|
T74982 |
Akt3 degrader 1
|
|
|
|
Akt3 Degrader 1 (compound 12l), a selective Akt3 degrader, effectively overcomes Osimertinib-induced resistance in H1975OR NSCLC cells. Besides its role in overcoming drug resistance, it exhibits anti-proliferative prope... |
|
T3467 |
Miransertib
|
ARQ-092,AKT inhibitor 2 |
Akt
,
Parasite
|
|
Miransertib (ARQ-092) is an orally bioavailable, selective, and potent allosteric Akt inhibitor. |
|
T11928 |
M2698
|
MSC2363318A |
Akt
,
mTOR
|
|
M2698 (MSC2363318A) is an inhibitor of p70S6K, Akt1 and Akt3 with IC50s of 1 nM. M2698 shows anti-cancer activity. |
|
T15374 |
Ipatasertib dihydrochloride
|
GDC-0068 dihydrochloride,RG-7440 dihydrochloride |
Akt
,
PKA
|
|
Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) is a highly selective and ATP-competitive inhibitor of pan-Akt (IC50s: 5, 18 and 8 nM for Akt1, Akt2 and Akt3, respectively). |
|
T14072 |
A-443654
|
|
ERK
,
VEGFR
,
GSK-3
,
FLT
,
Casein Kinase
,
MAPK
,
Akt
,
PKA
,
Chk
,
CDK
,
Src
,
PKC
,
S6 Kinase
|
|
A-443654 is a pan-Akt inhibitor. A-443654 has equal potency against Akt1, Akt2, or Akt3 within cells (Ki=160 pM). |
|
T38846 |
Vevorisertib trihydrochloride
|
ARQ 751 trihydrochloride |
Akt
|
|
Vevorisertib trihydrochloride (ARQ 751 trihydrochloride) is a selective and potent inhibitor of pan-AKT and AKT1-E17K mutations, inhibiting AKT1, AKT2 and AKT3. Vevorisertib trihydrochloride is used in the study of hepat... |
|
T7885 |
Afuresertib hydrochloride
|
|
ROCK
,
Akt
,
PKC
|
|
Afuresertib hydrochloride is an inhibitor of Akt kinase (Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3 respectively) |
|
T39733 |
Hu7691 free base
|
|
Akt
|
|
Hu7691 free base is an orally active, potent and selective Akt inhibitor with anti-proliferative and neurogenic effects on a variety of neuroblastoma cell lines.Hu7691 free base inhibits Akt1, Akt2, and Akt3 and induces ... |
|
T1952 |
MK-2206 dihydrochloride
|
MK-2206 2HCl |
Apoptosis
,
Akt
,
Autophagy
|
|
MK-2206 dihydrochloride (MK-2206 2HCl) is a variant Akt inhibitor that inhibits Akt1, Akt2, and Akt3 (IC50=8/12/65 nM) with orally active, highly potent and selective potency. MK-2206 dihydrochloride exhibits antitumor a... |
|
T1920 |
Capivasertib
|
AZD5363 |
Akt
,
PKA
,
mTOR
,
Autophagy
|
|
Capivasertib (AZD5363) is a broad-spectrum AKT inhibitor with inhibitory activity against Akt1, Akt2, and Akt3 (IC50=3/7/7 nM) with oral activity. Capivasertib has antitumor activity for the treatment of breast cancer. |
|
T3346 |
AKT inhibitor VIII
|
AKTi-1/2 |
Apoptosis
,
Akt
|
|
AKT inhibitor VIII (AKTi-1/2) is a highly specific Akt1/2 inhibitor (IC50: 58/210 nM). The selectivity for Akt1 is higher about 36-fold than Akt3. |
|
T1911 |
Afuresertib
|
GSK2110183C,GSK2110183 |
ROCK
,
Akt
,
PKC
|
|
Afuresertib (GSK2110183) is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. |
|
T6252 |
Ipatasertib
|
GDC-0068,RG7440 |
Akt
|
|
Ipatasertib (GDC-0068) (GDC-0068), a highly specific pan-Akt inhibitor, targets Akt1/2/3 with IC50 of 5 nM/18 nM/8 nM, respectively. |
|
T6849 |
Uprosertib
|
GSK2141795,GSK795 |
Akt
|
|
Uprosertib (GSK2141795) (GSK2141795) is a selective, ATP-competitive, and orally bioavailable Akt inhibitor with IC50 of 180 nM, 328 nM, and 38 nM for Akt 1, 2 and 3, respectively. Phase 2. |
|
T6304 |
AT7867
|
|
Akt
,
PKA
,
S6 Kinase
|
|
AT7867 is a potent ATP-competitive inhibitor of Akt1/2/3 and p70S6K/PKA with IC50 of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively; little activity outside the AGC kinase family. |
|
T6285 |
GSK-690693
|
GSK690693 |
Serine Protease
,
Akt
,
PKC
,
AMPK
,
Autophagy
|
|
GSK-690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. Phase 1. |
|
T2482 |
AT13148
|
|
ROCK
,
SGK
,
Akt
,
PKA
,
S6 Kinase
|
|
AT13148 is an oral-active and ATP-competitive, multi-AGC kinase inhibitor for Akt1/2/3, p70S6K, PKA, and ROCKI/II. |
|
T15428 |
Uprosertib hydrochloride
|
GSK2141795 (hydrochloride) |
Others
|
|
Uprosertib hydrochloride is a potent and selective inhibitor of pan-Akt (IC50: 180/328/38 nM for Akt1/Akt2/Akt3, respectively). |
