57
8
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
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。 | |||
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。 | |||
T9576 |
AMP-945
|
FAK | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
AMP-945 是一种粘着斑激酶抑制剂。 | |||
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。 | |||
T0680 |
Lamotrigine
LTG,BW430C,拉莫三嗪 |
5-HT Receptor; Sodium Channel; Autophagy | Autophagy; GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience |
Lamotrigine (BW430C) 是一种抗癫痫剂和情绪稳定剂,可研究癫痫、局灶性癫痫等。。它选择性地阻断电压门控钠离子通道,稳定突触前神经元膜,抑制谷氨酸释放。 | |||
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。 | |||
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。 | |||
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。 | |||
T8528 |
AC1903
|
TRP/TRPV Channel | Membrane transporter/Ion channel |
AC1903是一种选择性的TRPC5抑制剂,具有足细胞保护特性,对 TRPC4 或 TRPC6没有影响,并且在激酶谱分析中没有显示出脱靶效应。在局灶节段性肾小球硬化大鼠模型中,AC1903抑制严重蛋白尿,并且防止足细胞丢失。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
T27828 |
Licostinel
CGP 63446,ACEA1021,ACEA 1021,ACEA-1021,CGP-63446 |
GluR | Neuroscience |
Licostinel (CGP 63446) 是一种谷氨酸受体拮抗剂。 Licostinel 可防止永久性局灶性脑缺血。 | |||
T33824 |
Orotirelin
CG 3509,Orotireline |
Others | Others |
Orotirelin(CG 3509) 是促甲状腺激素释放激素类似物,可逆转了戊巴比妥诱导的睡眠时间。Orotirelin 可能对局灶性脑缺血的动物有益。 | |||
T67843 |
GSK215
|
FAK | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
GSK215是一种强效和选择性的粘着斑激酶(FAK)PROTAC 降解剂(pDC50=8.4)。GSK215包含 FAK 抑制剂 VS-4718和 VHL E3连接酶的粘合剂。GSK215可以诱导 FAK 的快速和长期降解。 | |||
TP2137L |
pp60 c-src (521-533) (phosphorylated) acetate
|
Others | Others |
pp60 c-src (521-533) (phosphorylated) acetate 是粘着斑形成和细胞扩散的调节剂。它还调节细胞运动,是由促运动透明质酸受体 RHAMM 触发的信号通路中的关键成分。 | |||
T40109 |
APOL1-IN-1
APOL1-IN-1 |
Others | Others |
APOL1-IN-1是一种有效的载脂蛋白 L1(APOL1) 的抑制剂,可用于研究局灶节段性肾小球硬化 (FSGS) 和非糖尿病肾病 (NDKD) 的发病原理,促进对此类疾病的研究。 | |||
T76681 |
Fresolimumab
GC1008 |
TGF-beta/Smad | Stem Cells |
Fresolimumab (GC1008) 是一种具有特异性的人抗转化生长因子 β单克隆抗体,可与人 TGFβ1、TGFβ2 和 TGFβ3 的活性形式结合,可用于研究成人局灶节段性肾小球硬化和癌症。 | |||
T15367 |
Gadoxetate Disodium
Gd-EOB-DTPA Disodium,钆塞酸二钠,ZK 139834 |
Others | Others |
Gadoxetate Disodium 是一种肝胆系统中磁共振成像 (MRI) 中的造影剂,能够在正常的功能性肝细胞中累积,可用于局灶性肝脏病变(如肝细胞癌或 T1 加权成像的肝转移)的研究。 | |||
T30087 |
Antroquinonol
|
Reactive Oxygen Species; Nrf2 | Immunology/Inflammation; Metabolism; NF-κB |
Antroquinonol 是一种来源于 Antrodia camphorata 的泛醌衍生物,具有抗炎和抗癌活性。Antroquinonol 通过增强 Nrf2 信号通路降低氧化应激,抑制局灶节段性肾小球硬化小鼠的炎症和硬化。Antroquinonol 具有治疗非小细胞肺癌的潜力,可用于结肠癌的研究。 | |||
T0153 |
Oltipraz
吡噻硫酮,NSC 347901,RP 35972 |
HIF/HIF Prolyl-Hydroxylase; HIV Protease; Reverse Transcriptase; Nrf2; HIF | Angiogenesis; Chromatin/Epigenetic; Immunology/Inflammation; Metabolism; Microbiology/Virology; Proteases/Proteasome |
Oltipraz (RP 35972) 是一种 Nrf2的强效激活剂。它时间依赖性地抑制 HIF-1α激活,IC50为 10 μM,浓度 ≥ 10 μM 时完全消除 HIF-1α诱导。 | |||
T27897 |
LY 215490
LY215490,LY-215490 |
||
LY 215490 is a selective, competitive and systemically active antagonist of AMPA receptor. LY 215490 has neuroprotective effect against focal ischaemia in a model of permanent MCA occlusion in the rat. | |||
T28277 |
OXA-11
OXA 11 |
||
OXA-11 is a potent inhibitor of focal adhesion kinase (FAK) with anti-tumor activity. | |||
T23539 |
Y 11
|
Others | Others |
focal adhesion kinase (FAK) inhibitor | |||
T16292 |
NFPS
|
Thrombin | Proteases/Proteasome |
NFPS exerts neuroprotection via glyR alpha1 subunit in the rat model of transient focal cerebral ischaemia and reperfusion. NFPS is a selective and non-competitive glycine transporter-1 (GlyT1) inhibitor (IC50s: 2.8 nM and 9.8 nM for hGlyT1 and rGlyT1, respectively). | |||
T70724 |
GSK-2256098 HCl
|
||
GSK-2256098 HCl is a focal adhesion kinase-1 (FAK) inhibitor with potential antiangiogenic and antineoplastic activities. | |||
T22397 |
PF-4618433
|
Others | Others |
PF-4618433 is a dual inhibitor of focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2). | |||
