Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
T5093 |
Pim1/AKK1-IN-1
LKB1/AAK1 dual inhibitor,MDK-2275 |
Pim; Hippo pathway | Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
Pim1/AKK1-IN-1 (LKB1/AAK1 dual inhibitor) 是多种酶抑制剂,能够作用于Pim1、AKK1、MST2 和 LKB1,Kd 值分别为 35、53、75 和 380 nM,还抑制 MPSK1 和 TNIK。 | |||
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)。 | |||
T60828 |
AAK1-IN-2
|
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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。 | |||
T60829 |
AAK1-IN-3
|
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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。 | |||
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]. | |||
T61499 |
AAK1-IN-4
|
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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]. | |||
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。 | |||
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。 | |||
T35856 |
BMS-986176
|
AAK1 (AP2 associated kinase 1) | Neuroscience |
BMS-986176 是一种有效的AAK1 抑制剂,IC50为 2.2 nM。BMS-986176在神经退行性疾病中有研究的价值。 | |||
T15781 |
LP-935509
|
Serine/threonin kinase; AAK1 (AP2 associated kinase 1) | Cell Cycle/Checkpoint; Metabolism; Neuroscience |
LP-935509 是一种选择性的、具有脑渗透的、小分子的衔接蛋白-2 相关激酶1 (AAK1) ATP 竞争性抑制剂,其 IC50=3.3 nM,Ki=0.9 nM。它是一种 BIKE 的有效抑制剂 (IC50=14 nM) 和中度的 GAK 抑制剂 (IC50=320 nM)。它能够逆转 SNL 手术后的疼痛。 | |||
T15780 |
LP-922761
|
AAK1 (AP2 associated kinase 1) | Neuroscience |
LP-922761 是一种具有有效性、选择性和口服活性的 AAK1 抑制剂,对 BMP-2 诱导蛋白激酶 (BIKE)有抑制作用。LP-922761 可用于治疗治疗神经性疼痛。 | |||
T10572 |
BMT-124110
|
AAK1 (AP2 associated kinase 1) | Neuroscience |
BMT-124110是一种具有选择性的AAK1抑制剂(IC50: 0.9 nM),具有抗伤害感受活性。BMT-090605抑制BMP -2诱导蛋白激酶BIKE,其IC50为 17 nM。BMT-090605抑制细胞周期蛋白 G 相关激酶GAK,其IC50:为99 nM。 | |||
T10572L |
BMT-124110 Formate
BMT-124110 Formate(1679371-59-5 Free base) |
Serine/threonin kinase; TGF-beta/Smad; AAK1 (AP2 associated kinase 1) | Cell Cycle/Checkpoint; Metabolism; Neuroscience; Stem Cells |
BMT-124110 Formate 是一种具有选择性的AAK1抑制剂(IC50: 0.9 nM),具有抗伤害感受活性。BMT-124110 Formate 抑制BMP -2诱导蛋白激酶BIKE,其IC50为 17 nM。BMT-124110 Formate 抑制细胞周期蛋白 G 相关激酶GAK,其IC50:为99 nM。 | |||
T36680 |
SM1-71
|
Serine/threonin kinase; MAPK; LIM Kinase; TGF-beta/Smad; AAK1 (AP2 associated kinase 1) | Cell Cycle/Checkpoint; MAPK; Metabolism; Neuroscience; Stem Cells |
