151
39
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T41099 |
EGFR Protein Tyrosine Kinase Substrate
|
||
EGFR Protein Tyrosine Kinase Substrate is a EGFR protein tyrosine kinase substrate. | |||
TP1269 |
Tyrosine Protein Kinase JAK 2 (Phospho-Tyr8, 9)
Tyrosine Protein Kinase JAK2 Phospho-Tyr8, 9 |
||
Tyrosine Protein Kinase JAK 2 (Phospho-Tyr8, 9) is a peptide derived from mouse JAK2, specifically composed of amino acids 475 to 491. | |||
T2314 |
PF-431396
|
FAK; PYK2 | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
PF 431396 是一种具有口服活性的 FAK (IC50:2 nM) 和 Pyk2 (IC50:11 nM)的抑制剂。 | |||
T5480 |
BI-4464
|
FAK; Ligands for Target Protein for PROTAC | Angiogenesis; Cytoskeletal Signaling; PROTAC; Tyrosine Kinase/Adaptors |
BI-4464 是一种高选择性的 ATP 竞争性 PTK2/FAK 抑制剂,IC50=17 nM。它可用于PROTAC 降解剂的 PTK2 配体。 | |||
T6997 |
SU6656
|
FAK; Akt; Src | Angiogenesis; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
SU6656 是Src 家族激酶抑制剂,抑制 Src,Yes,Lyn,Fyn 的IC50分别为 280,20,130,170 nM。它还能抑制p-AKT。它可抑制FAK Y576/577、 Y925、Y861位点的磷酸化。 | |||
T9576 |
AMP-945
|
FAK | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
AMP-945 是一种粘着斑激酶抑制剂。 | |||
T9973 |
FAK-IN-7
|
FAK | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
FAK-IN-7 有潜在的抗增殖活性,是一种 FAK 抑制剂。 | |||
T2001 |
PF-573228
PF 573228 |
Apoptosis; FAK | Angiogenesis; Apoptosis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
PF-573228是一种选择性的 FAK 抑制剂,对 FAK 纯化重组催化片段的 IC50值为4 nM。 | |||
T2465 |
PF-562271
PF562271,PF 562271 |
FAK; PYK2; CDK | Angiogenesis; Cell Cycle/Checkpoint; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
PF-562271 是一种可逆的,有效的,ATP 竞争性的 FAK (IC50:1.5 nM)和 Pyk2 (IC50:13 nM)激酶抑制剂。 | |||
T6177 |
PF-562271 besylate
PF-00562271 Besylate |
FAK; PYK2; CDK | Angiogenesis; Cell Cycle/Checkpoint; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
PF-562271 besylate (PF-00562271 Besylate) 是一种可逆的,有效的,ATP 竞争性的 FAK(IC50:1.5 nM)和 Pyk2 (IC50:13 nM)激酶抑制剂。 | |||
T1835 |
Ibrutinib
伊布替尼,依鲁替尼,PCI-32765 |
Tyrosine Kinases; Src; BTK; Ligands for Target Protein for PROTAC | Angiogenesis; PROTAC; Tyrosine Kinase/Adaptors |
Ibrutinib (PCI-32765) 是一种不可逆的、选择性的 Btk 抑制剂,IC50=0.5 nM,它是一种 Btk 配体,用于合成一系列 PROTAC 分子,如 P13I。P13I 作用于人 Burkitt’s 淋巴瘤 RAMOS 细胞,浓度为 10 和 100 nM 时,分别降解 73% 和 89% Btk。 | |||
T2655 |
CEP-37440
CEP37440 |
FAK; ALK | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
CEP-37440 是一种新型的 FAK (IC50:2.3 nM) 和 ALK (IC50:120 nM) 双重抑制剂。 | |||
T21768 |
PF-562271 hydrochloride
PF-562271 HCl |
FAK; PYK2; CDK | Angiogenesis; Cell Cycle/Checkpoint; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
PF-562271 hydrochloride (PF-562271 HCl) 是一种可逆的,有效的,ATP 竞争性的 FAK (IC50:1.5 nM)和 Pyk2 (IC50:13 nM)激酶抑制剂。 | |||
T4337 |
