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Targets Recommended: AAK1 (AP2 associated kinase 1) Sirtuin

32

抑制剂 & 化合物

6

重组蛋白

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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)。
T60828 AAK1-IN-2

Others Others
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。
T63031 PAK1-IN-1

Others Others
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。
T41166 NVS PAK1 C

Others Others
NVS PAK1 C is a negative control of NVS PAK1 1, a potent and selective PAK1 inhibitor.
T70741 AZ-TAK1

Others Others
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...
T34630 SGC-AAK1-1N

SGCAAK11N,SGCAAK1-1N,SGC-AAK11N

Others Others
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)。
T64265 JAK1/TYK2-IN-3

Others Others
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。
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).
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).
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。
T35928 NVS-PAK1-C

NVS-PAK1-C

Others Others
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)。
T72421 LRRK2/NUAK1/TYK2-IN-1

Others Others
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。
T63834 AAK1-IN-3 TFA

Others Others
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。
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。
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。
T63833 AAK1-IN-2 TFA

Others Others
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。
T36782 TAK1-IN-2

TAK1-IN-2

Others Others
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.
T70877 JAK1-IN-B61

Others Others
JAK1-IN-B61 is a JAK1 inhibitor.
T72957 DRAK1/2-IN-1

Others Others
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

Others Others
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].
T61693 AAK1-IN-5

Others Others
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].
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。
T62155 JAK1-IN-9

Others Others
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。
T39314 JAK1/TYK2-IN-1

JAK1/TYK2-IN-1

Others Others
JAK1/TYK2-IN-1 is a dual inhibitor of TYK2 and JAK1 ( IC 50 = 29 and 41 nM respectively).
T60829 AAK1-IN-3

Others Others
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。
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

Others Others
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)。

化合物

AK-1
Cat.No: T5618
Synonym:
Target: Sirtuin
NVS-PAK1-1
Cat.No: T16367
Synonym:
Target: PAK
JAK1/2/3 Inhibitor 1
Cat.No: T77504
Synonym:
Target: PKA
SGC-AAK1-1
Cat.No: T12885
Synonym:
Target: AAK1 (AP2 associated kinase 1)
TAK1-IN-3
Cat.No: T40577
Synonym:
Target: MAPK
JAK1-IN-8
Cat.No: T35899
Synonym: JAK1-IN-8
Target: JAK
AAK1-IN-2
Cat.No: T60828
Synonym:
Target: Others
PAK1-IN-1
Cat.No: T63031
Synonym:
Target: Others
NVS PAK1 C
Cat.No: T41166
Synonym:
Target: Others
AZ-TAK1
Cat.No: T70741
Synonym:
Target: Others
SGC-AAK1-1N
Cat.No: T34630
Synonym: SGCAAK11N,SGCAAK1-1N,SGC-AAK11N
Target: Others
JAK1/TYK2-IN-3
Cat.No: T64265
Synonym:
Target: Others
JAK1-IN-4
Cat.No: T15606
Synonym:
Target: JAK
TAK1/MAP4K2 inhibitor 1
Cat.No: T10444
Synonym:
Target: Others
JAK1-IN-11
Cat.No: T79079
Synonym:
Target: JAK
NVS-PAK1-C
Cat.No: T35928
Synonym: NVS-PAK1-C
Target: Others
LRRK2/NUAK1/TYK2-IN-1
Cat.No: T72421
Synonym:
Target: Others
AAK1-IN-3 TFA
Cat.No: T63834
Synonym:
Target: Others
JAK1-IN-10
Cat.No: T79078
Synonym:
Target: JAK
TAK1 inhibitor
Cat.No: T67909
Synonym: compound 13a
Target: Topoisomerase
AAK1-IN-2 TFA
Cat.No: T63833
Synonym:
Target: Others
TAK1-IN-2
Cat.No: T36782
Synonym: TAK1-IN-2
Target: Others
JAK1-IN-B61
Cat.No: T70877
Synonym:
Target: Others
DRAK1/2-IN-1
Cat.No: T72957
Synonym:
Target: Others
AAK1-IN-4
Cat.No: T61499
Synonym:
Target: Others
AAK1-IN-5
Cat.No: T61693
Synonym:
Target: Others
EAK16-II
Cat.No: T82513
Synonym:
Target:
JAK1-IN-9
Cat.No: T62155
Synonym:
Target: Others
JAK1/TYK2-IN-1
Cat.No: T39314
Synonym: JAK1/TYK2-IN-1
Target: Others
AAK1-IN-3
Cat.No: T60829
Synonym:
Target: Others
BMS-911543
Cat.No: T6790
Synonym: BMS911543
Target: Tyrosine Kinases, Histone Methyltransferase, JAK
JAK-IN-23
Cat.No: T62556
Synonym:
Target: Others
Cat. No. Product Name Species Expression System
TMPH-02961 JAK1 Protein, Mouse, Recombinant (His)

