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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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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; PROTACs | Angiogenesis; Cytoskeletal Signaling; PROTAC; 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 |
Others | Others |
OXA-11 is a potent inhibitor of focal adhesion kinase (FAK) with anti-tumor activity. | |||
T70724 |
GSK-2256098 HCl
|
Others | Others |
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). | |||
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
|
Others | Others |
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
|
Others | Others |
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; PROTACs | Others; PROTAC |
PROTAC FAK degrader 1 is a selective and potent degrader of focal adhesion kinase (Fak) (IC50 of 6.5 nM). | |||
T70352 |
PH11
|
Others | Others |
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。 |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPJ-00678 |
STX6 Protein, Human, Recombinant
STX6,Syntaxin-6 |
Human | E. coli |
Syntaxin-6 (STX6) is a single-pass type IV membrane protein, which belongs to the Syntaxin family. STX6 is mainly localized in the plasma membrane. STX6 contains one t-SNARE coiled-coil homology domain and involved in intracellular vesicle trafficking. When STX6 function is inhibited, internalization through caveolae is dramaticaliy reduced, whereas other endocytic mechanisms are unaffected. It is reported that STX6 is necessary for proper expression of focal adhesion kinase and integrin alpha5 ... | |||
TMPH-01539 |
ILK Protein, Human, Recombinant (His)
ILK-1,ILK,Integrin-linked protein kinase,59 kDa ser... |
Human | Baculovirus Insect Cells |
Receptor-proximal protein kinase regulating integrin-mediated signal transduction. May act as a mediator of inside-out integrin signaling. Focal adhesion protein part of the complex ILK-PINCH. This complex is considered to be one of the convergence points of integrin- and growth factor-signaling pathway. Could be implicated in mediating cell architecture, adhesion to integrin substrates and anchorage-dependent growth in epithelial cells. Regulates cell motility by forming a complex with PARVB. P... | |||
TMPY-03060 |
Parvin alpha/PARVA Protein, Human, Recombinant (GST)
parvin, alpha,parvin, α,MXRA2,CH-ILKBP,Parvin α/PARVA |
Human | E. coli |
Actopaxin, also known as alpha-parvin, belongs to the parvin family. It is widely expressed, with highest levels in heart, skeletal muscle, kidney and liver. Actopaxin contains 2 CH (calponin-homology) domains and probably plays a role in the regulation of cell adhesion and cytoskeleton organization. It interacts with integrin-linked protein kinase and probably with actin and the LD1 and LD4 motifs of PXN. Actopaxin binds directly to both F-actin and paxillin LD1 and LD4 motifs. Actopaxin also e... | |||
TMPY-02198 |
ILKAP Protein, Human, Recombinant (His)
ILKAP3,PP2C-δ,PP2C-DELTA,integrin-linked kinase-ass... |
Human | HEK293 Cells |
Integrin-linked kinase-associated serine/threonine phosphatase 2C, also known as ILKAP, is a cytoplasm protein that belongs to the PP2C family. ILKAP contains one PP2C-like domain. ILKAP is widely expressed. Highest levels expressed in striated muscle. Much lower levels are evident in various smooth muscle tissues. ILKAP may play a role in the regulation of cell cycle progression via dephosphorylation of its substrates whose appropriate phosphorylation states might be crucial for cell proliferat... |