48
4
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T1817 |
GNF-2
GNF2 |
SARS-CoV; Bcr-Abl | Angiogenesis; Cytoskeletal Signaling; Microbiology/Virology; Tyrosine Kinase/Adaptors |
GNF-2 是一种高选择性的非 ATP 竞争性 Bcr-Abl 抑制剂。 它抑制 Ba/F3.p210 增殖,IC50为 138 nM。 | |||
T6223 |
U0126-EtOH
U0126 Ethanol,U0126 |
Mitophagy; Influenza Virus; MEK; Autophagy | Autophagy; MAPK; Microbiology/Virology |
U0126-EtOH (U0126 Ethanol) 是一种非 ATP 竞争性的选择性MEK1和MEK2抑制剂,IC50分别为 72 nM 和 58 nM。U0126-EtOH 可抑制自噬和线粒体自噬。 | |||
T10898 |
Samuraciclib hydrochloride
ICEC0942 hydrochloride,CT7001 hydrochloride |
Apoptosis; CDK | Apoptosis; Cell Cycle/Checkpoint |
Samuraciclib hydrochloride (ICEC0942 hydrochloride) 是一种具有选择性,ATP 竞争性和口服活性的CDK7抑制剂,IC50为 41 nM。它以 GI50值为 0.2-0.3 µM 来抑制乳腺癌细胞系的生长,具有抗肿瘤作用。 | |||
T14988 |
CMPD1
|
MAPK | MAPK |
CMPD1 是非 ATP 竞争性 p38 MAPK 介导的 MK2磷酸化选择性抑制剂(Ki:330 nM)。 | |||
T6152 |
PD318088
|
MEK | MAPK |
PD318088 是非 ATP 竞争性的MEK1/2变构抑制剂,是 PD184352 的结构类似物。它在MEK1 活性位点与 ATP 结合位点相邻的区域与 ATP 同时结合,可用于癌症研究。 | |||
T8685 |
SP-146
|
Aurora Kinase | Cell Cycle/Checkpoint; Chromatin/Epigenetic |
SP-146 是一种选择性、有效且非 ATP 竞争性的 Aurora B 抑制剂(IC50:0.316 nM)。 | |||
T6636 |
Refametinib
BAY 86-97661,瑞法替尼//瑞美替尼,BAY 869766,RDEA119 |
MEK | MAPK |
Refametinib (RDEA119) 是可口服的、非 ATP 竞争和选择性的 MEK1/MEK2变构抑制剂,IC50分别为 19 和 47 nM。 | |||
T6546 |
IPA-3
IPA3,IPA 3 |
PAK | Cytoskeletal Signaling |
IPA-3 是一种选择性的非 ATP 竞争性 Pak1 抑制剂,IC50 为 2.5 μM。 | |||
T73331 |
GSK3-IN-3
|
Mitophagy; GSK-3 | Autophagy; PI3K/Akt/mTOR signaling; Stem Cells |
GSK3-IN-3 是一种线粒体自噬 (mitophagy) 诱导剂和GSK-3 抑制剂(IC50 : 3.01 μM),可诱导帕金依赖性线粒体自噬。 GSK3-IN-3 具有非 ATP 和非底物竞争性,对 6-OHDA 有神经保护作用。 | |||
T16560 |
Poloxin
|
PLK | Cell Cycle/Checkpoint |
Poloxin 是一种 polo 样激酶 1 的 ATP 非竞争性抑制剂,靶向 polo-box 结构域,IC50值约为 4.8 μM。 | |||
T6083 |
AZD8330
ARRY-424704,ARRY-704 |
ERK; MEK | MAPK |
AZD8330 (ARRY-704) 是非竞争性的 MEK1/MEK2抑制剂,IC50为 7 nM。 | |||
T3067 |
Tideglusib
NP-12,NP031112 |
GSK-3 | PI3K/Akt/mTOR signaling; Stem Cells |
Tideglusib (NP031112) 是不可逆的 GSK-3抑制剂,能够抑制 GSK-3βWT (IC50:5 nM) 和 GSK-3βC199A (IC50:60 nM)。 | |||
T2443 |
CI-1040
PD 184352 |
Apoptosis; MEK | Apoptosis; MAPK |
CI-1040 (PD 184352) 是一种有口服活性的高度特异性MEK 小分子抑制剂,对 MEK1 的IC50值为 17 nM 。 | |||
T2125 |
Trametinib
GSK1120212,曲美替尼,JTP-74057 |
Apoptosis; MEK; Autophagy | Apoptosis; Autophagy; MAPK |
