Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T5618 |
AK-1
|
Sirtuin | Chromatin/Epigenetic; DNA Damage/DNA Repair |
AK-1是一种特异性有效和细胞可渗透的SIRT2抑制剂,其IC50值为 12.5 μM。它可防止阿尔茨海默病模型中的海马神经退行性变并诱导结肠癌细胞中的细胞周期停滞。 | |||
T16367 |
NVS-PAK1-1
|
PAK | Cytoskeletal Signaling |
NVS-PAK1-1 是一种有效的选择性变构 PAK1 抑制剂,IC50值为5 nM。 | |||
T77504 |
JAK1/2/3 Inhibitor 1
|
PKA | Tyrosine Kinase/Adaptors |
JAK1/2/3 Inhibitor 1 是一种有效的蛋白激酶抑制剂。2,4-dichlorothieno[3,2-d]pyrimidine 具有抗肿瘤活性可抑制多种癌细胞株的生长。它通过与癌细胞的骨架结合,抑制新蛋白质的生成,从而抑制癌细胞的生长。 | |||
T12885 |
SGC-AAK1-1
|
AAK1 (AP2 associated kinase 1) | Neuroscience |
SGC-AAK1-1 是选择性的 AAK1(AP2 相关的激酶 1) 抑制剂,IC50=270 nM,Ki=9 nM,也抑制 BMP2K。它用于与 AAK1 相关的 Wnt 途径的研究。 | |||
T40577 |
TAK1-IN-3
|
MAPK | MAPK |
TAK1-IN-3 是一种新型 ATP 竞争性 TAK1 抑制剂,可用于研究癌症。 | |||
T35899 |
JAK1-IN-8
JAK1-IN-8 |
JAK | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
JAK1-IN-8,Janus 激酶 1 (JAK1)的特异性抑制剂(IC50<500 nM)。 | |||
T63031 | PAK1-IN-1 | ||
PAK1-IN-1 是一种选择性的、有效的 PAK1 抑制剂 (IC50: 9.8 nM)。PAK1-IN-1 通过剂量依赖性方式抑制 PAK1 相关肿瘤细胞的迁移和侵袭。 | |||
T60828 |
AAK1-IN-2
|
||
AAK1-IN-2 (compound (S)-31) 可用于神经性疼痛的研究,它是衔接蛋白 2 相关激酶 1 (AAK1)的选择性抑制剂 (IC50 = 5.8 nM),具有脑渗透性。 | |||
T41166 | NVS PAK1 C | ||
NVS PAK1 C is a negative control of NVS PAK1 1, a potent and selective PAK1 inhibitor. | |||
T64265 | JAK1/TYK2-IN-3 | ||
JAK1/TYK2-IN-3 是一种选择性的、有效的、口服具有活力的 TYK2 (IC50: 6 nM) 和 JAK1 (IC50: 37 nM) 双重抑制剂。JAK1/TYK2-IN-3 能够选择性的作用于 JAK2 和JAK3,其 IC50 值为 140 nM 和 362 nM。JAK1/TYK2-IN-3 能够调节 TYK2/JAK1 相关基因的表达,并调节 Th1 、Th2 和 Th17 细胞的形成,发挥其抗炎活性。 | |||
T34630 |
SGC-AAK1-1N
SGCAAK11N,SGCAAK1-1N,SGC-AAK11N |
||
SGC-AAK1-1N 是一种有效且选择性的 AAK1(AP2 相关激酶 1)小分子抑制剂(IC50=1.8 μM)。 | |||
T70741 |
AZ-TAK1
|
||
AZ-Tak1 is a potent and a relatively selective inhibitor of TAK1 kinase activity, with an IC50 of 0.009 mM. AZ-Tak1 treatment decreased the level of p38 and ERK in mantle cell lymphoma cells, and induced apoptosis in a dose and time dependent manner, with an IC50 of 0.1–0.5 mM. Using the annexin-V and PI staining and FACS analysis, After 48 hours of incubation, AZ-Tak1 (0.1 mM) induced apoptosis in 28%, 34% and 86% of Mino, SP53, and Jeko cells, respectively, which was increased to 32%, 42%, and... | |||
T63834 | AAK1-IN-3 TFA | ||
AAK1-IN-3 TFA 是一种能够透过血脑屏障的适配蛋白 2 相关激酶 1 (AAK1) 抑制剂 (IC50: 11 nM),是一种喹啉类似物。AAK1-IN-3 对神经病理性疼痛表现出研究潜力。 | |||
T35928 |
NVS-PAK1-C
NVS-PAK1-C |
||
NVS-PAK1-C 是一种有效的、ATP 竞争的特异性变构 PAK1抑制剂探针。NVS-PAK1-C 可抑制去磷酸化的 PAK1(IC50= 5 nM) 和磷酸化的 PAK1(IC50= 6 nM)。NVS-PAK1-C 也可以抑制去磷酸化的 PAK2 (IC50=270 nM) 和磷酸化的 PAK2 (IC50=720 nM)。 | |||
T79079 |
JAK1-IN-11
|
JAK | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
JAK1-IN-11(compound 11)是一种针对JAK1和JAK2具有显著抑制效果的化合物,其中对JAK1的IC50为0.02 nM,对JAK2的IC50为0.44 nM,表现出对JAK1较高的选择性。 | |||
T15606 |
JAK1-IN-4
|
JAK | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
JAK1-IN-4 is a selective JAK1 inhibitor (IC50s: 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, and JAK3, respectively). JAK1-IN-4 inhibits STAT3 phosphorylation in NCI-H 1975 cells (IC50, 227 nM). | |||
T72421 |
LRRK2/NUAK1/TYK2-IN-1
|
||
LRRK2/NUAK1/TYK2-IN-1 (conpound 226) 显示出对 LRRK2(Wt)、LRRK2(G2019)、TYK2和 NUAK1的抑制活性,其IC50值小于 10 nM。LRRK2/NUAK1/TYK2-IN-1 可用于自身免疫性疾病研究。 | |||
T10444 |