PCI 29732
PCI29732,PCI-29732 |
Others; BCRP; BTK | Angiogenesis; Membrane transporter/Ion channel; Others; Tyrosine Kinase/Adaptors |
PCI 29732 是一种有效的可逆BTK 抑制剂,对 BTK、Lck 和 Lyn 的Kiapp 值分别为 8.2、4.6 和 2.5 nM。它通过竞争性结合ABCG2 的 ATP 结合位点来抑制ABCG2的功能。 | |||
T10285 |
ALK inhibitor 1
|
FAK; IGF-1R; ALK | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
ALK inhibitor 1 是嘧啶类 ALK 的有效抑制剂。它是一种睾丸特异性丝氨酸/苏氨酸激酶 2 (TSSK2;IC50=31 nM) 和粘着斑激酶 (FAK;IC50=2 nM) 抑制剂。 | |||
T1918 |
NVP-TAE 226
TAE226 |
Apoptosis; FAK; c-Met/HGFR; PYK2; IGF-1R | Angiogenesis; Apoptosis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
NVP-TAE 226 (TAE226) 是一种具有 ATP 竞争性的双重FAK 和IGF-1R 抑制剂,IC50分别为 5.5 nM、140 nM。它还抑制Pyk2、胰岛素受体,IC50分为 3.5 nM、40 nM。 | |||
T3041 |
ALK inhibitor 2
|
FAK; ALK | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
ALK inhibitor 2 是嘧啶类 ALK 的有效抑制剂。它是一种睾丸特异性丝氨酸/苏氨酸激酶 2 (TSSK2;IC50=37 nM) 和粘着斑激酶 (FAK;IC50=5 nM) 抑制剂。 | |||
T2281 |
GSK2256098
GSK 2256098,GSK-2256098,GTPL7939 |
Apoptosis; FAK | Angiogenesis; Apoptosis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
GSK2256098 (GTPL7939) 是一种选择性FAK 激酶抑制剂,抑制胰腺癌细胞的生长和存活。 | |||
T2066 |
Quizartinib
AC220,奎扎替尼 |
Apoptosis; FLT; Autophagy; Ligands for Target Protein for PROTAC | Angiogenesis; Apoptosis; Autophagy; PROTAC; Tyrosine Kinase/Adaptors |
Quizartinib (AC220) 是一种具有口服活性的高选择性Ⅱ 型 FLT3酪氨酸激酶抑制剂,可诱导细胞凋亡。它抑制 Wt FLT3 和 突变型 FLT3-ITD 自磷酸化,IC50分别为 4.1 nM 和 1.1 nM。它可通过优化的 linker 与 VHL 配体连接,从而形成 PROTAC Flt3 降解剂。 | |||
T7541 |
PTP inhibitor 1
PTP Inhibitor II,alpha-溴-4-甲氧基苯乙酮 |
Phosphatase | Metabolism |
PTP inhibitor 1 是蛋白酪氨酸磷酸酶 (PTP) 抑制剂,具有抗血管生成作用。 | |||
T1996 |
Defactinib
PF-04554878,VS-6063 |
FAK | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Defactinib (VS-6063) 是新型的 FAK 抑制剂,能够时间和剂量依赖性的抑制 FAK 在 Tyr397 位点磷酸化。 | |||
T0827 |
Cefsulodin sodium
Cefsulodine sodium,Sulcephalosporin,头孢磺啶钠 |
Antibacterial; Antibiotic | Microbiology/Virology |
Cefsulodin sodium (Sulcephalosporin) 是β内酰胺抗生素,对缘脓杆菌和肠杆菌有活性。 | |||
T0263 |
Chloropyramine hydrochloride
Nilfan,盐酸氯吡胺,Alergosan,Halopyramine hydrochloride |
FAK; VEGFR; Histamine Receptor | Angiogenesis; Cytoskeletal Signaling; GPCR/G Protein; Immunology/Inflammation; Neuroscience; Tyrosine Kinase/Adaptors |
Chloropyramine hydrochloride (Alergosan) 是一种组胺受体 H1 拮抗剂,可抑制VEGFR-3和FAK 的生化功能。 | |||
T4636 |
Protein kinase inhibitors 1
|
Others; DYRK | Cell Cycle/Checkpoint; Others; Tyrosine Kinase/Adaptors |
Protein kinase inhibitors 1 是新型的 HIPK2 抑制剂,其 IC50=74 nM,Kd=9.5 nM。 | |||
T24730 |
Roslin 2 bromide
Roslin-2,Benzylhexamethylenetetramine bromide,Roslin2 |
FAK; p53 | Angiogenesis; Apoptosis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Roslin 2 bromide (Benzylhexamethylenetetramine bromide) 是一种 p53 再激活剂,可破坏 FAK 和 p53 的结合。 Roslin 2 bromide 具有抗癌作用。 | |||