Trametinib (GSK1120212) 是一种 MEK 抑制剂,抑制 MEK1 和 MEK2 (IC50=0.7/0.9 nM),具有 ATP 非竞争性和口服活性。Trametinib 可以激活自噬,诱导凋亡。 | |||
T1803 |
GNF-5
GNF 5 |
SARS-CoV; Bcr-Abl | Angiogenesis; Cytoskeletal Signaling; Microbiology/Virology; Tyrosine Kinase/Adaptors |
GNF-5是 Bcr-Abl 的特异性非 ATP 竞争性抑制剂,IC50为0.22uM。它是 GNF-2 的类似物,具有改进的药代动力学特性。 | |||
T4442 |
MK2-IN-1 hydrochloride
MK2 Inhibitor,MK 25 |
MAPK | MAPK |
MK2-IN-1 hydrochloride (MK 25) 是一种高效的选择性 MAPKAPK2(MK2)激酶抑制剂,其 IC50值为0.11uM。 | |||
T6189 |
Mirdametinib
PD325901,PD0325901 |
Apoptosis; MEK; Autophagy | Apoptosis; Autophagy; MAPK |
Mirdametinib (PD325901) 是一种 MEK 抑制剂 (IC50=0.33 nM),具有选择性、非 ATP 竞争性和口服活性。Mirdametinib 具有抗肿瘤活性,可以抑制 p-ERK1/2 的表达并诱导细胞凋亡。 | |||
T2623 |
PD98059
PD 98059 |
ERK; Aryl Hydrocarbon Receptor; MEK; Autophagy | Autophagy; Immunology/Inflammation; MAPK |
PD98059 是一种 MEK 抑制剂,抑制 MEK1 和 MEK2 (IC50=2/50 μM),具有非 ATP 竞争性。PD98059 也是一种 AHR 的配体而起拮抗作用。PD98059 可以抑制细胞自噬。 | |||
T4398 |
LX2343
|
Beta Amyloid; Beta-Secretase; BACE; PI3K; Autophagy | Autophagy; Neuroscience; PI3K/Akt/mTOR signaling |
LX2343 是一种非 ATP 竞争性 PI3K 抑制剂,IC50 为 15.99±3.23 μM。它是一种 BACE1 酶抑制剂,IC50 值为 11.43±0.36 μM。它在促进 Aβ 清除中刺激自噬。 | |||
T73269 |
CK2α-IN-1
|
Casein Kinase | Metabolism; Stem Cells |
CK2α-IN-1 是一种选择性非 ATP 竞争的 CK2α 抑制剂 ,IC50 为 7.0 µM, Ki 为 1.6 µM。CK2α-IN-1 具有潜在的抗癌活性,可用于研究癌症。 | |||
T5818 |
Rigosertib sodium
Rigosertib,Estybon,ON-01910 |
Apoptosis; PLK; PI3K | Apoptosis; Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling |
Rigosertib sodium (ON-01910) 是一种选择性的非 ATP 竞争性PLK1抑制剂,IC50值为 9 nM。它是一种多激酶抑制剂和选择性抗癌剂,通过抑制PI3K/Akt 途径诱导细胞凋亡,促进组蛋白 H2AX 的磷酸化并诱导细胞周期中的 G2/M 期停滞。 | |||
T6673 |
SKI II
SphK-I2 |
Apoptosis; Wnt/beta-catenin; S1P Receptor | Apoptosis; Cytoskeletal Signaling; GPCR/G Protein; Stem Cells |
SKI II (SphK-I2) 是一种口服有效的合成鞘氨醇激酶 (SK)抑制剂,抑制 SK1 和 SK2,IC50值分别为 78 μM 和 45 μM。它通过诱导溶酶体/蛋白酶体降解,不可逆地抑制SK1。 | |||
T16750 |
Rigosertib
ON-01910,瑞格色替 |
Apoptosis; FLT; PLK; PI3K; Bcr-Abl; CDK; PDGFR; Src | Angiogenesis; Apoptosis; Cell Cycle/Checkpoint; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
Rigosertib (ON-01910) 是一种多激酶抑制剂和选择性抗癌剂,通过抑制 PI3K/Akt 途径诱导细胞凋亡,促进组蛋白 H2AX 的磷酸化并诱导细胞周期中的 G2/M 期停滞。它是一种选择性的非 ATP 竞争性PLK1抑制剂,IC50值为 9 nM。 | |||
T71399 |
Plogosertib
CYC140 |
||
