC-8212 HCl) 是一种具有口服活性的 phosphodiesterase 3 (PDE3) 抑制剂。Vesnarinone HCl 可对钙离子和钾离子进行调节, 增加钙通量,减少钾通量。Vesnarinone HCl 是一种新的正性肌力化合物,可增强心肌收缩力,可用于心力衰竭的研究。 | |||
T1083L |
Theophylline monohydrate
Quibron,茶碱一水合物 |
HDAC; PDE; Adenosine Receptor | Chromatin/Epigenetic; DNA Damage/DNA Repair; GPCR/G Protein; Metabolism; Neuroscience |
Theophylline monohydrate (Quibron) 似乎抑制磷酸二酯酶和前列腺素的产生,调节钙通量和细胞内钙分布,并拮抗腺苷。茶碱是黄嘌呤的天然生物碱衍生物,从植物山茶花和小粒咖啡中分离出来。在生理上,该药剂可放松支气管平滑肌,产生血管舒张(脑血管除外),刺激中枢神经系统,刺激心肌,利尿,增加胃酸分泌;它还可以抑制炎症并改善横膈膜的收缩性。 | |||
T11277 |
FG 7142
ZK 39106,LSU-65 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
FG 7142 (LSU-65) 是一种非选择性苯二氮卓类反向激动剂,对含 α1 亚基的 GABAA 受体具有高亲和力,Ki 为 91 nM。它还调节 GABA 诱导的 GABAA 受体上的氯离子通量,表达 α1 亚基,EC50为 137 nM。它可增加酪氨酸羟基化并导致小鼠大脑皮层中 β-肾上腺素受体的上调。 | |||
T14899 |
CCR1 antagonist 8
|
CCR | Immunology/Inflammation; Microbiology/Virology |
CCR1 antagonist 8, a third azaindazole series compound, is a CCR1 antagonist (IC50: 1.8 nM in Ca2+ flux assay). | |||
T12819 |
S130
|
Cysteine Protease | Proteases/Proteasome |
S130 is a high affinity, selectiveATG4B (a major cysteine protease) inhibitor (IC50 of 3.24 μM).It suppresses autophagy flux. | |||
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. | |||
T10710 |
CCR1 antagonist 9
|
CCR | Immunology/Inflammation; Microbiology/Virology |
CCR1 antagonist 9 is an effective and selective CCR1 antagonist (IC50: 6.8 nM in calcium flux assay). | |||
T14373 | AZD2423 | CCR | Immunology/Inflammation; Microbiology/Virology |
AZD2423 is a potent, selective, orally bioavailable, and non-competitive CCR2 chemokine receptor negative allosteric modulator and it has an IC50 of 1.2 nM for CCR2 Ca2+ flux [1][2][3]. | |||
T11452 |
GPR120 Agonist 1
|
GPR | Endocrinology/Hormones; GPCR/G Protein |
GPR120 Agonist 1 is a selective GPR120 agonist. In GPR120 transfected HEK293 cells, GPR120 Agonist 1 displays good EC50 of 42 nM and 77 nM for human and mouse GPR120 (the calcium flux assay), respectively. | |||
T10204 |
A-317491 sodium salt hydrate
A-317491 sodium salt hydrate (475205-49-3 free base) |
Others | Others |
A-317491 sodium salt hydrate is a non-nucleotide P2X3 and P2X2/3 receptor antagonist, which inhibits calcium flux mediated by the receptors. | |||
T40064 |
V-9302 hydrochloride
|
||
V-9302 hydrochloride is a potent and selective competitive antagonist that inhibits transmembrane glutamine flux by specifically targeting the amino acid transporter ASCT2 (SLC1A5), and not ASCT1. In HEK-293 cells, V-9302 hydrochloride effectively inhibits ASCT2-mediated glutamine uptake with an IC50 value of 9.6 μM. | |||
T24623 |
PF-06807656
PF 06807656 |
||
PF-06807656 is insensitive to the introduction of the N171D mutation in the ROMK conduction pore that greatly diminishes the activity of other small-molecule inhibitors. PF-06807656 is an effective ROMK inhibitor (Tl+ flux IC50 = 160 nM). | |||
T11966 |
MCHR1 antagonist 2
|
HER; Melanin-concentrating Hormone Receptor (MCHR) | Angiogenesis; GPCR/G Protein; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
MCHR1 antagonist 2 是有效的黑色素聚集激素受体 1 拮抗剂,IC50为 65 nM。它也抑制hERG,在IMR-32 细胞中的IC50为 4.0 nM。 | |||
T28893 |
SX-517
