48
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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T14152 |
Akt1 and Akt2-IN-1
|
Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
Akt1 and Akt2-IN-1 is an allosteric inhibitor of Akt1 (IC50=3.5 nM) and Akt2 (IC50=42 nM). It has potent and balanced activity. | |||
T3467 |
Miransertib
ARQ-092,AKT inhibitor 2 |
Akt; Parasite | Cytoskeletal Signaling; Microbiology/Virology; PI3K/Akt/mTOR signaling |
Miransertib (ARQ-092) 是一种具有口服活性的,选择性和变构性Akt 抑制剂。它有效抑制利什曼原虫,还是 AKT1-E17K 突变蛋白抑制剂,可研究PI3K/AKT 驱动的肿瘤和 Proteus 综合征。 | |||
T15374 |
Ipatasertib dihydrochloride
GDC-0068 dihydrochloride,RG-7440 dihydrochloride |
Akt; PKA | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) 是ATP 竞争性的pan-Akt 选择性抑制剂,抑制Akt1,Akt2,Akt3,IC50分别为 5,18,8 nM。 | |||
T7885 |
Afuresertib hydrochloride
|
ROCK; Akt; PKC | Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Stem Cells |
Afuresertib hydrochloride 是一个口服有效的,ATP 竞争性的选择性泛Akt 抑制剂,作用于Akt1、Akt2和Akt3,Ki 值分别为 0.08、2和 2.6 nM。 | |||
T23695 |
Akt-I-1,2
|
Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
Akt-I-1,2 是 Akt1 和 Akt2 的选择性抑制剂。 | |||
T7315 |
BAY1125976
|
Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
BAY1125976 是选择性Akt1/Akt2变构抑制剂。在10 μM ATP 时,它抑制 Akt1 和 Akt2 活性的IC50值分别为 5.2 nM 和 18 nM。 | |||
T1952 |
MK-2206 dihydrochloride
MK-2206 2HCl |
Apoptosis; Akt; Autophagy | Apoptosis; Autophagy; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
MK-2206 dihydrochloride (MK-2206 2HCl) 是一种变构 Akt 抑制剂,抑制 Akt1、Akt2 和 Akt3 (IC50=8/12/65 nM),具有口服活性的、高效选择性。MK-2206 dihydrochloride 具有抗肿瘤活性。 | |||
T38846 |
Vevorisertib trihydrochloride
ARQ 751 trihydrochloride |
Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
Vevorisertib trihydrochloride(ARQ 751 trihydrochloride) 是一种具有选择性和有效性的 pan-AKT 和 AKT1-E17K 突变抑制剂,抑制 AKT1 、AKT2 和 AKT3 。 Vevorisertib trihydrochloride 可用于研究肝癌和晚期实体瘤。 | |||
T14072 |
A-443654
|
ERK; VEGFR; GSK-3; FLT; Casein Kinase; MAPK; Akt; PKA; Chk; CDK; Src; PKC; S6 Kinase | Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; MAPK; Metabolism; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors |
A-443654 是 pan-Akt 抑制剂,对Akt1,Akt2,和Akt3具有同等效力的抑制作用,Ki=均为 160 pM。 | |||
T39733 |
Hu7691 free base
|
Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
Hu7691 free base 是一种具有口服活性、高效性和选择性的 Akt 抑制剂,对多种神经母细胞瘤细胞系的抗增殖和神经发生作用。Hu7691 free base 抑制 Akt1、Akt2 和 Akt3 ,诱导神经母细胞瘤细胞分化。 | |||
T1920 |
Capivasertib
AZD5363 |
Akt; PKA; mTOR; Autophagy | Autophagy; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
Capivasertib (AZD5363) 是一种广谱的 AKT 抑制剂,对 Akt1、Akt2 和 Akt3 均有抑制活性 (IC50=3/7/7 nM),具有口服活性。Capivasertib 具有抗肿瘤活性,可以用于治疗乳腺癌。 | |||
T14034 |
3CAI
|
Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
3CAI 是特异性的AKT1和AKT2抑制剂。 | |||
T1911 |
Afuresertib
GSK2110183C,GSK2110183 |
ROCK; Akt; PKC | Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Stem Cells |
Afuresertib (GSK2110183) 是一个选择性,ATP 竞争性,口服有效的泛 Akt 抑制剂,作用于 Akt1、Akt2和 Akt3,Ki 值分别为 0.08、2、2.6 nM。 | |||
T6252 |
Ipatasertib
GDC-0068,RG7440,帕他色替 |
Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
Ipatasertib (GDC-0068) 是选择性的,ATP 竞争性的pan-Akt 抑制剂,能够抑制Akt1 (IC50:5 nM),Akt2 (IC50:18 nM),Akt3 (IC50:8 nM)。 | |||
T3346 |
AKT inhibitor VIII
AKTi-1/2 |
Apoptosis; Akt | Apoptosis; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
AKT inhibitor VIII (AKTi-1/2) 是一种细胞渗透的喹喔啉化合物,可逆的选择性抑制Akt1、Akt2和Akt3的活性,IC50值分别为 58 nM、210 nM 和 2119 nM。 | |||
T16836 |
SAFit2
|
FKBP | Apoptosis; Autophagy; Immunology/Inflammation |
SAFit2是一种高效、具有选择性的fk506结合蛋白51(FKBP51)抑制剂(Ki:6 nM)。SAFit2能增强AKT2-AS160的结合,参与体内糖皮质激素释放的下游反应,是治疗肥胖、慢性疼痛、抑郁和焦虑的候选化合物。 | |||
T6304 |
AT7867
|
Akt; PKA; S6 Kinase | Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
AT7867 是 ATP 竞争性的Akt1/Akt2/Akt3和p70S6K/PKA 抑制剂,IC50分别为 32、17、47 和 85、20 nM。 | |||
T6849 |
Uprosertib
GSK2141795,GSK795,优普色替 |
Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
Uprosertib (GSK2141795) 是一种有效的,选择性的 Akt 广谱抑制剂,对 Akt1/Akt2/Akt3 的 IC50值分别为 180/328/38 nM。 | |||
T2482 |
AT13148
|
ROCK; SGK; Akt; PKA; S6 Kinase | Cell Cycle/Checkpoint; Cytoskeletal Signaling; MAPK; Metabolism; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors |
AT13148 是一种 ATP 竞争性 AGC 激酶口服抑制剂,能够抑制 Akt1/Akt2/Akt3、p70S6K、PKA 和 ROCKI/ROCKII 的活性,IC50值分别为 38/402/50、8、3 和 6 nM/4 nM。 | |||
T6285 |
GSK-690693
GSK690693 |
Serine Protease; Akt; PKC; AMPK; Autophagy | Autophagy; Chromatin/Epigenetic; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Proteases/Proteasome |
GSK-690693 是一种泛 Akt 抑制剂,对 Akt1、Akt2和 Akt3的 IC50分别为 2 nM、13 nM 和9 nM。它也是一种 AMPK 的抑制剂,影响 ULK1 的活性,并能显著抑制 STING 依赖的 IRF3 的激活。 | |||
T6303 |
CCT128930
|
Akt; PKA; S6 Kinase; Autophagy | Autophagy; Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
CCT128930 是一种 ATP 竞争性,选择性 AKT 抑制剂。它通过靶向 AKT 的 Met282 (PKA-AKT 嵌合体的 Met173),对 PKA 激酶具有 28 倍的选择性,对 p70S6K 具有 20 倍的选择性,具有抗肿瘤活性。 | |||
T11664 |
INY-03-041
|
Others | Others |
INY-03-041, a potent and highly selective PROTAC-based pan-AKT degrader, inhibits AKT1, AKT2, and AKT3 with IC50s of 2.0 nM, 6.8 nM, and 3.5 nM, respectively. This compound consists of the ATP-competitive AKT inhibitor GDC-0068 conjugated to Lenalidomide. | |||
T15428 |
Uprosertib hydrochloride
GSK2141795 (hydrochloride) |
Others | Others |
Uprosertib hydrochloride is a potent and selective inhibitor of pan-Akt (IC50: 180/328/38 nM for Akt1/Akt2/Akt3, respectively). | |||
T61680 | AKT-IN-5 | ||
AKT-IN-5 (Example 8) is a chemical compound known as an Akt inhibitor, specifically targeting Akt1 and Akt2. Its potency is reflected in IC50 values of 450 nM and 400 nM for Akt1 and Akt2, respectively [1]. | |||
T10275 |
AKT-IN-3
|
Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
AKT-IN-3 is a potent, orally active low hERG blocking Akt inhibitor (IC50: 1.4 nM, 1.2 nM, and 1.7 nM for Akt1, Akt2, and Akt3). AKT-IN-3 (compound E22) also exhibits good inhibitory activity against other AGC family kinases, such as PKA, PKC, ROCK1, RSK1 | |||
T39930 |
MS98
|
||
