Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T21761 |
HNMPA
|
IGF-1R | Tyrosine Kinase/Adaptors |
HNMPA 是膜不可渗透的胰岛素受体酪氨酸激酶 (insulin receptor tyrosine kinase) 抑制剂。HNMPA 可以抑制人胰岛素受体的酪氨酸和丝氨酸自磷酸化。HNMPA 对环 AMP 依赖性蛋白激酶或蛋白激酶 C 活性没有影响。 | |||
T36287 |
Pirtobrutinib
|
BTK | Angiogenesis; Tyrosine Kinase/Adaptors |
Pirtobrutinib (LOXO-305) is an advanced BTK inhibitor that displays high selectivity and operates through a non-covalent mechanism. This compound effectively inhibits various BTK C481 substitution mutations, leading to tumor regression in BTK-dependent lymphoma tumors in mouse xenograft models. Furthermore, Pirtobrutinib exhibits remarkable selectivity for BTK, with more than a 300-fold difference compared to 370 other kinases tested. Notably, at a concentration of 1 μM, Pirtobrutinib demonstrat... | |||
T9564 |
IRE1α kinase-IN-1
|
IRE1 | Cell Cycle/Checkpoint |
IRE1α kinase-IN-1 是IRE1α 的选择性抑制剂(IC50为 77 nM),对 IRE1α 的选择性高于 IRE1β 亚型 100 倍。它抑制内质网诱导的 IRE1α 寡聚和自磷酸化,并抑制 IRE1α RNase 活性 (IC50=80 nM)。 | |||
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。 | |||
T1770 |
GNE-9605
|
LRRK2 | Autophagy |
GNE-9605 是一个高效,选择性和能脑渗透的LRRK2抑制剂,IC50为19 nM。 | |||
T22396 |
PF-6274484
PF 6274484 |
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
PF-6274484 是一种EGFR 抑制剂,对于 EGFR-L858R/T790M 和 WT-EGFR 的 Ki 值分别为 0.14 和 0.18 nM。它在 H1975 肿瘤细胞和 A549 肿瘤细胞中抑制EGFR-L858R/T790M 自身磷酸化和EGFR-WT,IC50分别为6.6和 5.8 nM。 | |||
T7673 |
ATH686
ATH 686 |
Apoptosis; FLT | Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors |
ATH686 是一种选择性的,ATP 竞争性的FLT3抑制剂,具有抗白血病作用。它靶向突变 FLT3 蛋白激酶活性,并通过诱导凋亡和抑制细胞周期来抑制具有 FLT3 突变的细胞的增殖。 | |||
T38562 |
AKN-028
|
FLT | Angiogenesis; Tyrosine Kinase/Adaptors |
AKN-028 是酪氨酸激酶 FLT3的抑制剂,可剂量依赖性的诱导 FLT3的自磷酸化。 | |||
T4327 |
Prexasertib dihydrochloride
LY2606368 (dihydrochloride),Prexasertib HCl,LY2606368 |
Apoptosis; Chk; S6 Kinase | Apoptosis; Cell Cycle/Checkpoint; MAPK; PI3K/Akt/mTOR signaling |
Prexasertib dihydrochloride (LY2606368) 是一种选择性的,ATP 竞争性的细胞周期检测点激酶 1 抑制剂,Ki 为 0.9 nM,IC50为 <1 nM。它抑制 CHK2(IC50=8 nM) 和 RSK1 (IC50=9 nM)。它引起双链 DNA 断裂和复制突变,导致细胞凋亡,有抗肿瘤活性。 | |||
T4205 |
AG-494
Tyrphostin AG-494,AG 494,Tyrphostin B48 |
EGFR; CDK | Angiogenesis; Cell Cycle/Checkpoint; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
AG-494 (Tyrphostin B48) 是一种高效、选择性的 EGFR 酪氨酸激酶抑制剂,IC50为0.7 μM。它阻断 Cdk2 的激活并抑制 EGF 依赖的 DNA 合成。它抑制 EGFR、ErbB2、HER1-2 和 PDGF-R 的自磷酸化,IC50为 1.1、39、45 和 6 μM。 | |||
T4310 |
Prexasertib
5-[[5-[2-(3-氨基丙氧基)-6-甲氧基苯基]-1H-吡唑-3-基]氨基]-2-吡嗪甲腈,LY2606368 |
Apoptosis; Chk | Apoptosis; Cell Cycle/Checkpoint |
Prexasertib (LY2606368) 是一种具有潜在抗肿瘤活性的检查点激酶 1 抑制剂。它可引起双链 DNA 断裂和复制突变,导致细胞凋亡。 | |||
T1667 |
Tandutinib
MLN518,CT53518,NSC726292,坦度替尼 |
Apoptosis; FLT; CSF-1R; PDGFR; Src; c-Kit | Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors |
Tandutinib (CT53518) 是一种选择性 FLT3抑制剂,其 IC50为 0.22 μM。它还抑制c-Kit 和PDGFR,其IC50分别为 0.17 μM 和 0.20 μM。它可穿透血脑屏障,用于急性骨髓性白血病。 | |||
T14137 |
AG 1295
|
PDGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