T71450 |
Ilacirnon sodium
|
||
Ilacirnon sodium is a potent CCR2 antagonist that may be useful in the treatment of renal diseases including Focal Segmental Glomerulosclerosis and Diabetic Nephropathy. | |||
T38068 | Aptiganel hydrochloride | ||
Potent and noncompetitive NMDA receptor antagonist (IC50 = 36 nM). Exhibits >70-fold selectivity for NMDA receptor over σ receptor. Neuroprotective in a rat model of focal ischemia. | |||
T11260 | FAK inhibitor 2 | FAK | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
FAK inhibitor 2, antitumor and anti-angiogenesis activitiesis ,is a potent focal adhesion kinase (FAK) inhibitor with an IC50 of 0.07 nM . | |||
T35075 | VSWRAPTA | ||
VSWRAPTA is a promoter of neuronal branching via transcellular activation of the focal adhesion kinase (FAK) and the ERK1/2 signaling pathway in vitro. | |||
T21586 |
Methsuximide
|
||
Methsuximide 是一种抗惊厥药,对于癫痫小发作、精神运动和局灶性运动发作有效。 | |||
T11806 |
L-NIO dihydrochloride
|
NOS | Immunology/Inflammation |
L-NIO dihydrochloride induces a consistentfocal ischemic infarctin rats. L-NIO dihydrochloride is a potent, non-selective and NADPH-dependent nitric oxide synthase (NOS) inhibitor, with Kis of 1.7, 3.9, 3.9 μM for neuronal (nNOS), endothelial (eNOS), and inducible (iNOS), respectively. | |||
T13840 |
PROTAC FAK degrader 1
|
Others | Others |
PROTAC FAK degrader 1 is a selective and potent degrader of focal adhesion kinase (Fak) (IC50 of 6.5 nM). | |||
T68740 |
NVP-TAC544
|
||
NVP-TAC544 is a novel focal adhesion kinase (FAK) inhibitor, potently blocking kinase activity of FAK along with Aurora A, activated Cdc42-associated kinase 1 (ACK1), Met, insulin receptor (IR), TrkA, and IGF-1R. | |||
T60492 |
Lamotrigine hydrate
|
||
Lamotrigine hydrate 是口服有效的抗惊厥剂或抗癫痫剂 ,通过选择性地阻断电压门控Na+通道,稳定突触前神经元膜并抑制谷氨酸释放。Lamotrigine hydrate 可用于研究癫痫、局灶性癫痫等神经性疾病。 | |||
T60667 |
NAT
|
||
NAT 是 NAMPT 激活剂的苗头化合物。NAMPT 是研究与 NAD 耗竭相关的许多疾病 ,例如如神经退行性疾病的有吸引力的靶点,由于其为 NAD 回收途径中的限速酶。 | |||
T41164 |
FC 11
|
||
FC 11 is a highly potent focal adhesion Ki nase (FAK) PROTAC®Degrader (DC50 values are 40 to 370 pM depending on cell line), which is composed of the FAK inhibitor PF 562217 joined by a linker to the cereblon-binding ligand Pomalidomide. The effects of FC 11 are reversible upon compound wash out. FC 11 also degrades autophosphorylated FAK (pFAKtyr397), displaying near complete degradation after 3 hours at 100 nM in TM3 cells. | |||
T70352 |
PH11
|
||
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... | |||
T8406L |
Gadobutrol Monohydrate
Gd-DO3A-butrol |
||
Gadobutrol is a medicinal product used in diagnostic magnetic resonance imaging (MRI) in adults and children. It provides contrast enhancement during cranial, spinal, breast, or other investigations. In the central nervous system, Gadobutrol works by high |
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。 | |||
TN1068 |
Tricin
|
Others; CDK | Cell Cycle/Checkpoint; Others |
Tricin 是米糠中大量存在的一种天然类黄酮。它通过抑制 CDK9 来抑制HCMV 的复制。它通过上调 FAK 靶向 microRNA-7 的表达来抑制 C6 胶质瘤细胞的增殖和侵袭。 | |||
T3900 |
Emodin-8-glucoside
大黄素-8-β-D-吡喃葡萄糖苷,Emodin glucoside B,Anthraglycoside B |
Others | Others |
Emodin-8-glucoside (Anthraglycoside B) 是从芦荟中分离出的蒽醌衍生物,与 DNA 的小沟结合。它具有保护缺血和再灌注引起的局灶性脑损伤的作用。它直接刺激成骨细胞的细胞增殖和分化。 | |||
T2S1008 |
Oxysophoridine
Sophoridine N-oxide,氧化槐定碱 |
Apoptosis; Antioxidant | Apoptosis; oxidation-reduction |
Oxysophoridine (Sophoridine N-oxide) 是从苦豆子中提取的一种生物碱,具有抗发炎,抗氧化应激和抗凋亡的作用。 | |||
T3414 |
Morroniside
莫诺苷,奎宁树 |
Apoptosis; MMP; Pyroptosis | Apoptosis; Immunology/Inflammation; Proteases/Proteasome |
Morroniside 通过抑制神经元凋亡和 MMP9/2 的表达从而发挥神经保护作用,可作为 db/db 小鼠肝脏炎症反应和脂质代谢的调节剂。它通过抑制高血糖和氧化应激表现出对糖尿病肾损伤和人脐静脉内皮细胞的保护作用。 | |||
TN4115 |
Gardenine
|
Others | Others |
Gardenin has regulatory effect on the gene expression in rats with focal cerebral ischemia. |