T2609 |
Masitinib
AB1010,马赛替尼 |
Apoptosis; FAK; c-Fms; FGFR; Bcr-Abl; PDGFR; Src; c-Kit; Hck | Angiogenesis; Apoptosis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Masitinib (AB1010) 是生物口服可利用的选择性 c-Kit 抑制剂 (对于人重组c-Kit,IC50=200 nM),它还抑制PDGFRα/β(IC50s=540/800 nM),Lyn(对 LynB 的IC50=510 nM),Lck,较小程度上抑制FGFR3和FAK。它有抗增殖,促凋亡活性,且毒性低。 | |||
T4185 |
lavendustin C
HDBA,NSC 666251,N-(2,5-二羟基苄基)-5-氨基水杨酸 |
CaMK; EGFR; Tyrosinase; Src | Angiogenesis; JAK/STAT signaling; Neuroscience; Proteases/Proteasome; Tyrosine Kinase/Adaptors |
lavendustin C (NSC 666251) 是 Ca2+钙调蛋白依赖性激酶 II 抑制剂,IC50为 0.2 µM。它抑制 EGFR 相关酪氨酸激酶和 pp60c-src(+)激酶,IC50分别为 0.012 和 0.5 µM。 | |||
T1950 |
PND-1186
PND1186,PND 1186,VS-4718,SR-2516 |
Apoptosis; FAK | Angiogenesis; Apoptosis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
PND-1186 (VS-4718) 是一种高特异性的FAK 可逆抑制剂,IC50为 1.5 nM。它选择性促进肿瘤细胞凋亡。 | |||
T7119 |
Y15
1,2,4,5-苯四胺四盐酸盐,1,2,4,5-Benzenetetramine tetrahydrochlor,FAK Inhibitor 14 |
FAK | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Y15 (1,2,4,5-Benzenetetramine tetrahydrochlor) 是一种特异性的粘着斑激酶抑制剂,能够降低其自身磷酸化活性,抑制癌细胞的活力,阻断肿瘤生长。 | |||
T2160 |
Suramin Sodium Salt
苏拉明钠,BAY-205,Suramin hexasodium salt,苏拉明钠盐,NF-060 |
Apoptosis; Phosphatase; SARS-CoV; Sirtuin; Reverse Transcriptase; Topoisomerase; Parasite | Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair; Metabolism; Microbiology/Virology |
Suramin Sodium Salt (BAY-205) 是可逆的竞争性蛋白酪氨酸磷酸酶抑制剂。它抑制 IP5K,是抗寄生虫,抗肿瘤和抗血管生成剂。它是sirtuins 的有效抑制剂,也是 SARS-CoV-2 RNA 依赖性 RNA 聚合酶抑制剂。 | |||
T31458 |
DiFMUP
|
||
DiFMUP is the fluorescent substrate of protein tyrosine phosphatase. | |||
T21761 |
HNMPA
|
IGF-1R | Tyrosine Kinase/Adaptors |
HNMPA 是膜不可渗透的胰岛素受体酪氨酸激酶 (insulin receptor tyrosine kinase) 抑制剂。HNMPA 可以抑制人胰岛素受体的酪氨酸和丝氨酸自磷酸化。HNMPA 对环 AMP 依赖性蛋白激酶或蛋白激酶 C 活性没有影响。 | |||
T7381 |
TCS 401
|
Phosphatase | Metabolism |
TCS 401 是一种选择性的蛋白酪氨酸磷酸酶 1B 抑制剂。 | |||
T12578 |
(E,E)-RAMB4
PTP1B-IN-8 |
Phosphatase | Metabolism |
PTP1B-IN-8 is a potent and selective inhibitor of protein tyrosine phosphatase-1B (PTP1B). | |||
T4256 |
PTP1B-IN-2
|
Phosphatase | Metabolism |
PTP1B-IN-2 是一种蛋白酪氨酸磷酸酶抑制剂,IC50=50 nM。 | |||
T4511 |
ST271
ST 271 |
Phospholipase; Tyrosine Kinases | Metabolism; Tyrosine Kinase/Adaptors |
ST271 是蛋白质酪氨酸激酶 (PTK) 抑制剂,抑制 fMet-Leu-Phe 和 PAF 引起的 phospholipase D 活化的IC50值分别为 6.7 和 9 μM。 | |||
T7900 |
BAY-474
|
c-Met/HGFR | Tyrosine Kinase/Adaptors |
BAY-474 是酪氨酸蛋白激酶 c-MET 抑制剂,能够用于表观遗传学探针。 | |||
T7356 |
PTP1B-IN-1
PTP1B inhibitor,5-苯基-1,2,5-噻二唑烷-3-酮 1,1-二氧化物 |
Phosphatase | Metabolism |
PTP1B-IN-1 (PTP1B inhibitor) 是一种蛋白质酪氨酸磷酸酶 1B 的有效抑制剂 (IC50 : 1.6 mM) | |||
TP1051L |