AG 1295 是选择性血小板衍生生长因子受体酪氨酸激酶抑制剂。它能抑制 PDGFR 的自磷酸化,对 EGF 受体的自磷酸化无影响。 | |||
T3545 |
RG13022
RG 13022,Tyrphostin RG13022 |
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
RG13022 (Tyrphostin RG13022) 是一种酪氨酸激酶抑制剂,抑制EGF 受体自身磷酸化的IC50值为4 μM。 | |||
T6619 |
Desmethyl Erlotinib hydrochloride
OSI420,OSI-420,DesMethyl Erlotinib (CP-473420) HCl,去甲厄洛替尼,CP-473420,Desmethyl Erlotinib,OSI 420 |
EGFR; Drug Metabolite | Angiogenesis; JAK/STAT signaling; Metabolism; Tyrosine Kinase/Adaptors |
Desmethyl Erlotinib hydrochloride (OSI 420) 是 Erlotinib 的活性代谢物。Erlotinib 是 EGFR 酪氨酸激酶抑制剂。 | |||
T4053 |
AST 487
NVP-AST 487 |
VEGFR; FLT; c-RET; Bcr-Abl; c-Kit | Angiogenesis; Apoptosis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
AST 487 (NVP-AST 487) 是 RET 激酶抑制剂 (IC50:880 nM),能够抑制 RET 自磷酸化,及下游效应器激活,也抑制 Flt-3 (IC50:520 nM)。 | |||
T16550 |
PKR-IN-C16
|
Others | Others |
PKR-IN-C16 是一种特异性蛋白激酶抑制剂。它能够抑制 PKR 的自磷酸化,解除 PKR 在原代神经元细胞培养中诱导的翻译阻断。 | |||
T3599 |
BFH772
BFH-722 |
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
BFH772 是 VEGFR2抑制剂(IC50:3 nM),具有口服活性。 | |||
T30855 |
CGP77675
CGP-77675,1-(4-(4-amino-5-(3-methoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)phenethyl)piperidin-4-ol,ZINC1488120,CGP 77675 |
EGFR; VEGFR; Bcr-Abl; Src | Angiogenesis; Cytoskeletal Signaling; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
CGP77675 (ZINC1488120) 是一种有效的选择性 Src 家族激酶抑制剂,IC50 为 5-20 和 40 nM,用于肽底物的磷酸化和纯化的 Src 的自磷酸化。 CGP77675 具有抗癌活性。 | |||
T5168 |
EGFR-IN-12
EGFR Inhibitor |
Apoptosis; EGFR | Angiogenesis; Apoptosis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
EGFR-IN-12 (EGFR Inhibitor) 是一种 4,6-二取代的嘧啶,可诱导细胞凋亡,具有抗肿瘤活性。它是ATP 竞争性,不可逆且高度选择性的EGFR 抑制剂,IC50为 21 nM。它对EGFR 的选择性高于 HER4 和 55种其他激酶。它还抑制突变型EGFRL858R 和EGFRL861Q,IC50分别为 63 nM 和 4 nM。 | |||
T3691 |
(Rac)-SAR131675
SAR131675 |
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
(Rac)-SAR131675 是一种有效的、选择性的VEGFR3抑制剂,其IC50=23 nM。 | |||
T69863 | Dihydrogenistein | ||
Dihydrogenistein is a derivative of Genistein -- a compound that exhibits specific inhibitory activity against tyrosine kinases including autophosphorylation of epidermal growth factor receptor kinase. | |||
T22462 | 1,2,3,4,5,6-Hexabromocyclohexane | Others | Others |
The compound effectively and directly inhibits JAK2 tyrosine kinase autophosphorylation and specifically inhibits ligand-dependent JAK2 activation. It has no cytotoxicity at 100 μM. A 16-hour treatment with compound (1 μM) decreases JAK2 tyrosine autophos | |||
T39185 |
pp60 (v-SRC) Autophosphorylation Site, Phosphorylated
pp60 (v-SRC) Autophosphorylation Site, Phosphorylated |
||
pp60 (v-SRC) Autophosphorylation Site, Phosphorylated is a phosphorylated peptide derived from an EGFR substrate. It serves as a valuable tool for quantifying phosphorylated substrates in screening EGFR Kinase inhibitors. | |||
T69260 |
Genistein Diglucuronide
|
||
Genistein Diglucuronide is a metabolite of Genistein which exhibits specific inhibitory activity against tyrosine kinases including autophosphorylation of epidermal growth factor receptor kinase. | |||