Plogosertib (CYC140) 是一种选择性的、有效的、具有口服活性的 ATP 竞争性的 PLK1抑制剂 (IC50: 3 nM)。Plogosertib 是一种有抗增殖活性的抗癌剂,可用于多种肿瘤的研究,包括食管癌、胃癌、白血病、非小细胞肺癌、卵巢癌和鳞状细胞癌。 | |||
T14069 |
A-3 hydrochloride
|
CaMK; Casein Kinase; PKA; PKC | Chromatin/Epigenetic; Cytoskeletal Signaling; Metabolism; Neuroscience; Stem Cells; Tyrosine Kinase/Adaptors |
A-3 hydrochloride 是一种细胞可渗透的、可逆的、ATP 竞争性非选择性拮抗剂。它抑制 PKA 、酪蛋白激酶 II 和肌球蛋白轻链激酶,Ki 值分别为4.3 µM、5.1 µM 和7.4 µM。它还抑制 PKC 和酪蛋白激酶 I 的活性,Ki 分别为 47 µM 和 80 µM。 | |||
T6070 |
(E/Z)-Rigosertib sodium
N-[2-甲氧基-5-[[[2-(2,4,6-三甲氧基苯基)乙烯基]磺酰]甲基]苯基]甘氨酸钠盐,(E/Z) ON-01910 sodium |
PLK | Cell Cycle/Checkpoint |
ON-01910 是一种非 ATP 竞争性 PLK1 抑制剂(IC50 为 9 nM,在无细胞试验中)。它对 Plk2 的选择性高出 30 倍,对 Plk3 没有活性。 Rigosertib 抑制 PI3K/Akt 通路并激活氧化应激信号。 Rigosertib 可诱导多种癌细胞凋亡。它是一种合成的苄基苯乙烯基砜类似物,具有潜在的抗肿瘤活性。 | |||
T4391 |
Syk Inhibitor II dihydrochloride
Syk Inhibitor II (hydrochloride) |
Others; Tyrosine Kinases; Syk; PKC; BTK | Angiogenesis; Chromatin/Epigenetic; Cytoskeletal Signaling; Others; Tyrosine Kinase/Adaptors |
Syk Inhibitor II (hydrochloride) 是一种非受体酪氨酸激酶,磷酸化后,它与 FcRγ 链的基于免疫受体酪氨酸的激活基序结合,并介导与血小板功能和炎症相关的下游信号传导。 Syk inhibitor II 是一种可渗透细胞的嘧啶-甲酰胺化合物,以 ATP 竞争性方式选择性和可逆地阻断 Syk (IC50 = 41 nM)。它对 PKCε、PKCβII、ZAP-70、Btk 和 Itk 的效力要低得多(IC50s 分别为5.1、11、11.2、15.5 和 22.6 μM)。 | |||
T16559 |
Poloxime
|
PLK | Cell Cycle/Checkpoint |
Poloxime is a hydrolysis product of poloxin and is a non-ATP-competitive Plk1 inhibitor. It also has moderate Plk1 inhibitory activity. | |||
T69045 |
ON012380
|
||
ON012380 is a non-ATP-competitive Bcr-Abl inhibitor, potently inhibiting imatinib-resistant Bcr-Abl mutants such as T315I. | |||
T36778 |
MK2-IN-1
MK2-IN-1 (MK2 Inhibitor) |
||
MK2-IN-1 is a potent and selecitve MAPKAPK2(MK2) inhibitor(IC50=0.11 uM) with a non-ATP competitive binding mode. | |||
T63330 |
Clamikalant sodium
|
||
Clamikalant sodium 是非选择性的、 ATP 敏感性的钾 (KATP) 通道阻滞剂,能够用于研究心律不齐。 | |||
T8537 |
Tripolin A
(3E)-3-[(2,5-二羟基苯基)亚甲基]-1,3-二氢-2H-吲哚-2-酮 |
Aurora Kinase | Cell Cycle/Checkpoint; Chromatin/Epigenetic |
Tripolin A 是一种特异性的非 ATP 竞争性 Aurora A 激酶抑制剂,对Aurora A 和Aurora B 的IC50分别为1.5 μM 和7 μM。 | |||
T63929 |
Selumetinib sulfate
|
||
Selumetinib (AZD6244) 是高效的、选择性的、非 ATP 竞争性的 MEK1/2 抑制剂,可抑制 MEK1/2 磷酸化水平,对 MEK1 的 IC50 值为 14 nM。 | |||
T39430 |
XMU-MP-3
|
||
