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Akt1 Inhibitors

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By Targets:	Akt (54) AMPK (1) Apoptosis (12) Autophagy (9) Bacterial (1) Bcr-Abl (1) CaMK (1) Caspase (2) CDK (2) FXR (1) Insulin Receptor (1) JNK (1) MDM-2/p53 (1) Microtubule/Tubulin (1) mTOR (1) Organoid (5) Parasite (2) PDK-1 (1) Phosphatase (1) PI3K (1) PKA (6) PKC (4) PROTAC Linkers (1) PROTACs (4) PTEN (1) Ribosomal S6 Kinase (RSK) (5) ROCK (5) Ser/Thr Protease (1) SGK (2) SphK (2)
By Research Areas:	Cancer (57) Infection (3) Inflammation/Immunology (3) Metabolic Disease (3) Neurological Disease (1)
Click Chemistry:	PROTAC Synthesis (1) Alkynes (1)

Inhibitors & Agonists

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-146459

Akt1-IN-1	Akt	Cancer
Akt1-IN-1 (compound 5b) is a potent and selective *Akt1* inhibitor with an IC₅₀ value of 18.79 nM in MIA Paca-2 cells. Akt1-IN-1 does not exhibit obvious teratogenicity, hepatotoxicity and cardiotoxicity (No Observed Adverse Effect Level > 100 µM). Akt1-IN-1 can be used for researching anticancer .

HY-100018

BAY1125976

Akt Cancer

BAY1125976 is a selective allosteric Akt1/Akt2 inhibitor; inhibits Akt1 and Akt2 activity with IC₅₀ values of 5.2 nM and 18 nM at 10 μM ATP, respectively.

BAY1125976	Akt	Cancer
BAY1125976 is a selective allosteric *Akt1/Akt2* inhibitor; inhibits Akt1 and Akt2 activity with IC₅₀ values of 5.2 nM and 18 nM at 10 μM ATP, respectively.

HY-137458A

Vevorisertib trihydrochloride ARQ 751 trihydrochloride	Akt	Cancer
Vevorisertib (ARQ 751) trihydrochloride is a selective, allosteric, pan-AKT and AKT1-E17K mutant inhibitors. Vevorisertib trihydrochloride potently inhibit phosphorylation of AKT. Vevorisertib trihydrochloride has Kd values of 1.2 nM and 8.6 nM for AKT1 and AKT1-E17K, respectively. Vevorisertib trihydrochloride has IC₅₀ values of 0.55, 0.81, and 1.3 nM for AKT1, AKT2, and AKT3, respectively. Vevorisertib trihydrochloride can be used for the research of cancer .

HY-129119

Akt1/Akt2-IN-2	Akt Caspase	Cancer
Akt1/Akt2-IN-2 (compound 7) is an allosteric dual *Akt1* and Akt2 inhibitor (IC₅₀=138 nM and 212 nM, respectively). Akt1/Akt2-IN-2 increases activity of caspase-3, and inhibits viability of a number of tumor cells .

HY-148868A

Akt1&PKA-IN-2	Akt CDK	Cancer
Akt1&PKA-IN-2 ((R)-29) is an inhibitor of PKB/AKT with cyclin-dependent kinase 2 (CDK2) selectivity. Akt1&PKA-IN-2 inhibits AKT1, PKAa and CDK2 ^a with IC₅₀ values of 0.007 µM, 0.01 µM and 0.69 µM, respectively .

HY-50862

Akt1/Akt2-IN-1

Akt Cancer

Akt1/Akt2-IN-1 (Compound 17) is an allosteric inhibitor of Akt1 (IC₅₀=3.5 nM) and Akt2 (IC₅₀=42 nM), with potent and balanced activity .
HY-16666

3CAI

2 Publications Verification

Akt Cancer

3CAI is a potent and specific AKT1 and AKT2 inhibitor.
HY-13254A

A-674563 hydrochloride

4 Publications Verification

Akt Cancer

A-674563 hydrochloride is a potent and selective Akt1 inhibitor with K_i of 11 nM.
HY-13254

A-674563

4 Publications Verification

Akt Cancer

A-674563 is an orally active and selective Akt1 inhibitor with a K_i of 11 nM.

Akt1/Akt2-IN-1	Akt	Cancer
Akt1/Akt2-IN-1 (Compound 17) is an allosteric inhibitor of *Akt1* (IC₅₀=3.5 nM) and Akt2 (IC₅₀=42 nM), with potent and balanced activity .

3CAI 2 Publications Verification	Akt	Cancer
3CAI is a potent and specific *AKT1* and AKT2 inhibitor.

A-674563 hydrochloride 4 Publications Verification	Akt	Cancer
A-674563 hydrochloride is a potent and selective *Akt1* inhibitor with K_i of 11 nM.

A-674563 4 Publications Verification	Akt	Cancer
A-674563 is an orally active and selective *Akt1* inhibitor with a K_i of 11 nM.

HY-148868

Akt1&PKA-IN-1	Akt PKA CDK	Others
Akt1&PKA-IN-1 is a potent dual Akt/PKA inhibitor with IC₅₀ values of 0.03 , 0.11 μM, and 9.8 μM for PKAa, Akt, and CDK2, respectively. Akt1&PKA-IN-1 is selective for cyclin-dependent kinase 2 (CDK2) .

HY-16032

Akt1-IN-2

Akt Cancer

AKT-I-1 is a selective inhibitor of Akt1, with an IC₅₀ of 4.6 µM .
HY-112148

AKT-IN-2

Akt Cancer

AKT-IN-2 is a potent, selective and orally bioavailable AKT inhibitor with an IC₅₀ of 5 nM for AKT1 .