Protein Kinase C Peptide Substrate acetate
Protein Kinase C Peptide Substrate acetate(120253-69-2 free base) |
Others | Others |
Protein Kinase C Peptide Substrate acetate(120253-69-2 free base) 以依赖于第二信使和特定衔接蛋白的方式靶向特定细胞间隔物,以响应激活 g 蛋白偶联受体、酪氨酸激酶受体或酪氨酸激酶偶联受体的细胞外信号。 | |||
T50088 |
N-phenylthiophene-2-carboximidamide
|
Others | Others |
N-phenylthiophene-2-carboximidamide 是一种噻吩衍生物,可以作为蛋白酪氨酸激酶(PTKs)的抑制剂和 G 蛋白偶联受体(GPCR)的配体发挥作用。 | |||
T7101 |
Tyrphostin AG30
Tyrphostin AG30(AG30),酪氨酸磷酸化抑制剂 AG 30 |
EGFR; Tyrosine Kinases | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Tyrphostin AG30 (AG30) 是一种有效的蛋白质酪氨酸激酶 (PTK) 抑制剂,选择性地抑制 c-ErbB 的自我更新诱导,并能抑制原发性红细胞 c-ErbB 激活 STAT5。 | |||
T3211 |
Midostaurin
米哚妥林,N-Benzoylstaurosporine,PKC412,CGP41231,CGP 41251,苯甲酰基十字孢碱 |
Others; PKC | Chromatin/Epigenetic; Cytoskeletal Signaling; Others |
Midostaurin (PKC412) 是一种多靶点蛋白激酶抑制剂,有抗肿瘤活性,对 PKCα/β/γ、Syk、Flk-1、Akt、PKA、c-Kit、c-Fgr、c-Src、FLT3、PDFRβ和VEGFR1/2的IC50值范围为 22 到500 nM 之间。 | |||
T19498 |
p-Cresyl sulfate potassium
p-Tolyl sulfate potassium salt,p-Cresol sulfate potassium,p-Methylphenyl potassium sulfate,对甲基硫酸钾,Potassium p-tolyl sulfate |
Endogenous Metabolite | Metabolism |
p-Cresyl sulfate potassium (p-Tolyl sulfate potassium salt) 是一种尿毒症毒素,能够与原型蛋白质结合。 | |||
T14841 |
BVT948
|
Phosphatase; P450; Histone Methyltransferase | Chromatin/Epigenetic; Metabolism |
BVT948 是一种蛋白酪氨酸磷酸酶抑制剂,还可以抑制赖氨酸甲基转移酶 SETD8 (KMT5A) 和几种细胞色素 P450 (P450) 同工型。 | |||
T13013 |
Sodium stibogluconate
Stibogluconate trisodium nonahydrate,葡萄糖酸锑钠 |
Phosphatase | Metabolism |
Sodium stibogluconate (Stibogluconate trisodium nonahydrate) 是一种有效的蛋白酪氨酸磷酸酶 (phosphatase) 抑制剂。 它在10,100 和 100 μg/mL 时分别抑制 99% 的 SHP-1,SHP-2 和 PTP1B 活性。 | |||
T10190 |
7-BIA
|
Phosphatase | Metabolism |
7-BIA 是一种受体型蛋白酪氨酸磷酸酶 D (PTPRD) 抑制剂,具有抗抗成瘾作用,可用于研究神经性疼痛。 | |||
T67893 |
PTP1B-IN-22
|
Phosphatase | Metabolism |
PTP1B-IN-22是一种蛋白酪氨酸磷酸酶1B (PTP1B)抑制剂,可抑制骨骼肌 L6肌管的葡萄糖摄取。 | |||
T6217 |
LFM-A13
|
PLK; JAK; BTK | Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors |
LFM-A13 是一种 BTK,JAK2,PLK 有效抑制剂,可抑制 BTK、Plx1 和 PLK3 的活性,IC50分别为 2.5、10 和 61 μM。 | |||
T37184 |
CX08005
2-[(2-tetradecoxyphenyl)carbamoyl]benzoic acid |
Phosphatase | Metabolism |
CX08005 是一种蛋白酪氨酸磷酸酶 1B 抑制剂,可减轻与非酒精性脂肪肝相关的肝脏脂质蓄积和微循环障碍。 | |||
T4491 |
LMPTP INHIBITOR 1 hydrochloride
LMPTP INHIBITOR 1 hydrochloride (1908414-82-3(free base)) |
Phosphatase | Metabolism |
LMPTP INHIBITOR 1 hydrochloride 是一种高选择性的低分子量蛋白酪氨酸磷酸酶 (LMPTP) 抑制剂。LMPTP INHIBITOR 1 (hydrochloride) 能够抑制 LMPTP-A 的活性,IC50值为 0.8 μM。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TN1433 | Batatasin III | FAK; Others; Akt | Angiogenesis; Cytoskeletal Signaling; Others; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