XMU-MP-3 is a robust, non-covalent inhibitor of BTK, exhibiting exceptional potency with IC50 values of 10.7 nM and 17.0 nM for BTK WT and BTK C481S mutation, respectively, in the presence of 10 μM ATP. Moreover, XMU-MP-3 elicits apoptosis. | |||
T70152 | Miransertib mesylate | ||
Miransertib mesylate is a selective AKT inhibitor that binds to and inhibits the activity of AKT in a non-ATP competitive manner, which may result in the inhibition of the PI3K/AKT signaling pathway. This may result in reduction in tumor cell proliferation and the induction of tumor cell apoptosis. | |||
T37313 | ITH15004 | ||
ITH15004 is a non-nucleotide antagonist of the purinergic P2X7receptor (IC50= 9 μM in HEK293 cells expressing the human receptor).1It inhibits ATP-induced currents inX. laevisoocytes expressing the human P2X7receptor when used at a concentration of 100 μM. ITH15004 (1 μM) decreases IL-1β release from LPS-primed, ATP-stimulated isolated mouse peritoneal macrophages. It has high permeability in a parallel artificial membrane permeability assay (PAMPA). 1.Calzaferri, F., Narros-Fernández, P., de Pa... | |||
T11170 | eIF4A3-IN-1 | Others | Others |
eIF4A3-IN-1 is a selective eukaryotic initiation factor 4A3 (eIF4A3) inhibitor (IC50=0.26 μM; Kd=0.043 μM), which binds to a non-ATP binding site of eIF4A3 and shows significant cellular nonsense-mediated RNA decay (NMD) inhibition at 10 and 3 μM and can be as a probe for further study of eIF4A3, the exon junction complex (EJC), and NMD. | |||
T68267 | RO5068760 | ||
RO5068760 , a substituted hydantoin, is a potent, highly selective, non-adenosine triphosphate (ATP)-competitive MEK1/2 inhibitors. RO5068760 shows significant efficacy in a broad spectrum of tumors with aberrant mitogen-activated protein kinase pathway activation. In vitro, RO5068760 demonstrates MEK1 kinase inhibitory activity with an IC50 of 0.025 μM in a cRaf/MEK/ERK cascade assay RO5068760 showed superior efficacy in tumors harboring B-RafV600E mutation. | |||
T79688 |
FAK-IN-11
|
FAK | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
FAK-IN-11 (Compound 4l) 作为FAK抑制剂,与FAK的ATP结合袋相结合,进而抑制其蛋白磷酸化。该化合物对MDA-MB-231细胞具有细胞毒性,IC50值为 13.73μM,并能诱导该细胞通过非凋亡途径死亡。 | |||
T40100 |
D-Luciferin 6′-methyl ether
6′-Methoxyluciferin,D-Luciferin 6′-methyl ether |
||