SX 517 |
||
SX-517 is a potent noncompetitive boronic acid CXCR1/2 antagonist. SX-517 inhibits CXCL1-induced Ca(2+) flux (IC50 = 38 nM) in human PMNs. | |||
T38157 |
Ricinelaidic Acid
|
||
Ricinelaidic acid is a 12-hydroxy fatty acid and an antagonist of leukotriene B4 (LTB4) receptors (Ki = 2 μM in porcine neutrophil membranes). It inhibits chemotaxis and calcium flux induced by LTB4 in isolated human neutrophils (IC50s = 10 and 7 μM, respectively). Ricinelaidic acid (1 mg/kg, i.v.) inhibits bronchoconstriction induced by LTB4 in rats by 46%. | |||
T60749 |
Autophagy-IN-2
|
||
Autophagy-IN-2 (Compound 7h) 是自噬通量的抑制剂,可诱导癌细胞凋亡,具有研究三阴性乳腺的潜力。 | |||
T61420 |
CXCR4 antagonist 6
|
||
CXCR4 antagonist 6 (compound 46) is a highly potent inhibitor of CXCR4 with an IC50 value of 79 nM. It effectively inhibits the cytosolic calcium flux induced by CXCL12, achieving an IC50 of 0.25 nM. Moreover, CXCR4 antagonist 6 demonstrates significant mitigation of cell migration mediated by the CXCL12/CXCR4 interaction. Notably, this compound exhibits remarkable efficacy in a mouse model of cancer metastasis [1]. | |||
T36812 |
Linoleic Acid Amide
9,12-Octadecadienamide,Linoleamide,Linoleic Acid Amide |
Calcium Channel | Membrane transporter/Ion channel; Metabolism |
Linoleic Acid Amide (Linoleamide) 衍生自亚油酸,通过抑制肌肉/内质网 Ca2+-ATP 酶来调节 Ca2+ 通量。 | |||
T39662 | CCR4 antagonist 3 hydrochloride | ||
CCR4 antagonist 3 hydrochloride is an orally active, potent and selective CCR4 antagonist. CCR4 antagonist 3, featuring a novel piperidinyl-azetidine motif, has IC 50 s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4 antagonist 3 has antitumor activity. | |||
T39661 |
CCR4 antagonist 3
CCR4 antagonist 3 |
||
CCR4 antagonist 3 is an orally active, potent and selective CCR4 antagonist. CCR4 antagonist 3, featuring a novel piperidinyl-azetidine motif, has IC 50 s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4 antagonist 3 has antitumor activity. | |||
TP2141 |
Balixafortide TFA (1051366-32-5 free base)
Balixafortide TFA,POL6326 TFA |
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
Balixafortide TFA (POL6326 TFA) is a selective, well-tolerated peptidic CXCR4 antagonist (IC50 < 10 nM). It shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks β-arrestin recruitment and calcium fl | |||
TP2141L |
Balixafortide
POL6326 |
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM and it is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects[1][2]. Balixafortide blocks β-arresti | |||
T79668 |
PIK5-12d
|
Autophagy | Autophagy |
PIK5-12d为一种高效的PROTAC PIKfyve降解剂,具有显著的DC50值为1.48 nM。该化合物在多种前列腺癌细胞系中有效诱导细胞质空泡化,同时阻碍自噬流的进行,有效抑制前列腺癌细胞的增殖,并展现出抗肿瘤活性。 | |||
T14215 | AMG 837 sodium salt | Others | Others |
AMG 837 sodium salt is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents. IC50 value: 13 nM (EC50) [1] Target: GPR40 agonist AMG 837 displayed the expected t | |||
T65489 |
Tris(4,7-diphenyl-1,10-phenanthroline)ruthenium(II) dichloride
|
||