Batatasin III 通过抑制上皮间质转化和 FAK-AKT 信号来抑制癌症迁移和侵袭,并具有抗癌活性。 Batatasin III 对整株生长有长期抑制作用,显示出抑制萌发活性。 | |||
T5S0761 |
Nitidine chloride
|
Apoptosis; ERK; FAK; p38 MAPK; NF-κB; Topoisomerase; STAT; Parasite | Angiogenesis; Apoptosis; Cytoskeletal Signaling; DNA Damage/DNA Repair; JAK/STAT signaling; MAPK; Microbiology/Virology; NF-κB; Stem Cells; Tyrosine Kinase/Adaptors |
Nitidine chloride 是从Zanthoxylum nitidum (Roxb) DC 中分离得到的,具有抗疟疾活性。它通过多个靶点通路,起抗癌作用,抑制STAT3、DNA 拓扑异构酶1和2A、ERK 和c-Src/FAK 相关信号通路。它通过MAPK 和NF-kB 途径抑制Lps 诱导的炎性细胞因子的产生。 | |||
T3122 |
Fangchinoline
Tetrandrine B,防己诺林碱,(+)-Limacine,Hanfangichin B,防己醇灵,(+)-Fangchinoline |
Apoptosis; FAK; HIV Protease; Autophagy | Angiogenesis; Apoptosis; Autophagy; Cytoskeletal Signaling; Microbiology/Virology; Proteases/Proteasome; Tyrosine Kinase/Adaptors |
Fangchinoline (Tetrandrine B) 是从Stephaniatetrandra 中分离出来的,一种具有广泛生物学活性的天然产物。它是新型HIV-1抑制剂,通过损害 gp160 蛋白水解过程来抑制 HIV-1 复制。它靶向Focal adhesion kinase (FAK)并抑制肿瘤细胞中 FAK 介导的的信号传导途径。 | |||
T1695 |
DL-O-Tyrosine
|
Amino Acids and Derivatives | Metabolism |
DL-O-Tyrosine 是苯丙氨酸的代谢物,是形成儿茶酚胺的前体。它被用作β-地中海贫血中蛋白质氧化损伤的生物标志物。 | |||
TN1096 |
Ginsenoside Ra1
人参皂苷 Ra1,人参皂苷Ra1 |
Others; Tyrosine Kinases | Others; Tyrosine Kinase/Adaptors |
Ginsenoside Ra1 是来自人参的成分。 Ginsenoside Ra1 对缺氧/复氧诱导的蛋白酪氨酸激酶 (PTK) 活化具有显着抑制作用。 | |||
TN1053 |
Aloe-emodin-8-O-β-D-glucopyranoside
Aloe-emodin-8-O-beta-D-glucopyranoside,芦荟大黄素-8-O-β-D-葡萄糖苷 |
Phosphatase | Metabolism |
Aloe-emodin-8-O-β-D-glucopyranoside (Aloe-emodin-8-O-beta-D-glucopyranoside) 是一种分离自Saussrurea lappa 中的化合物,是一种温和的人类蛋白酪氨酸磷酸酶 1B 抑制剂,其IC50=26.6 μM。 | |||
T1737 |
Genistein
NPI 031L,三叶草,染料木素,金雀异黄酮 |
Apoptosis; EGFR; Endogenous Metabolite; Autophagy | Angiogenesis; Apoptosis; Autophagy; JAK/STAT signaling; Metabolism; Tyrosine Kinase/Adaptors |
Genistein (NPI 031L) 是一种大豆异黄酮,是一种多重的酪氨酸激酶抑制剂,通过改变细胞凋亡,细胞周期和血管生成以及抑制转移对多种癌症有化疗作用。 | |||
T6427 |
Butein
2’,3,4,4’-tetrahydroxy Chalcone,紫铆因 |
Apoptosis; EGFR; Others; PDE; Autophagy | Angiogenesis; Apoptosis; Autophagy; JAK/STAT signaling; Metabolism; Others; Tyrosine Kinase/Adaptors |
Butein (2’,3,4,4’-tetrahydroxy Chalcone) 是一种 cAMP 特异性PDE 抑制剂,也是蛋白酪氨酸激酶抑制剂,还是一种SIRT1激活剂。它通过 AKT 和 ERK/p38 MAPK 通路,靶向 FoxO3a 使 HeLa 细胞对 Cisplatin 敏感。 | |||
TN1470 |
Cassiaside B2
决明子苷B2 |
Phosphatase; MAO; 5-HT Receptor | GPCR/G Protein; Metabolism; Neuroscience |
Cassiaside B2 是蛋白酪氨酸磷酸酶1B (PTP1B) 和人单胺氧化酶A (hMAO-A) 的抑制剂。Cassiaside B2是 5-HT2C 受体的激动剂, 具有抗过敏活性。Cassiaside B2 是萘吡喃酮参比提取物(NRE)的有效成分之一。 | |||
TN2019 |
Orobol
3'-Hydroxygenistein,3’,4’,5,7-tetrahydroxy-isoflavon,3',4',5,7-四羟基异黄酮 |
BCL; Caspase; PI3K | Apoptosis; PI3K/Akt/mTOR signaling; Proteases/Proteasome |