D-Luciferin 6′-methyl ether (also known as 6′-Methoxyluciferin or compound 19a) is a highly effective inhibitor of luciferase obtained from the North American firefly Photinus pyralis (referred to as PpyLuc). It exhibits an IC50 value of 0.1 μM. This compound, which is an analog of D-luciferin, interacts non-specifically with the ATP and luciferin binding sites within the active site of PpyLuc. | |||
T62118 |
KIF18A-IN-4
|
||
KIF18A-IN-4 是一种中度有效的 ATP 和微管 (microtubule) 非竞争性 KIF18A 抑制剂,其 IC50 值为 6.16 μM。KIF18A-IN-4 能够选择性的作用于大量有丝分裂驱动蛋白和激酶,对微管蛋白组装无直接影响。KIF18A-IN-4 显示出抗肿瘤作用。 | |||
T12068 |
MK-8033 hydrochloride
|
Others | Others |
MK-8033 hydrochloride 是一种有效的、具有口服活性的 ATP 竞争性 c-Met/Ron 双重抑制剂 ,对c-Met 的为1 nM ,对Ron 的IC50为7nM。MK-8033 hydrochloride 对活化的激酶构象 (activated kinase conformation)具有很高的亲和力,可用于乳腺癌,膀胱癌、非小细胞肺癌 (NSCLC)等癌症的研究。 | |||
T83529 |
(Rac)-Luciferin 6′-methyl ether sodium
(Rac)-6′-Methoxyluciferin sodium |
||
D-Luciferin 6'-methyl ether (6'-Methoxyluciferin; compound 19a) sodium 是北美萤火虫Photinus pyralis荧光素酶 (PpyLuc) 的有效抑制剂,具有0.1 μM的IC50值。作为D-荧光素的类似物,本化合物在PpyLuc的ATP及荧光素结合位点展示了非特异性的相互作用。 | |||
T61431 | Topoisomerase IIα-IN-4 | ||
Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive inhibitor of human DNA topoisomerase II, specifically inhibiting TopoIIα with an IC50 value of 3.8 μM and TopoIIβ with an IC50 value of 10.1 μM. It demonstrates significant efficacy in inducing apoptosis and arresting the cell cycle in HepG2 cells. Moreover, Topoisomerase IIα-IN-4 exhibits robust antitumor effects against various human cancer cell lines, making it a valuable compound for cancer research [1]. | |||
T71556 |
MK-1496
|
||
MK1496 is a n orally bioavailable Polo-like kinase 1 (Plk1) inhibitor with potential antineoplastic activity. Polo-like kinase 1 inhibitor MK1496 selectively inhibits Plk1, inducing selective G2/M arrest followed by apoptosis in a variety of tumor cells while causing reversible cell arrest at the G1 and G2 stage without apoptosis in normal cells. Plk1, named after the polo gene of Drosophila melanogaster, is a serine/threonine protein kinase involved in regulating mitotic spindle function in a n... | |||
T62911 |
Dalmelitinib
|
||
Dalmelitinib 是一种选择性的、口服具有活力的 c-Met 激酶抑制剂 (IC50: 2.9 nM),能够结合 c-Met 的 ATP-binding 区域。 Dalmelitinib 能够诱导 MET 的磷酸化,部分或完全抑制 AKT 和 ERK 的磷酸化。Dalmelitinib 对癌细胞 (c-Met 癌基因扩增) 的增殖表现出有效的抑制作用,可以用于研究癌症(如非小细胞肺癌)。 | |||
