31
3
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。 | |||
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。 | |||
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。 | |||
T9576 |
AMP-945
|
FAK | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
AMP-945 是一种粘着斑激酶抑制剂。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
T23539 |
Y 11
|
Others | Others |
focal adhesion kinase (FAK) inhibitor | |||
T28277 |
OXA-11
OXA 11 |
||
OXA-11 is a potent inhibitor of focal adhesion kinase (FAK) with anti-tumor activity. | |||
T22397 |
PF-4618433
|
Others | Others |
PF-4618433 is a dual inhibitor of focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2). | |||
T70724 |
GSK-2256098 HCl
|
||
GSK-2256098 HCl is a focal adhesion kinase-1 (FAK) inhibitor with potential antiangiogenic and antineoplastic activities. | |||
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. | |||
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. | |||
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). | |||
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... | |||
T83680 |
Azurin (50-77) (P. aeruginosa) TFA
Azurin p28,p28 |
||
Azurin (50-77)是一种含铜细菌蛋白azurin的肽段,存在于P. aeruginosa中,具有细胞周期停滞、抑制癌细胞增殖和调节血管生成活性。作为VEGFR2的抑制剂(IC20约为10.7 µM),Azurin (50-77)(20 µM)能在MCF-7乳腺癌细胞中诱导G2/M期的细胞周期停滞。在50 µM的浓度下,减少MCF-7和ZR-75-1乳腺癌细胞的增殖。Azurin (50-77)以25 µM的浓度减少VEGF-A诱导的毛细管管腔形成(IC50 = 12 µM),降低人脐静脉内皮细胞(HUVECs)中与细胞膜相关的F-actin、焦点粘附激酶(FAK)和paxillin的水平,并增加胞外的血小板内皮细胞粘附分子-1(PECAM-1)的水平。在体内,Azurin (50-77)(每日10 mg/kg)在MCF-7小鼠异种移植模型中减少肿瘤体积。 |
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。 |