Orobol (3’,4’,5,7-tetrahydroxy-isoflavon) 是酪氨酸特异性蛋白激酶和磷脂酰肌醇转换的抑制剂。Orobol 抑制 PI3K,对 PI3K α/β/γ/K/δ 的 IC50 为 3.46-5.27 μM。 Orobol 具有抗皮肤老化和抗肥胖的作用。 | |||
T0610 |
Piceatannol
白皮杉醇,trans-Piceatannol,Astringenin |
Apoptosis; Serine/threonin kinase; PKA; Syk; PKC; Autophagy | Angiogenesis; Apoptosis; Autophagy; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; Metabolism; Tyrosine Kinase/Adaptors |
Piceatannol (Astringenin) 是一种Syk 抑制剂,可降低由 TNF 诱导的 iNOS 表达,可研究急性肺损伤。它是存在于各种水果和蔬菜中天然存在的多酚二苯乙烯,可诱导细胞自噬和凋亡,具有抗癌和抗炎特性。 | |||
TN2111 |
Prunin
Naringenin 7-0-glucoside,柚皮素-7-O-葡萄糖苷 |
Phosphatase; Anti-infection; Virus Protease | Metabolism; Microbiology/Virology |
Prunin (Naringenin 7-0-glucoside) 是一种人肠道病毒 A71 抑制剂。它抑制蛋白酪氨酸磷酸酶 1B,IC50值为 5.5 μM。 | |||
T4S0878 |
Prunetin
樱黄素,Prunusetin |
ERK; Dehydrogenase; NF-κB | MAPK; Metabolism; NF-κB |
Prunetin (Prunusetin) 是一种O-甲基化异黄酮,具有抗炎的作用。它是人醛脱氢酶的有效抑制剂。 | |||
T4S0498 |
Glaucocalyxin A
蓝萼甲素,Wangzaozin B,Leukamenin F |
Apoptosis; Akt; Caspase; PI3K | Apoptosis; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Proteases/Proteasome |
Glaucocalyxin A (Leukamenin F) 是来自日本黑纹病菌的一种对映型月桂基二萜,具有抗肿瘤作用。它通过调节PI3K/Akt 信号通路抑制 GLI1 的核易位,诱导骨肉瘤凋亡。 | |||
T3S1612 |
kuwanon G
桑黄酮G,Moracenin B,桑黄酮 G,Kuwanone G |
Phosphatase; Antibacterial; Bombesin Receptor; AChR; AChE; Glucosidase | GPCR/G Protein; Metabolism; Microbiology/Virology; Neuroscience |
Kuwanon G (Moracenin B) 是一种从桑树中得到的黄酮类蛙皮素受体拮抗剂,具有杀菌作用。 | |||
TN5400 |
Aerugidiol
|
||
Aerugidiol inhibits protein tyrosine phosphatase 1B (PTP1B). | |||
T20555 |
Glycyltyrosine
NSC 118362,Gly Tyr,NSC-118362,Gly-Tyr,NSC118362,N-Glycyl-L-tyrosine |
||
Glycyltyrosine, a dipeptide composed of tyrosine and glycine, is an incomplete breakdown product of protein catabolism or protein digestion. | |||
T19885 |
Methyllucidone
|
||
Methyllucidone is an inhibitor of STAT3 that acts by regulating the expression of the protein tyrosine phosphatase MEG2. | |||
TN3042 |
4-Hydroxycinnamamide
|
ATPase; EGFR; Potassium Channel; p38 MAPK; Calcium Channel; Sodium Channel; AMPK | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; MAPK; Membrane transporter/Ion channel; Metabolism; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
4-Hydroxycinnamamide has antioxidant activity. 4-Hydroxycinnamamide derivatives are specific inhibitors of tyrosine-specific protein kinases. | |||
T39219 | Ficusonolide | ||
Ficusonolide exhibits significant antidiabetic activity through its interactions with dipeptidyl peptidase-IV (DPP-IV), protein tyrosine phosphatase 1B (PTP-1B), α-glucosidase, and α-amylase. | |||
TN3335 |
Abyssinone V
|
Phosphatase | Metabolism |
Abyssinone V 是一种从刺桐茎皮中分离的天然化合物,是蛋白质酪氨酸磷酸酶 1B (PTP1B) 的抑制剂。 | |||
T13740 |
Isotanshinone IIA
|
Others | Others |