MS98 is a highly effective and specific PROTAC AKT degrader compound that effectively targets and depletes total AKT (T-AKT) within cells, exhibiting a DC 50 value of 78 nM. This compound readily binds to AKT1, AKT2, and AKT3 with respective dissociation constants (Kd s) of 4 nM, 140 nM, and 8.1 nM. | |||
T25791 |
Merck-22-6
Merck 22 6,Merck226 |
||
Merck-22-6 is an allosteric dual inhibitor of Akt1, Akt2. | |||
T74983 | MS15 | ||
MS15 是一种有效且选择性的AKTPROTAC 降解剂。 MS15 可抑制 AKT1、-2 和 -3 活性,IC50值分别为 798 nM、90 nM 和 544 nM。 | |||
T62842 | AKT-IN-8 | ||
AKT-IN-8 是一种 AKT 的有效抑制剂,能够作用于 AKT1 (IC50: 4.46 nM)、AKT2 (IC50: 2.44 nM) 和 AKT3 (IC50: 9.47 nM)。 | |||
T39899 | Hu7691 | Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
Hu7691 是一种具有口服活性、选择性和高效性的 Akt 抑制剂,抑制 Akt1、Akt2 和 Akt3,抑制神经母细胞瘤细胞增殖,诱导神经母细胞瘤细胞的分化。 | |||
T63039 |
AKT-IN-13
|
||
AKT-IN-13 (compound 4b) 是一种 Akt 的有效抑制剂,能够作用于 Akt1 (IC50: 1.6 nM)、Akt2 (IC50: 2.4 nM) 和 Akt3 (IC50: 0.3 nM) 。AKT-IN-13 能够用于研究抗癌。 | |||
T39928 | MS170 | ||
MS170 is a highly effective and specific PROTAC AKT degrader compound that exhibits potent activity. It efficiently reduces the levels of total AKT (T-AKT) within cells, with a DC 50 value of 32 nM. Furthermore, MS170 demonstrates strong binding affinity towards AKT isoforms, specifically AKT1, AKT2, and AKT3, with respective dissociation constants (Kd) of 1.3 nM, 77 nM, and 6.5 nM. | |||
T74001 | INY-03-041 trihydrochloride | ||
INY-03-041 trihydrochloride 是一种有效的、高选择性的、基于PROTAC 的泛-AKT 降解剂,由ATP 竞争性AKT 抑制剂Ipatasertib 结合Lenalidomide 组成。INY-03-041 trihydrochloride 可抑制AKT1,AKT2和AKT3,IC50分别为 2.0 nM,6.8 nM 和 3.5 nM。 | |||
T21624 | AT7867 dihydrochloride | ||
AT7867 dihydrochloride 是一种有效的ATP 竞争性的Akt1/Akt2/Akt3和p70S6K/PKA 抑制剂,IC50值分别为 32 nM/17 nM/47 nM 和 85 nM/20 nM,具有癌症治疗的潜力。 | |||
T38847 |
Vevorisertib
Vevorisertib,ARQ 751 |
||
Vevorisertib (ARQ 751) is a highly effective oral compound that selectively inhibits pan-AKT serine/threonine kinases such as AKT1 (with an IC50 value of 0.55 nM), AKT2 (with an IC50 value of 0.81 nM), and AKT3 (with an IC50 value of 1.31 nM). This compound, either as a standalone treatment option or in combination with other anti-cancer agents, is ideally suited for conducting research on solid tumors characterized by PIK3CA/AKT/PTEN mutations[4]. | |||
T63200 | NTQ1062 | ||
NTQ1062 (compound 22b) 是口服具有活力的、有效的Akt 抑制剂,能够作用于 Akt1 (IC50: 0.4 nM)、Akt2 (IC50: 6.3 nM) 和 Akt3 (IC50: 0.1 nM)。NTQ1062 对多种癌细胞表现出抗增殖作用,能够将细胞周期阻滞在 G0/G1 期,诱导细胞凋亡 (apoptosis)。NTQ1062 在 LNCap 异种移植瘤小鼠模型中显示出显著的的抗肿瘤效果。 | |||
T77968 |
MS15 TFA
|
PROTACs | PROTAC |
MS15 TFA,作为一种有效且选择性的AKTPROTAC降解剂,能够针对AKT-1、-2 及 -3活性进行抑制,其IC50值分别为798 nM、90 nM和544 nM。 | |||
T81784 |
MK-2206 free base
|
Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
MK-2206 free base是一种口服活性、高选择性的变构Akt抑制剂,IC50分别针对Akt1、Akt2、Akt3为8、12和65 nM 。多种乳腺癌细胞系、PIK3CA突变以及PTEN缺失细胞系对此化合物敏感,显示出抗癌活性。 | |||
T62609 |
MK-2206
|
||
MK-2206 是一种具有口服具有活力的、高效选择性的变构 Akt 抑制剂,能够作用于 Akt1 (IC50: 8 nM)、Akt2 (IC50: 12 nM) 和 Akt3 (IC50: 65 nM)。许多乳腺癌细胞系、PIK3CA 突变体和 PTEN 丢失细胞系对 MK-2206 敏感。MK-2206 具有抗癌作用。 | |||
T62149 |
ALM301
|
||
