Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T3593 |
Src Inhibitor 1
Src Kinase Inhibitor 1,Src-l1 |
Src | Angiogenesis; Tyrosine Kinase/Adaptors |
Src Inhibitor 1 (Src Kinase Inhibitor 1) 是一种选择性的、高效的、ATP-竞争性的双位点 Src 酪氨酸激酶抑制剂,能够抑制 Src (IC50:44 nM) 和 Lck (IC50:88 nM)。 | |||
T1826 |
PI3K-IN-1
Voxtalisib Analogue,Voxtalisib (SAR245409, XL765) Analogue,XL765,SAR245409 |
DNA-PK; PI3K | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
PI3K-IN-1 (Voxtalisib Analogue) 是 PI3K 抑制剂,PI3K-IN-1(25 μM) 能够阻断 PI3K/Akt 信号通路。 | |||
T6028 |
PF 477736
PF 00477736,PF-477736,PF-736,PF-00477736,PF477736 |
c-Fms; VEGFR; FGFR; FLT; c-RET; Chk; CDK; Src; Aurora Kinase | Angiogenesis; Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Tyrosine Kinase/Adaptors |
PF 477736 (PF-736,PF-00477736) 是一种特异性、有效且具有 ATP 竞争性的 Chk1 抑制剂,Ki 值为0.49 nM。它也是Chk2抑制剂,Ki 值为 47 nM。它还抑制VEGFR2、Fms、Yes、Aurora-A、FGFR3、Flt3和Ret。 | |||
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。 | |||
T5524 |
Aurora kinase inhibitor-3
Aurora Kinase Inhibitor III |
Aurora Kinase | Cell Cycle/Checkpoint; Chromatin/Epigenetic |
Aurora kinase inhibitor-3 (Aurora Kinase Inhibitor III) 是一种有效的,选择性 Aurora A 激酶抑制剂,IC50为 42 nM。 | |||
T0152 |
Bosutinib
伯舒替尼,SKI-606 |
Bcr-Abl; Src; Autophagy | Angiogenesis; Autophagy; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Bosutinib (SKI-606) 是一种合成的喹诺酮衍生物和双激酶抑制剂,靶向 Abl 和 Src 激酶的 IC50分别为 1 nM 和 1.2 nM。 | |||
T38511 |
AWL-II-38.3
|
Ephrin Receptor | Tyrosine Kinase/Adaptors |
AWL-II-38.3 is a highly effective inhibitor of EphA3, a receptor for ephrin-A. It demonstrates potent kinase inhibitory activity against EphA3 and does not show significant cellular activity against Src-family kinases or b-raf [1] [2]. | |||
T37600 | Dasatinib N-oxide | Others | Others |
Dasatinib N-oxide 是 Dasatinib 的一种次要代谢物。Dasatinib 是口服有效的 Src/Bcr-Abl 抑制剂。 | |||
T36432 |
A2ti-1
|
Virus Protease | Microbiology/Virology |
A2ti-1 是一种具有高选择性的附件蛋白 A2/S100A10 杂四聚体(A2t)抑制剂(IC50 : 24 μM), 抑制ARV介导的Src和p38丝裂原活化蛋白激酶(MAPK)的激活。A2ti-1 可用于研究人类乳头瘤病毒 16 型(HPV16)感染。 | |||
T4263 |
BAY 61-3606
2-[[7-(3,4-二甲氧基苯基)咪唑并[1,2-C]嘧啶-5-基]氨基]-3-吡啶甲酰胺,Syk inhibitor IV |
Apoptosis; Syk | Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors |
BAY 61-3606 (Syk inhibitor IV) 是一种具有口服活性的,ATP 竞争性的可逆选择性Syk 抑制剂。它作用于乳腺癌细胞,通过下调 Mcl-1 促进 TRAIL 诱导的细胞凋亡。它降低神经母细胞瘤细胞中的 ERK1/2 和 Akt 磷酸化,也降低 K-rn 细胞裂解物中 Syk 磷酸化。 | |||
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。 | |||
T13156 |
TG 100572
|
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
TG 100572 is a inhibitor of multi-targeted kinase which inhibits receptor tyrosine kinases and Src kinases(IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively). | |||
T14370 |
AZD0424
|
Others | Others |
AZD0424, an orally active compound characterized as a dual selective Src/Abl kinase inhibitor, exhibits potential antineoplastic activity[1] and promotes apoptosis and cell cycle arrest in lymphoma cells[2]. | |||
T81577 |
P60v-src(137-157)
|
||
P60v-src(137-157)为合成抑肽,针对p60v-src酪氨酸激酶展现抑制作用(IC50: 7.5 μM)。 | |||
T63825 | Antiallergic agent-1 | ||