Janus kinase 1,Jak1,Tyrosine-prot...

Mouse E. coli
Tyrosine kinase of the non-receptor type, involved in the IFN-alpha/beta/gamma signal pathway. Kinase partner for the interleukin (IL)-2 receptor as well as interleukin (IL)-10 receptor. Directly phosphorylates STAT but also activates STAT signaling through the transactivation of other JAK kinases associated with signaling receptors. JAK1 Protein, Mouse, Recombinant (His) is expressed in E. coli expression system with N-6xHis tag. The predicted molecular weight is 39.1 kDa and the accession numb...
TMPH-02273 JAK1 Protein, Human, Recombinant (His)

JAK1,Janus kinase 1,Tyrosine-prot...

Human P. pastoris (Yeast)
Tyrosine kinase of the non-receptor type, involved in the IFN-alpha/beta/gamma signal pathway. Kinase partner for the interleukin (IL)-2 receptor as well as interleukin (IL)-10 receptor. Directly phosphorylates STAT but also activates STAT signaling through the transactivation of other JAK kinases associated with signaling receptors.
TMPH-03456 CAK1 Protein, S. cerevisiae, Recombinant (His & Myc)

CAK1,CIV1,Serine/threonine-protei...

Saccharomyces cerevisiae Baculovirus Insect Cells
CAK1 Protein, S. cerevisiae, Recombinant (His & Myc) is expressed in Baculovirus insect cells with N-10xHis and C-Myc tag. The predicted molecular weight is 46.1 kDa and the accession number is P43568.
TMPH-03457 CAK1 Protein, S. cerevisiae, Recombinant (E. coli, His & Myc)

Serine/threonine-protein kinase CAK1,C...

Saccharomyces cerevisiae E. coli
CAK1 Protein, S. cerevisiae, Recombinant (E. coli, His & Myc) is expressed in E. coli expression system with N-10xHis and C-Myc tag. The predicted molecular weight is 49.6 kDa and the accession number is P43568.
TMPH-02272 JAK1 Protein, Human, Recombinant (E. coli, His)

Tyrosine-protein kinase JAK1,JAK<...

Human E. coli
Tyrosine kinase of the non-receptor type, involved in the IFN-alpha/beta/gamma signal pathway. Kinase partner for the interleukin (IL)-2 receptor as well as interleukin (IL)-10 receptor. Directly phosphorylates STAT but also activates STAT signaling through the transactivation of other JAK kinases associated with signaling receptors.
TMPH-02091 PAK1 Protein, Human, Recombinant (His & SUMO)

Serine/threonine-protein kinase PAK 1,p2

Human E. coli
PAK1 Protein, Human, Recombinant (His & SUMO) is expressed in E. coli.

重组蛋白

JAK1 Protein, Mouse, Recombinant (His)
Cat.No: TMPH-02961
Species: Mouse
Expression System: E. coli
JAK1 Protein, Human, Recombinant (His)
Cat.No: TMPH-02273
Species: Human
Expression System: P. pastoris (Yeast)
CAK1 Protein, S. cerevisiae, Recombinant (His & Myc)
Cat.No: TMPH-03456
Species: Saccharomyces cerevisiae
Expression System: Baculovirus Insect Cells
CAK1 Protein, S. cerevisiae, Recombinant (E. coli, His & Myc)
Cat.No: TMPH-03457
Species: Saccharomyces cerevisiae
Expression System: E. coli
JAK1 Protein, Human, Recombinant (E. coli, His)
Cat.No: TMPH-02272
Species: Human
Expression System: E. coli
PAK1 Protein, Human, Recombinant (His & SUMO)
Cat.No: TMPH-02091
Species: Human
Expression System: E. coli
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