ALM301 是一种高度特异性的、口服具有活力的 AKT 抑制剂,能够作用于 AKT1 (IC50: 0.13 μM)、AKT2 (IC50: 0.09 μM) 和 AKT3 (IC50: 2.75 μM)。ALM301 在体外能够抑制 AKT 磷酸化,并对下游信号具有调节作用。ALM301 对癌细胞增殖和肿瘤生长表现出抑制作用。 | |||
T62907 | TAS-117 hydrochloride | ||
TAS-117 hydrochloride 是一种选择性的、有效的、口服具有活力的别构 Akt 抑制剂,作用于 Akt1 (IC50: 4.8 nM) 、Akt2 (IC50: 1.6 nM) 和 Akt3 (IC50: 44 nM)。TAS-117 hydrochloride 能够激发抗骨髓瘤活性,增强蛋白酶体抑制诱导的致命内质网应激,可以诱导细胞凋亡和自噬。 | |||
T6303L |
CCT128930 hydrochloride
CCT128930 hydrochloride(885499-61-6 Free base) |
Apoptosis; Akt; PKA; mTOR; Autophagy | Apoptosis; Autophagy; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
CCT128930 hydrochloride (CCT128930 hydrochloride) 是一种选择性 AKT 抑制剂,具有抗肿瘤活性。它通过靶向 AKT 的 Met282 (PKA-AKT 嵌合体的 Met173),对 PKA 激酶具有 28 倍的选择性,对 p70S6K 具有 20 倍的选择性。 | |||
T17346 | 9-Decyn-1-ol | Others | Others |
9-Decyn-1-ol is an alkyl/ether-based PROTAC linker suitable for synthesizing PROTACs. It serves as a conjugation agent to combine GDC-0068 and Lenalidomide, resulting in the formation of INY-03-041. INY-03-041 is a potent and highly selective pan-Akt degrader that operates through the PROTAC mechanism. It effectively inhibits Akt1, Akt2, and Akt3 with IC50 values of 2.0 nM, 6.8 nM, and 3.5 nM, respectively[1]. | |||
T22247 | Miransertib (ARQ 092) HCl | ||
Miransertib hydrochloride (ARQ-092 hydrochloride) is a powerful, orally bioavailable, selective, and allosteric inhibitor of Akt. It exhibits an inhibitory concentration (IC50) of 2.7 nM, 14 nM, and 8.1 nM against Akt1, Akt2, and Akt3, respectively. In addition to its Akt inhibitory activity, Miransertib hydrochloride also demonstrates significant potency as an inhibitor of the AKT1-E17K mutant protein. This compound shows promise in research related to PI3K/AKT-driven tumors and Proteus syndrom... | |||
T18065 |
Lenalidomide-C9-aldehyde
|
Others | Others |
Lenalidomide-C9-aldehyde is a synthesized E3 ligase ligand-linker conjugate that incorporates the Lenalidomide based cereblon ligand and a linker. Lenalidomide-C9-aldehyde can be used in the synthesis of a series of PROTACs, such as INY-03-041. INY-03-041 | |||
T13134 |
(+)-Tetrabenazine
(+)-TBZ,(3R,11bR)-Tetrabenazine,(3R,11bR)-TBZ |
Monoamine Transporter | Membrane transporter/Ion channel |
(+)-Tetrabenazine ((3R,11bR)-Tetrabenazine) 是一种可逆的囊泡单胺转运蛋白2 (VMAT-2)抑制剂,对 VMAT2转运的抑制作用是VMAT1的10倍。 | |||
T28923 |
TAS-117
TAS117,TAS 117 |
||
TAS-117, a PKB/Akt inhibitor, is used potentially for the treatment of solid tumors. | |||
T39519 |
GSK269962A hydrochloride
GSK 269962 hydrochloride |
||
GSK269962A hydrochloride (GSK 269962 hydrochloride) is a highly potent inhibitor of ROCK1 and ROCK2, with IC50 values of 1.6 nM and 4 nM, respectively, for recombinant human isoforms. This compound exhibits both anti-inflammatory and vasodilatory properties. |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2790 |
Oridonin
NSC-250682,Rubescenin,冬凌草甲素,Isodonol,Rubescensin A |
Akt; Antibacterial | Cytoskeletal Signaling; Microbiology/Virology; PI3K/Akt/mTOR signaling |
Oridonin (NSC-250682) 是从Rabdosia rubescens 中得到的二萜,是一种AKT 抑制剂,对 AKT1 和 AKT2 的IC50值分别为 8.4 和 8.9 μM,具有抗菌、抗炎、抗肿瘤等功效。 |