Antiallergic agent-1 是 Src 家族激酶抑制剂,是一种新的有价值的先导化合物,具有作为抗过敏剂的潜力。 | |||
T14074 |
A-770041
|
Src | Angiogenesis; Tyrosine Kinase/Adaptors |
A-770041 是选择性和口服活性的 Src 家族 Lck 抑制剂,是参与 T 细胞信号传导的另一种 Src 家族激酶。它是 Lck (1 mM ATP) 抑制剂,IC50为147 nM,对 Fyn 的选择性是 300 倍, | |||
T37597 |
Squarunkin A hydrochloride
|
||
Squarunkin A hydrochloride 是一种有效的选择性UNC119-货物相互作用抑制剂。Squarunkin A hydrochloride 选择性地抑制Src 激酶 N 末端的肉豆蔻酰化肽与 UNC119A 的结合,IC50 值为 10 nm。Squarunkin A hydrochloride 会干扰细胞中Src 激酶的活化。 | |||
T13156L |
TG 100572 Hydrochloride
|
VEGFR; FGFR; PDGFR; Src | Angiogenesis; Tyrosine Kinase/Adaptors |
TG 100572 Hydrochloride 是一种多靶点激酶抑制剂,能够抑制受体酪氨酸激酶和Src 激酶。 | |||
T13157L | TG 100801 Hydrochloride | VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
TG 100801 Hydrochloride is a prodrug to treat age-related macular degeneration. TG 100572 is a inhibitor of multi-targeted kinase(IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, | |||
T22067 |
CHMFL-ABL-053
|
||
CHMFL-ABL-053 (Compound 18a) 是一种有效的、选择性的、具有口服活性的 BCR-ABL、SRC 和 p38激酶抑制剂,IC50值分别为 70、90 和 62 nM。CHMFL-ABL-053 是一种潜在有效的慢性粒细胞白血病 (CML) 候选药物 [1]。 | |||
T36779 |
NG 25 (hydrochloride hydrate)
|
||
NG 25 is a type II kinase inhibitor that inhibits MAP4K2 and TAK1 (IC50s = 21.7 and 149 nM, respectively).1It also inhibits the Src family kinases Src and LYN (IC50s = 113 and 12.9 nM, respectively) and Abl family kinases (IC50s = 75.2 nM), as well as CSK, FER, and p38α (IC50s = 56.4, 82.3, and 102 nM, respectively). NG 25 (100 nM) prevents TNF-α-induced IKKα/β phosphorylation and IκB-α degradation in L929 cells. It inhibits secretion of IFN-α and IFN-β induced by CpG type B and CL097, respectiv... | |||
T35536 |
Tpl2 Kinase Inhibitor (hydrochloride)
|
||
Tpl2 kinase inhibitor is an inhibitor of tumor progression locus 2 (Tpl2; IC50= 0.05 μM).1It is selective for Tpl2 over MEK, p38 MAPK, Src, MK2, and PKC (IC50s = >40, 180, >400, 110, and >400 μM, respectively). Tpl2 kinase inhibitor inhibits LPS-induced TNF-α production in isolated human monocytes and whole blood (IC50s = 0.7 and 8.5 μM, respectively). It enhances differentiation induced by calcitriol in HL-60 and U937 leukemia cells when used at a concentration of 5 μM.2Tpl2 kinase inhibitor (5... | |||
T36650 |
Ansatrienin B
|
||
Ansatrienin B is an ansamycin antibiotic and antifungal agent first isolated from S. collinus and S. rishiriensis., In fetal rat long bones, it is an inhibitor of parathyroid hormone-induced calcium release (IC50 = 21 nM), which is a measure of bone resorption, and pp60c-src kinase (IC50 = 50 nM). It is an inhibitor of translation at the protein synthesis stage by specific inhibition of L-leucine incorporation (IC50 = 58 nM in A549 cells). It also inhibits TNF-α-induced expression of intercellul... | |||
T80653 |
Larixol
(+)-Larixol |
Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
Larixol作为一种fMLP抑制剂,在免疫调节作用上,能够抑制Src激酶、ERK1/2、p38以及AKT的磷酸化信号。它能够通过干扰fMLP受体Gi蛋白的βγ亚基与下游分子之间的作用,抑制fMLP引发的呼吸爆发。此外,Larixol可有效降低由fMLP (0.1 μM) 诱导的超氧阴离子生成(IC50: 1.98 μM)、组织蛋白酶G的释放(IC50: 2.76 μM)及趋化反应,有助于缓解中性粒细胞的过度激活,减少炎症或组织损伤。Larixol衍生物对FSGS相关TRPC6功能突变有显著的抑制效果。 |