Isotanshinone IIA, could non-competitively inhibit Protein Tyrosine Phosphatase 1B (PTP1B) activity with an IC50 0f 11.4 μM. is an abietane-type diterpene metabolite. | |||
TN3505 | Beta-Peltoboykinolic acid | Phosphatase | Metabolism |
Beta-Peltoboykinolic acid has in vitro protein tyrosine phosphatase 1B (PTP1B) inhibitory, it inhibits PTP1B with IC50 values of 5.2+/-0.5 microM. It also has cytotoxic activity. | |||
TN2887 |
3,4-Secocucurbita-4,24-diene-3,26,29-trioic acid
|
Phosphatase | Metabolism |
(24E)-3,4-Seco-cucurbita-4,24-diene-3,26,29-trioic acid can inhibit the activity of protein tyrosine phosphatase 1B (PTP1B), with IC 50 values of 0.4uM. | |||
T73073 |
PTP1B-IN-21
|
||
PTP1B-IN-21 是蛋白酪氨酸磷酸酶 1B (PTP1B) 的选择性抑制剂 (IC50=1.56 μM),抑制力超出高度同源 T 细胞蛋白酪氨酸磷酸酶 (TCPTP;IC50>100 μM),PTP1B 是抑制 2 型糖尿病的重要靶点。 | |||
T73072 |
PTP1B-IN-20
|
||
PTP1B-IN-20 是蛋白酪氨酸磷酸酶 1B (PTP1B) 的选择性抑制剂 (IC50=1.05 μM),抑制力超出高度同源 T 细胞蛋白酪氨酸磷酸酶 (TCPTP;IC50=78.0 μM),PTP1B 是抑制 2 型糖尿病的重要靶点。 | |||
T38587 |
Chrysophanol triglucoside
|
||
Chrysophanol triglucoside is an anthraquinone isolated from Cassia obtusifolia , inhibits protein tyrosine phosphatases 1B (PTP1B) and α-glucosidase with IC 50 s of 80.17 and 197.06 μM, respectively. Chrysophanol triglucoside has the potential for diabetes research. | |||
TN2913 | 3-Acetoxy-11-ursen-28,13-olide | Phosphatase | Metabolism |
3β-Acetoxy-urs-11-en-28,13-olide exhibits significant protein tyrosine phosphatase 1B (PTP1B) inhibitory activity, it is a mixed-type PTP1B inhibitor. It exhibits weak-moderate antiproliferative activity against the A2780 human ovarian cancer cell line. | |||
TN1775 |
Isocryptotanshinone
|
ERK; JNK; STAT | JAK/STAT signaling; MAPK; Stem Cells |
Isocryptotanshinone inhibits protein tyrosine phosphatase 1B (PTP1B) activity with 50% inhibitory concentration values of 56.1±6.3 μM, PTP1B acts as a negative regulator of insulin signaling, and selective inhibition of PTP1B has served as a potential drug target for the treatment of type 2 diabetes. | |||
T3827 |
Rhein-8-glucoside calcium
大黄酸-8-O-β-D-葡萄糖苷,Rhein-8-O-β-D-glucopyranoside,Rhein-8-glucoside calcium salt |
Phosphatase; Antibacterial | Metabolism; Microbiology/Virology |
Rhein-8-glucoside calcium (Rhein-8-glucoside calcium salt) salt 是一种从 Saussurea lappa 根的 EtOH 提取物中,分离得到的蒽醌类 hPTP1B 抑制剂,IC50值为11.5 μM,具有抗菌作用。 | |||
T38069 |
Aquastatin A
|
||
Aquastatin A is a fungal metabolite originally isolated fromF. aquaeductuumthat has diverse biological activities.1It is active againstS. aureus(MIC = 32 μg/ml) and inhibits enoyl-acyl carrier protein reductase (Fabl; IC50= 3.2 μM) andS. aureusfatty acid synthesis (IC50= 3.5 μM).2Aquastatin A also inhibits the Na+/K+-ATPase and H+/K+-ATPase (IC50s = 7.1 and 6.2 μM, respectively), as well as protein tyrosine phosphatase 1B (PTP1B; IC50= 0.19 μM).1,3 1.Hamano, K., Kinoshita-Okami, M., Minagawa, K.... | |||
