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48

抑制剂 & 化合物

1

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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,Akt2Akt3,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、Akt2Akt3,Ki 值分别为 0.08、22.6 nM。
T23695 Akt-I-1,2

Akt Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
Akt-I-1,2Akt1 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、Akt2Akt3 (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 、AKT2AKT3 。 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、Akt2Akt3 ,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、Akt2Akt3 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、Akt2Akt3,Ki 值分别为 0.08、22.6 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、Akt2Akt3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、Akt2Akt3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、Akt2Akt3,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,AKT2AKT3,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、Akt2Akt3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.

化合物

Akt1 and Akt2-IN-1
Cat.No: T14152
Synonym:
Target: Akt
Miransertib
Cat.No: T3467
Synonym: ARQ-092,AKT inhibitor 2
Target: Akt, Parasite
Ipatasertib dihydrochloride
Cat.No: T15374
Synonym: GDC-0068 dihydrochloride,RG-7440 dihydrochloride
Target: Akt, PKA
Afuresertib hydrochloride
Cat.No: T7885
Synonym:
Target: ROCK, Akt, PKC
Akt-I-1,2
Cat.No: T23695
Synonym:
Target: Akt
BAY1125976
Cat.No: T7315
Synonym:
Target: Akt
MK-2206 dihydrochloride
Cat.No: T1952
Synonym: MK-2206 2HCl
Target: Apoptosis, Akt, Autophagy
Vevorisertib trihydrochloride
Cat.No: T38846
Synonym: ARQ 751 trihydrochloride
Target: Akt
A-443654
Cat.No: T14072
Synonym:
Target: ERK, VEGFR, GSK-3, FLT, Casein Kinase, MAPK, Akt, PKA, Chk, CDK, Src, PKC, S6 Kinase
Hu7691 free base
Cat.No: T39733
Synonym:
Target: Akt
Capivasertib
Cat.No: T1920
Synonym: AZD5363
Target: Akt, PKA, mTOR, Autophagy
3CAI
Cat.No: T14034
Synonym:
Target: Akt
Afuresertib
Cat.No: T1911
Synonym: GSK2110183C,GSK2110183
Target: ROCK, Akt, PKC
Ipatasertib
Cat.No: T6252
Synonym: GDC-0068,RG7440,帕他色替
Target: Akt
AKT inhibitor VIII
Cat.No: T3346
Synonym: AKTi-1/2
Target: Apoptosis, Akt
SAFit2
Cat.No: T16836
Synonym:
Target: FKBP
AT7867
Cat.No: T6304
Synonym:
Target: Akt, PKA, S6 Kinase
Uprosertib
Cat.No: T6849
Synonym: GSK2141795,GSK795,优普色替
Target: Akt
AT13148
Cat.No: T2482
Synonym:
Target: ROCK, SGK, Akt, PKA, S6 Kinase
GSK-690693
Cat.No: T6285
Synonym: GSK690693
Target: Serine Protease, Akt, PKC, AMPK, Autophagy
CCT128930
Cat.No: T6303
Synonym:
Target: Akt, PKA, S6 Kinase, Autophagy
INY-03-041
Cat.No: T11664
Synonym:
Target: Others
Uprosertib hydrochloride
Cat.No: T15428
Synonym: GSK2141795 (hydrochloride)
Target: Others
AKT-IN-5
Cat.No: T61680
Synonym:
Target:
AKT-IN-3
Cat.No: T10275
Synonym:
Target: Akt
MS98
Cat.No: T39930
Synonym:
Target:
Merck-22-6
Cat.No: T25791
Synonym: Merck 22 6,Merck226
Target:
MS15
Cat.No: T74983
Synonym:
Target:
AKT-IN-8
Cat.No: T62842
Synonym:
Target:
Hu7691
Cat.No: T39899
Synonym:
Target: Akt
AKT-IN-13
Cat.No: T63039
Synonym:
Target:
MS170
Cat.No: T39928
Synonym:
Target:
INY-03-041 trihydrochloride
Cat.No: T74001
Synonym:
Target:
AT7867 dihydrochloride
Cat.No: T21624
Synonym:
Target:
Vevorisertib
Cat.No: T38847
Synonym: Vevorisertib,ARQ 751
Target:
NTQ1062
Cat.No: T63200
Synonym:
Target:
MS15 TFA
Cat.No: T77968
Synonym:
Target: PROTACs
MK-2206 free base
Cat.No: T81784
Synonym:
Target: Akt
MK-2206
Cat.No: T62609
Synonym:
Target:
ALM301
Cat.No: T62149
Synonym:
Target:
TAS-117 hydrochloride
Cat.No: T62907
Synonym:
Target:
CCT128930 hydrochloride
Cat.No: T6303L
Synonym: CCT128930 hydrochloride(885499-61-6 Free base)
Target: Apoptosis, Akt, PKA, mTOR, Autophagy
9-Decyn-1-ol
Cat.No: T17346
Synonym:
Target: Others
Miransertib (ARQ 092) HCl
Cat.No: T22247
Synonym:
Target:
Lenalidomide-C9-aldehyde
Cat.No: T18065
Synonym:
Target: Others
(+)-Tetrabenazine
Cat.No: T13134
Synonym: (+)-TBZ,(3R,11bR)-Tetrabenazine,(3R,11bR)-TBZ
Target: Monoamine Transporter
TAS-117
Cat.No: T28923
Synonym: TAS117,TAS 117
Target:
GSK269962A hydrochloride
Cat.No: T39519
Synonym: GSK 269962 hydrochloride
Target:
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。

天然产物

Oridonin
Cat.No: T2790
Synonym: NSC-250682,Rubescenin,冬凌草甲素,Isodonol,Rubescensin A
Target: Akt, Antibacterial
TargetMol Loading
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