Tris(4,7-diphenyl-1,10-phenanthroline)ruthenium(II) dichloride is used as a probe for luminescent detection and quantitation of oxygen (absorption λmax=455 nm, luminescence λmax=613 nm). It is also used for fibre optic sensors. At the same time, Tris(4,7-diphenyl-1,10-phenanthroline)ruthenium(II) dichloride can be used in studies on oxygen in skin and skin tumors as well as measurement of oxygen flux through the skin. | |||
T75999 |
Balixafortide TFA
|
||
Balixafortide TFA (POL6326 TFA) 是一种有效的,选择性的,耐受性好的肽类CXCR4拮抗剂,其IC50小于 10 nM。Balixafortide TFA 对CXCR4的选择性比包括CXCR7在内的许多受体高出 1000 倍。Balixafortide TFA 以 IC50< 10 nM 阻断β-arrestin 募集和钙通量。Balixafortide TFA 还是一种有效的造血干细胞和祖细胞 (HSPC) 动员剂,并具有抗癌作用。 | |||
T36064 |
N-Oleoyl Glutamine
|
||
N-Oleoyl glutamine is an endogenous N-acyl amine.1,2It is both formed and degraded by peptidase M20 domain-containing 1 (PM20D1), a factor secreted by thermogenic adipose cells. N-Oleoyl glutamine (50 μM) induces mitochondrial uncoupling to increase respiration in C2C12 cells by 64%.3It inhibits capsaicin-induced calcium flux in HEK293A cells co-transfected with transient receptor potential vanilloid 1 (TRPV1) and red fluorescent protein (RFP).2N-Oleoyl glutamine (100 mg/kg) reduces the number o... | |||
T14216 |
AMG 837
|
Others | Others |
AMG 837 was found to be a partial agonist on GPR40 with maximal activity 85% of that shown by DHA under our standard assay conditions. Overall, AMG 837 was both highly potent and selective in vitro. AMG 837 is a potent GPR40 agonist(EC50=13 nM) with a sup | |||
T11896 |
LV-320
|
Cysteine Protease | Proteases/Proteasome |
LV-320 是一种有效且非竞争性的ATG4B 抑制剂,其IC50值为 24.5 μM,Kd 值为 16 μM。 LV-320 抑制ATG4B 的酶促活性,阻断细胞自噬,并且稳定无毒,在体内具有活性。 | |||
T35918 |
N-Arachidonoyl Taurine
|
||
N-Arachidonoyl taurine is an arachidonoyl amino acid. It is oxygenated by 12(S)- and 15(S)-lipoxygenase and is converted to 12-HETE-taurine (12-HETE-T) in murine resident peritoneal macrophages. N-Arachidonoyl taurine is an activator of the transient receptor potential vanilloid (TRPV) channels TRPV1 and TRPV4 (EC50s = 28 and 21 μM, respectively). It increases calcium flux in HIT-T15 pancreatic β-cells and INS-1 rat islet cells when used at a concentration of 10 μM and increases insulin secretio... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TN1721 |
Gypenoside L
|
ERK; p38 MAPK; Calcium Channel; NF-κB; ROS | Immunology/Inflammation; MAPK; Membrane transporter/Ion channel; Metabolism; NF-κB |
Gypenoside L 是存在于绞股蓝中的一种皂苷,可增加 SA-β-半乳糖苷酶活性,促进衰老相关分泌细胞因子的产生。它还可以激活p38和ERK MAPK 通路和NF-κB 通路以诱导衰老,具有抗肿瘤和抗炎活性。 | |||
TN2118 |
Lup-20(29)-en-28-oic acid
Pulsatilla saponin D,白头翁皂苷D |
ERK; mTOR; Autophagy | Autophagy; MAPK; PI3K/Akt/mTOR signaling |
Lup-20(29)-en-28-oic acid exhibits anticancer activities in various cancer types, it Inhibits autophagic flux and synergistically enhances the anticancer activity of chemotherapeutic agents against HeLa cells.Pulsatilla saponin D has strong haemolytic act | |||
T19882 |
Bryonolic acid
UNII-J7YR6A878I,20-epi-Bryonolic acid |
Apoptosis; Antioxidant; Calcium Channel | Apoptosis; Membrane transporter/Ion channel; Metabolism; oxidation-reduction |
Bryonolic acid (20-epi-Bryonolic acid) 是一种从 Sandoricum indicum 提取的三萜类化合物,具有免疫调节、抗炎,抗氧化和抗癌等活性,通过抑制Ca2+内流和调节Ca2+-CaMKII-CREB信号通路中的基因表达来避免PC12细胞免受NMDA诱导的细胞凋亡反应。 |