T75495 | Rubrofusarin 6-O-β-D-glucopyranoside | ||
Rubrofusarin 6-O-β-D-glucopyranoside为Rubrofusarin的糖苷形式,具有抑制蛋白酪氨酸磷酸酶 1B (PTP1B) 的活性,IC50值为87.36 μM,适用于糖尿病和抑郁症研究。 | |||
TN3525 |
Boehmenan
|
ERK; Phosphatase; EGFR; PARP; MEK; Wnt/beta-catenin; Akt; Caspase; STAT; p53 | Angiogenesis; Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair; JAK/STAT signaling; MAPK; Metabolism; PI3K/Akt/mTOR signaling; Proteases/Proteasome; Stem Cells; Tyrosine Kinase/Adaptors |
(±)-Boehmenan shows potent protein-tyrosine phosphatase 1B (PTP1B) inhibitory activity in vitro with the IC(50) values of 43.5 uM, it inhibits PTP1B activity in a competitive manner. Boehmenan exhibits the potent cytotoxic effects against many cancer cell | |||
T79985 |
Cryptosporioptide A
|
Phosphatase | Metabolism |
Cryptosporioptide A (Compound 3)是一种从昆虫寄生真菌Cordyceps gracilioides中分离出的色素蛋白酪氨酸磷酸酶抑制剂,针对PTP1B、SHP2、CDC25B、LAR和SHP1等酶展示了抑制作用,其IC50值分别为7.3、5.7、7.6、>50、4.9 μg/mL。 | |||
TN4279 |
Isoderrone
|
Tyrosinase | Proteases/Proteasome |
Isoderrone 在体外对α-葡萄糖苷酶(α-glucosidase)有抑制作用;它是一种蛋白酪氨酸磷酸酶1B(PTP1B)抑制剂,IC50值为22.7±1.7μM,表明它可能是一种治疗2型糖尿病的新药。 | |||
TN1440 |
Beta-Hydroxyisovalerylshikonin
|
EGFR; Tyrosine Kinases; Prostaglandin Receptor; Src; AMPK; Fatty Acid Synthase | Angiogenesis; Chromatin/Epigenetic; GPCR/G Protein; Immunology/Inflammation; JAK/STAT signaling; Metabolism; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
Beta-hydroxyisovalerylshikonin 是分离自Lithospermium radix 的天然产物,具有抑制PTK 的作用, 对 EGFR 和 v-Src 受体作用的IC50分别为 0.7 μM 和 1 μM。它对多种肿瘤细胞系均有抑制作用,可以高效诱导 NCI-H522 和 DMS114 细胞的死亡。 | |||
TN2928 |
Pygenic acid A
3-Epicorosolic acid,脓毒酸A |
||
3-Epicorosolic acid has a potent inhibitory effect on Epstein-Barr virus early antigen (EBV-EA) induction, it has potential anti-inflammatory activities as well as cancer chemopreventive activity.3-Epicorosolic acid shows both potent α-glucosidase and pro | |||
T80007 |
Stevisalioside A
|
Phosphatase | Metabolism |
Stevisalioside A (Compound 2),一种从甜叶菊根提取的化合物,展现出抗糖尿病的口服活性。该化合物有效抑制PTP1B,IC50为526.8 μM,并能降低Stevisalioside A引起的高血糖小鼠血糖水平,改善餐后血糖峰值及口服葡萄糖和胰岛素耐量测试结果。 | |||
T36950 |
Rubrofusarin triglucoside
|
||
Rubrofusarin triglucoside is a glycoside compound isolated from Cassia obtusifolia Linn seeds. Rubrofusarin triglucoside inhibits human monoamine oxidase A (hMAO-A) with an IC50 of 85.5 μM[1]. [1]. Pradeep Paudel, et al. Rubrofusarin as a Dual Protein Tyrosine Phosphate 1B and Human Monoamine Oxidase-A Inhibitor: An in Vitro and in Silico Study. ACS Omega. 2019 Jul 3;4(7):11621-11630. |