T38841 |
IRE1α kinase-IN-2
IRE1α kinase-IN-2 |
||
IRE1α kinase-IN-2 is a highly potent inhibitor of IRE1α kinase, demonstrating an EC50 of 0.82 μM. It effectively impedes IRE1α kinase autophosphorylation with an IC50 of 3.12 μM. Additionally, IRE1α kinase-IN-2 effectively inhibits the splicing of XBP1 mRNA in wild-type cell lines. | |||
T12610L |
3-Hydroxy Midostaurin
CGP52421 |
FLT | Angiogenesis; Tyrosine Kinase/Adaptors |
3-Hydroxy Midostaurin (CGP 52421), a metabolite of PKC412, effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC50s of approximately 132 nM and 9.8 μM in culture medium and plasma, respectively. 3-Hydroxy Midostaurin is less selective but more cytotoxic than PKC412[1]. | |||
T78797 | FHND5071 | ||
FHND5071为选择性RET激酶抑制剂,通过抑制RET自磷酸化以发挥抗肿瘤效应,适用于肿瘤疾病研究。 | |||
T36718 |
Tie2 Inhibitor 7
|
||
Tie2 Inhibitor 7 blocks Tie2 kinase activity with a Ki value of 1.3 μM.. It has been shown to inhibit angiopoietin 1-induced Tie2 autophosphorylation and downstream signaling with an IC50 value of 0.3 μM. This compound can prevent endothelial cell tube formation and aberrant vessel growth in a rat model of Matrigel-induced choroidal neovascularization. | |||
T19119 |
3-Hydroxy Midostaurin-D5
CGP52421-D5 |
Others | Others |
3-Hydroxy Midostaurin-D5 (CGP52421-D5) is a deuterium-labeled 3-Hydroxy Midostaurin which is a metabolite of PKC412. PKC412 effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation (IC50s: 132 nM and 9.8 μM in culture medium and plasma). | |||
T73521 | Nec-3a | ||
Nec-3a,一种Necrostatin-3类似物,作为RIP1抑制剂(IC50: 0.44 μM),能够抑制RIP1激酶结构域的自磷酸化活性。 | |||
T40785 |
Gefitinib impurity 1
|
||
Gefitinib impurity 1 is a compound derived from Gefitinib, a potent and selective EGFR tyrosine kinase inhibitor (IC 50 = 33 nM). This orally active compound selectively inhibits tumor cell growth stimulated by EGF (IC 50 = 54 nM) and inhibits EGFR autophosphorylation induced by EGF in tumor cells. Additionally, Gefitinib induces autophagy and exhibits antitumor activity. | |||
T70444 |
Edicotinib HCl
|
||
Edicotinib, also known as JNJ-40346527, is a small molecule and orally available inhibitor of colony-stimulating factor-1 receptor (CSF1R; FMS) with potential antineoplastic activity. FMS tyrosine kinase inhibitor JNJ-40346527 blocks the receptor-ligand interaction between FMS and its ligand CSF1, thereby preventing autophosphorylation of FMS. As a result, unphosphorylated FMS cannot activate FMS-mediated signaling pathways, thus potentially inhibiting cell proliferation in FMS-overexpressed tum... | |||
T63978 | FAK-IN-2 | ||
FAK-IN-2 是一种有效的、口服具有活力的黏着斑激酶 (FAK) 抑制剂 (IC50: 35 nM),表现出抗肿瘤作用。FAK-IN-2 能够剂量依赖的方式共价抑制 FAK 的自磷酸化,也可以抑制肿瘤细胞的形成和迁移,诱导细胞凋亡。 | |||
T62871 | LRRK2-IN-6 | ||
LRRK2-IN-6 (compound 22) 是一种具有血脑屏障通透性的、口服具有活力的、选择性富含亮氨酸重复蛋白激酶 2 基因 (LRRK2) 抑制剂,能够抑制 GS LRRK2 (IC50: 4.6 μM) 和 WT LRRK2 (IC50: 49 μM)。LRRK2-IN-6 对 LRRK2 Ser1292 和 Ser925 的自磷酸化表现出抑制作用。 | |||