SM1-71 是一种有效的多靶点丙烯酰胺修饰的 TAK1 抑制剂,抑制 MKNK2、MAP2K1/2/3/4/6/7、GAK、AAK1、BMP2K、MAP3K7、MAPKAPK5、GSK3A/B、MAPK1/3、SRC、YES1、FGFR1、ZAK (MLTK)、MAP3K1、LIMK1 和 RSK2。SM1-71 可作为激酶探针,具有抗癌活性,抑制多种癌细胞系的增殖。 | |||
T77333L |
(Iso)-BMT-124110 Formate
(R)-N-(8-((2-amino-2,4-dimethylpentyl)oxy)-5H-chromeno[3,4-c]pyridin-2-yl)acetamide Formate(1679370-98-9 Free base) |
AAK1 (AP2 associated kinase 1) | Neuroscience |
(Iso)-BMT-124110 Formate 对蛋白丝氨酸/苏氨酸激酶AAK 有抑制作用 ,可用于治疗 帕金森病、精神分裂症、神经性疼痛和阿尔茨海默病。 | |||
T10571 |
BMS-901715
|
Others | Others |
BMS-901715 is an effective and selective inhibitor of adapter protein-2 associated kinase 1 (AAK1; IC50: 3.3 nM). | |||
T30543 |
BMS-911172
BMS911172,BMS 911172 |
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BMS-911172 是一种AAK1 激酶抑制剂,IC50为 35 nM。 | |||
T70459 | BMT-046091 | ||
BMT-046091 is a potent and selective radioligand which inhibits adaptor-associated kinase 1 (AAK1). | |||
T14691 | BMT-090605 | Others | Others |
BMT-090605 is a potent, selective AAK1 inhibitor, with an IC50 of 0.6 nM. BMT-090605 inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50s of 45 and 60 nM, respectively[1]. BMT-090605 shows antinociceptive activity | |||
T61941 | BMT-090605 hydrochloride | ||
BMT-090605 hydrochloride 是有效的,选择性的连接蛋白-2 相关激酶 1(AAK1)抑制剂,(IC50=0.6 nM)。BMT-090605 hydrochloride 抑制 BMP-2 诱导蛋白激酶 (BIKE) (IC50=45 nM)和细胞周期蛋白 G 相关激酶 GAK(IC50=60 nM)。BMT-090605 hydrochloride 显示抗伤害活性。BMT-090605 hydrochloride 在神经性疼痛中具有研究价值。 | |||
T82385 |
FMF-06-098-1
|
PROTACs | PROTAC |
FMF-06-098-1是一种多靶点蛋白降解剂。通过专一性降解作用,FMF-06-098-1针对多种激酶,能够有效降解AAK1, ABL2, AURKA, AURKB, BUB1B, CDC7, CDK1, CDK12, CDK13, CDK2, CDK4, CDK6, CDK7, CDK9, CHEK1, CSNK1D, EPHA1, PER, FGFR1, GAK, IRAK4, ITK, LIMK2, MAP4K2, MAP4K3, MAPK6, MAPK7, MARK4, MELK, PKN3, PLK4, PRKAA1, PTK2, PTK6, RPS6KA4, S1K2, STK35, TNK2, UHMK1, ULK1及WEE1等关键蛋白。 | |||
T62143 | LP-922761 hydrate | ||
LP-922761 hydrate 是一种选择性的、有效的、口服具有活力的 AAK1 抑制剂,在酶和细胞分析中 IC50 值分别为 4.8 nM 和 7.6 nM。LP-922761 hydrate 对 BMP-2 诱导蛋白激酶 (BIKE) 具有抑制作用 (IC50: 24 nM)。LP-922761 hydrate 对细胞 GAK、阿片类药物、肾上腺素 α2 或 GABAa 受体没有明显作用。 | |||
T74644 |
DB0614
|
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DB1113 (Example 24) 是一种靶向蛋白激酶降解的双功能化合物。DB1113 可降解ABL1,ABL2,BLK,CDK11B,CDK4,CSK,EPHA3,FER,GAK,LIMK1,MAP3K20,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK14,MAPK7,MAPK8,MAPK9,MAPKAPK2,MAPKAPK3,NLK,PDIK1L,PTK2B,RIPK1,RPS6KA1,RPS6KA3,SIK2,SIK3,STK35,TNK2 和ULK1。DB1113 可用于研究异常激酶活性介导的疾病或紊乱。 |