T68459 |
RO4927350
|
||
RO4927350 is a potent and highly selective non-ATP-competitive MEK1/2 inhibitor. RO4927350 selectively blocks the MAPK pathway signaling both in vitro and in vivo, which results in significant antitumor efficacy in a broad spectrum of tumor models. RO4927350 inhibits not only ERK1/2 but also MEK1/2 phosphorylation. In cancer cells, high basal levels of phospho-MEK1/2 rather than phospho-ERK1/2 seem to correlate with greater sensitivity to RO4927350. Furthermore, RO4927350 prevents a feedback inc... | |||
T35533 |
6-Hydroxypyridin-3-ylboronic Acid
|
||
6-Hydroxypyridin-3-ylboronic acid is a heterocyclic building block.1,2It has been used in the synthesis of non-nucleoside inhibitors of hepatitis C virus (HCV) RNA-dependent RNA polymerase nonstructural protein 5B (NS5B).16-Hydroxypyridin-3-ylboronic acid has also been used in the synthesis of mammalian target of rapamycin (mTOR) inhibitors.2 1.Hendricks, R.T., Spencer, S.R., Blake, J.F., et al.3-Hydroxyisoquinolines as inhibitors of HCV NS5b RNA-dependent RNA polymeraseBioorg. Med. Chem. Lett.1... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T3419 |
Chelerythrine chloride
白屈菜红碱,盐酸白屈菜红碱 |
Apoptosis; BCL; PKC; Autophagy | Apoptosis; Autophagy; Chromatin/Epigenetic; Cytoskeletal Signaling |
Chelerythrine chloride 是一种可渗透细胞的蛋白激酶 C 抑制剂,对磷酸盐受体具有竞争性,而对 ATP 是非竞争性的。它诱导细胞凋亡和自噬。 | |||
T6680 |
Staurosporine
Antibiotic AM-2282,星形孢菌素,AM-2282,CGP 41251,星孢菌素 |
Apoptosis; PKA; Antibacterial; Antibiotic; Src; PKC; Antifungal | Angiogenesis; Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; Microbiology/Virology; Tyrosine Kinase/Adaptors |
Staurosporine (AM-2282) 是一种蛋白激酶抑制剂,对 PKC、PKA、c-Fgr、Phosphorylase kinase 和 TAOK2 均有抑制活性 (IC50=6/15/2/3/3000 nM),具有 ATP 竞争性和非选择性。Staurosporine 也可以诱导凋亡。 | |||
T25192 |
Butyrolactone I
Olomoucin,丁酸内酯I |
CDK | Cell Cycle/Checkpoint |
Butyrolactone I (Olomoucin) 是 CDK 和 cdc2 激酶家族的 ATP 竞争性抑制剂。 Butyrolactone I 在非小细胞肺、小细胞肺和前列腺癌细胞系中显示出抗肿瘤作用。 | |||
T1723 |
Adenosine 5'-diphosphate
腺苷5'-二磷酸,Adenosine diphosphate,adenosine pyrophosphate,ADP |
Endogenous Metabolite | Metabolism |
Adenosine 5'-diphosphate (ADP) 是一种嘌呤核糖核苷5'-二磷酸,是 ATP 在 ATP 酶作用下去磷酸化的产物。Adenosine 5'-diphosphate (adenosine pyrophosphate) 可诱导人血小板聚集并通过作用于P2T-嘌呤受体抑制受刺激的腺苷酸环化酶。 |