|
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... |
|
T11664 |
INY-03-041
|
|
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 G... |
|
T39899 |
Hu7691
|
|
Akt
|
|
Hu7691 is an orally active, selective and potent Akt inhibitor that inhibits Akt1, Akt2 and Akt3, inhibits proliferation of neuroblastoma cells and induces differentiation of neuroblastoma cells. |
|
T63039 |
AKT-IN-13
|
|
|
|
AKT-IN-13 (compound 4b) is a potent inhibitor of Akt, acting on Akt1 (IC50: 1.6 nM), Akt2 (IC50: 2.4 nM) and Akt3 (IC50: 0.3 nM). AKT-IN-13 can be used in anticancer research. |
|
T10275 |
AKT-IN-3
|
|
Akt
|
|
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 kin... |
|
T62842 |
AKT-IN-8
|
|
|
|
AKT-IN-8 is a potent inhibitor of AKT, acting on AKT1 (IC50: 4.46 nM), AKT2 (IC50: 2.44 nM) and AKT3 (IC50: 9.47 nM). |
|
T74983 |
MS15
|
|
|
|
MS15 is a potent, selective degrader of AKT PROTAC, effectively inhibiting activities of AKT1, AKT2, and AKT3. It exhibits IC50 values of 798 nM for AKT1, 90 nM for AKT2, and 544 nM for AKT3, respectively [1]. |
|
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 de... |
|
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 ... |
|
T21624 |
AT7867 dihydrochloride
|
|
|
|
AT7867 dihydrochloride is a potent ATP-competitive inhibitor of Akt1 / Akt2 / Akt3 and p70S6K / PKA kinase with IC 50 s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively. AT7867 dihydrochloride is able to induce pharmac... |
|
T74001 |
INY-03-041 trihydrochloride
|
|
|
|
INY-03-041 trihydrochloride, a potent and highly selective PROTAC-based pan-AKT degrader, comprises Ipatasertib, an ATP-competitive AKT inhibitor, conjugated to Lenalidomide. It effectively inhibits AKT1, AKT2, and AKT3 ... |
|
T77968 |
MS15 TFA
|
|
PROTACs
|
|
MS15 TFA is a potent, selective AKT PROTAC degrader, effectively inhibiting AKT1, AKT2, and AKT3 with IC50 values of 798 nM, 90 nM, and 544 nM, respectively [1]. |
|
T62609 |
MK-2206
|
|
|
|
MK-2206 is an orally active, highly selective, metabotropic Akt inhibitor that acts on Akt1 (IC50: 8 nM), Akt2 (IC50: 12 nM) and Akt3 (IC50: 65 nM). Many breast cancer cell lines, PIK3CA mutants and PTEN-losing cell line... |
|
T62149 |
ALM301
|
|
|
|
ALM301 is a highly specific, orally active AKT inhibitor that acts on AKT1 (IC50: 0.13 μM), AKT2 (IC50: 0.09 μM) and AKT3 (IC50: 2.75 μM). ALM301 inhibits AKT phosphorylation in vitro and has a regulatory effect on downs... |
|
T62907 |
TAS-117 hydrochloride
|
|
|
|
TAS-117 hydrochloride is a selective, potent, orally active allosteric Akt inhibitor, acting on Akt1 (IC50: 4.8 nM), Akt2 (IC50: 1.6 nM) and Akt3 (IC50: 44 nM). TAS-117 hydrochloride stimulates anti-myeloma activity, enh... |
|
T81784 |
MK-2206 free base
|
|
Akt
|
|
MK-2206 free base is an allosteric Akt inhibitor that is both potent and selective, administered orally, exhibiting IC50 values of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. It demonstrates sensitivity in ... |
|
T63200 |
NTQ1062
|
|
|
|
NTQ1062 (compound 22b) is an orally active and potent Akt inhibitor that acts on Akt1 (IC50: 0.4 nM), Akt2 (IC50: 6.3 nM) and Akt3 (IC50: 0.1 nM). NTQ1062 showed significant anti-tumor effects in the LNCap xenograft tumo... |
|
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, ... |
|
T17346 |
9-Decyn-1-ol
|
|
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 poten... |
|
T18065 |
Lenalidomide-C9-aldehyde
|
|
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 PROT... |
|
T13134 |
(+)-Tetrabenazine
|
(+)-TBZ,(3R,11bR)-Tetrabenazine,(3R,11bR)-TBZ |
Monoamine Transporter
|
|
(+)-Tetrabenazine ((3R,11bR)-Tetrabenazine) is a reversible vesicular monoamine transporter 2 (VMAT-2) inhibitor, inhibits transport by VMAT2 with 10-fold greater potency than transport by VMAT1. |
|
T7315 |
BAY1125976
|
|
Akt
|
|
BAY1125976 is an allosteric inhibitor of Akt1 and Akt2 (IC50s of 5.2 and 18 nM, respectively, in a time-resolved FRET assay) |
|
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-inf... |