TAK1/MAP4K2 inhibitor 1
|
Others | Others |
TAK1/MAP4K2 inhibitor 1 is a potent dual inhibitor of TGFβ-activated kinase 1 (TAK1) and MAP4K2 (IC50s: 41.1 nM and 18.2 nM). | |||
T63833 | AAK1-IN-2 TFA | ||
AAK1-IN-2 TFA (compound (S)-31) 是一种选择性的、有效的、能够透过血脑屏障的 AAK1 抑制剂 (IC50: 5.8 nM)。AAK1-IN-2 TFA 能够用于研究神经性疼痛。 | |||
T67909 |
TAK1 inhibitor
compound 13a |
Topoisomerase | DNA Damage/DNA Repair |
TAK1 inhibitor 是一种抑制剂,对MCF-7、A549 、DU-145 、MDA MB-231有抑制作用,IC50分别为 0.021、0.14、0.064 、0.19 。化合物13 具有较好的抑菌活性,麦克风范围为93.7 ~ 46.9μg / mL,麦克风范围为7.8 ~ 5.8μg / mL。 | |||
T70877 | JAK1-IN-B61 | ||
JAK1-IN-B61 is a JAK1 inhibitor. | |||
T36782 |
TAK1-IN-2
TAK1-IN-2 |
||
TAK1-IN-2 is a potent and selective TAK1 inhibitor, with an IC50> of 2 nM[1]. TAK1-IN-2 (compound 54) (10 μM) has no effect on cell viability in TNF-α stimulated HCT-15 cells[1]. [1]. Veerman JJN, et, al. Discovery of 2,4-1 H-Imidazole Carboxamides as Potent and Selective TAK1 Inhibitors. ACS Med Chem Lett. 2021 Mar 3;12(4):555-562. | |||
T61693 | AAK1-IN-5 | ||
AAK1-IN-5 is a potent and specific inhibitor of adaptor protein-2-associated kinase 1 (AAK1), characterized by its ability to penetrate the central nervous system and its oral bioavailability. It displays high selectivity, with an AAK1 inhibitory potency (IC 50) of 1.2 nM, a binding affinity (K i) of 0.05 nM, and an inhibitory potency against cellular AAK1 activity (cell IC 50) of 0.5 nM. AAK1-IN-5 holds promise for investigating neuropathic pain in scientific research [1]. | |||
T79078 |
JAK1-IN-10
|
JAK | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
JAK1-IN-10(compound 9)为氰基取代的环肼类衍生物,表现出高选择性与效率作为JAK1抑制剂。 | |||
T72957 |
DRAK1/2-IN-1
|
||
DRAK1/2-IN-1 是一种活性的DRAK1和DRAK2双重抑制剂,Kd 值分别为 1 μM 和 6 μM。 | |||
T61499 |
AAK1-IN-4
|
||
AAK1-IN-4 is a potent and specific inhibitor of adaptor protein-2-associated kinase 1 (AAK1), capable of efficiently penetrating the central nervous system and exhibiting oral bioactivity. It has demonstrated a high degree of selectivity with an AAK1 inhibitory concentration (IC50) of 4.6 nM, a Filt dissociation constant (Ki) of 0.9 nM, and a cellular IC50 of 8.6 nM. AAK1-IN-4 holds promise as a valuable tool in the investigation of neuropathic pain [1]. | |||
T62155 | JAK1-IN-9 | ||
JAK1-IN-9 (compound 23a) 是一种有效的选择性JAK1抑制剂,IC50为 72 nM。JAK1-IN-9 对其他 JAK 亚型 具有 12 倍或更多的选择性。 | |||
T82513 |
EAK16-II
|
||
EAK16-II为两亲性肽,其通过浓度依赖性机制抑制EAKIIH6的自组装。 | |||
T60829 |
AAK1-IN-3
|
||
AAK1-IN-3 是一种喹啉类似物,可用于研究神经病理性疼痛。AAK1-IN-3 是衔接蛋白 2 相关激酶 1 (AAK1) 抑制剂,IC50为 11 nM,具有脑渗透性。 | |||
T39314 |
JAK1/TYK2-IN-1
JAK1/TYK2-IN-1 |
||
JAK1/TYK2-IN-1 is a dual inhibitor of TYK2 and JAK1 ( IC 50 = 29 and 41 nM respectively). | |||
T6790 |
BMS-911543
BMS911543 |
Tyrosine Kinases; Histone Methyltransferase; JAK | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors |
BMS-911543 是一种选择性 JAK2抑制剂,IC50值为 1.1 nM,对 JAK1、JAK3 和 TYK2 的选择性相对较弱,IC50值分别为 75、360 和 66 nM。 | |||
T62556 | JAK-IN-23 | ||
JAK-IN-23 是一种口服具有活力的、双重的 JAK/STAT 和 NF-κB 抑制剂。JAK-IN-23 能够抑制 J AK1 (IC50: 8.9 nM)、J AK2 (IC50: 15 nM)、J AK3 (IC50: 46.2 nM)。JAK-IN-23 能够较强抑制干扰素刺激基因 (ISG) (IC50: 3.3 nM) 和 NF-κB 通路 (IC50: 150.7 nM)。JAK-IN-23 表现出很强的抗炎效果,可以降低各种促炎因子的释放。JAK-IN-23 能够用于研究炎症性肠病 (IBD)。 |