T63057 |
LRRK2-IN-5
|
||
LRRK2-IN-5 (compound 25) 是一种口服具有活力的、能透过血脑屏障的、选择性富含亮氨酸重复蛋白激酶 2 基因 (LRRK2) 抑制剂,对 GS LRRK2 (IC50: 1.2 μM) 和 WT LRRK2 (IC50: 16 μM) 具有抑制作用。LRRK2-IN-5 能够抑制 LRRK2 Ser1292 和 Ser925 的自磷酸化。 | |||
T61358 |
AKN-028 acetate
|
||
AKN-028 acetate 是一种新型酪氨酸激酶 (TKI) 抑制剂,是一种有效的口服活性的 FMS 样受体酪氨酸激酶 3 (FLT3) 抑制剂,其 IC50值为 6 nM。AKN-028 acetate 抑制 FLT3 自磷酸化。AKN-028 acetate 诱导剂量依赖性的细胞毒性反应 (平均IC50=1 μM)。AKN-028 acetate 通过激活 caspase 3 诱导细胞凋亡 (apoptosis)。AKN-028 acetate 可用于急性髓系白血病 (AML) 的研究。 | |||
T1181L |
Gefitinib hydrochloride
|
||
Gefitinib hydrochloride (ZD1839 hydrochloride) 是一种有效,选择性和具有口服活性的EGFR 酪氨酸激酶抑制剂,IC50为 33 nM。Gefitinib hydrochloride 选择性抑制 EGF 刺激的肿瘤细胞生长 (IC50为 54 nM),并阻断 EGF 刺激的肿瘤细胞中EGFR 自磷酸化。Gefitinib hydrochloride 也诱导细胞自噬 (autophagy),具有抗肿瘤活性。 | |||
T63630 |
Gefitinib dihydrochloride
|
||
Gefitinib dihydrochloride 是有效的、选择性的、口服具有活力的 EGFR 酪氨酸激酶抑制剂 (IC50: 33 nM)。Gefitinib dihydrochloride 能够选择性抑制 EGF 刺激的肿瘤细胞生长,其IC50值为 54 nM,能够阻断 EGF 刺激的肿瘤细胞中EGFR 自磷酸化。Gefitinib dihydrochloride 可以诱导细胞自噬 (autophagy) 和凋亡 (apoptosis),能够用于进行癌症相关疾病,如肺癌和乳腺癌的研究。 | |||
T37468 |
Siamycin I
|
||
Siamycin I is a tricyclic peptide originally isolated from Streptomyces and has antiviral and antibacterial activities. It is active against laboratory strains and clinical isolates of HIV-1 (ED50s = 0.05-0.45 and 0.89-5.7 μM, respectively), as well as the CBL-20 strain of HIV-2 (ED50 = 0.45 μM), in vitro. Siamycin I inhibits HIV-induced fusion of C8166 T cells with HIV-1-infected CEM-SS cells with an ED50 value of 0.08 μM. It is also active against B. subtilis, M. luteus, and S. aureus (MICs = ... | |||
T69682 |
AEW541 HCl
|
||
AEW541, also known as NVP-AEW541, is a novel, potent IGF-IR kinase inhibitor. NVP-AEW541 is capable of distinguishing between the IGF-IR (IC50 = 0.086 microM) and the closely related InsR (IC50 = 2.3 microM) in cells. NVP- AEW541 abrogates IGF-I-mediated survival and colony formation in soft agar at concentrations that are consistent with inhibition of IGF-IR autophosphorylation. Note: AEW541 has a Cis-configuration on the cyclobutane ring. Its CAS# is 475489-16-8. Many vendors and Sc-finder sc... | |||
T35915 |
Erlotinib-13C6
Erlotinib-13C6 |
||
Erlotinib-13C6 (CP-358774-13C6) is a 13C-labeled Erlotinib. Erlotinib is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR[1]. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer[1].Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process[2]... | |||
T67442 |
CGP-53716
|
||
The growth factors, platelet-derived growth factor (PDGF) and basic fibroblast growth factor (bFGF) play major roles in enhanced smooth muscle cells growth in rodent blood vessels after vascular injury. Tyrosine kinase inhibition has been shown to be effective in blocking tyrosine phosphorylation at the PDGF and bFGF receptors in cultured fibroblast and vascular smooth muscle cells which in turn inhibits their proliferation[1]. CGP 53716 is a specific PDGFR tyrosine kinase inhibitor on SMC (smoo... |