Akt1-IN-2	Akt	Cancer
AKT-I-1 is a selective inhibitor of *Akt1, with an IC₅₀* of 4.6 µM .

AKT-IN-2	Akt	Cancer
AKT-IN-2 is a potent, selective and orally bioavailable AKT inhibitor with an IC₅₀ of 5 nM for *AKT1* .

HY-154960

Tubulin/AKT1-IN-1	Akt Apoptosis Microtubule/Tubulin	Cancer
Tubulin/AKT1-IN-1 (Compound D1-1) is an inhibitor of tubulin polymerization and AKT pathway activation. Tubulin/AKT1-IN-1 significantly inhibits the proliferation and metastasis of H1975 cells and slightly induced their apoptosis and can be used for non-small-cell lung cancer (NSCLC) research .

HY-138767

AKT-IN-5

Akt Cancer

AKT-IN-5 (Example 8) is a Akt inhibitor with IC₅₀ values of 450 nM and 400 nM for Akt1 and Akt2, respectively .

AKT-IN-5	Akt	Cancer
AKT-IN-5 (Example 8) is a Akt inhibitor with IC₅₀ values of 450 nM and 400 nM for *Akt1* and Akt2, respectively .

HY-15431

Capivasertib 45+ Cited Publications AZD5363	Akt Autophagy	Cancer
Capivasertib (AZD5363) is an orally active and potent pan-AKT kinase inhibitor with IC₅₀ of 3, 7 and 7 nM for *Akt1,Akt2* and Akt3, respectively.

HY-15965

Uprosertib 15+ Cited Publications GSK2141795	Akt	Cancer
Uprosertib (GSK2141795) is a potent and selective pan-Akt inhibitor with IC₅₀ values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively.

HY-15965A

Uprosertib hydrochloride GSK2141795 (hydrochloride)	Akt	Cancer
Uprosertib hydrochloride (GSK2141795 hydrochloride) is a potent and selective pan-Akt inhibitor with IC₅₀ values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively.

HY-19719

Miransertib 5+ Cited Publications ARQ-092	Akt Parasite	Infection Cancer
Miransertib (ARQ-092) is a potent, orally active, selective and allosteric Akt inhibitor with IC₅₀s of 2.7 nM, 14 nM and 8.1 nM for *Akt1, Akt2, Akt3, respectively. Miransertib is also a potent the AKT1-E17K mutant protein inhibitor* and has the potential for PI3K/AKT-driven tumors and Proteus syndrome research . Miransertib is effective against *Leishmania* .

HY-19719A

Miransertib hydrochloride 5+ Cited Publications ARQ-092 hydrochloride	Akt Parasite	Infection Cancer
Miransertib hydrochloride (ARQ-092 hydrochloride) is a potent, orally active, selective and allosteric Akt inhibitor with IC₅₀s of 2.7 nM, 14 nM and 8.1 nM for *Akt1, Akt2, Akt3, respectively. Miransertib hydrochloride is also a potent the AKT1-E17K mutant protein inhibitor* and has the potential for PI3K/AKT-driven tumors and Proteus syndrome research . Miransertib hydrochloride is effective against *Leishmania* .

HY-18271

CaMKII-IN-1 2 Publications Verification	CaMK Autophagy	Inflammation/Immunology
CaMKII-IN-1 is a potent and highly selective CaMKII inhibitor with IC50 of 63 nM; significantly high selectivity against CaMKIV, MLCK, p38a, Akt1, and PKC.

HY-151613

MS15	PROTACs Akt	Cancer
MS15 is a potent and selective AKT PROTAC degrader. MS15 inhibits the AKT1, -2, and -3 activities, with IC₅₀ values of 798 nM, 90 nM, and 544 nM, respectively .

HY-10425

A-443654

5+ Cited Publications

Akt Cancer

A-443654 is a pan-Akt inhibitor and has equal potency against Akt1, Akt2, or Akt3 within cells (K_i=160 pM) .
HY-143611

AKT-IN-8

Akt Cancer

AKT-IN-8 is a potent AKT inhibitor with IC₅₀s of 4.46, 2.44, and 9.47 nM for AKT1, AKT2, and AKT3, respectively .

A-443654 5+ Cited Publications	Akt	Cancer
A-443654 is a pan-Akt inhibitor and has equal potency against *Akt1, Akt2, or Akt3* within cells (K_i=160 pM) .

AKT-IN-8	Akt	Cancer
AKT-IN-8 is a potent AKT inhibitor with IC₅₀s of 4.46, 2.44, and 9.47 nM for AKT1, AKT2, and AKT3, respectively .

HY-15186A

Ipatasertib dihydrochloride 30+ Cited Publications GDC-0068 dihydrochloride; RG-7440 dihydrochloride	Organoid Akt	Cancer
Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) is a highly selective and ATP-competitive pan-Akt inhibitor with IC₅₀s of 5, 18 and 8 nM for *Akt1, Akt2* and Akt3, respectively.

HY-151613A

MS15 TFA	PROTACs Akt	Cancer
MS15 TFA is a potent and selective AKT PROTAC degrader. MS15 TFA inhibits the AKT1, -2, and -3 activities, with IC₅₀ values of 798 nM, 90 nM, and 544 nM, respectively .

HY-123390

DB07107

Bcr-Abl Akt Cancer

DB07107 is a potent agent resistant T315I mutant Bcr-Abl tyrosine kinase inhibitor. DB07107 is also a potent Akt1 inhibitor with an IC₅₀ value of 360 nM .

DB07107	Bcr-Abl Akt	Cancer
DB07107 is a potent agent resistant T315I mutant Bcr-Abl tyrosine kinase inhibitor. DB07107 is also a potent *Akt1* inhibitor with an IC₅₀ value of 360 nM .

HY-15727

Afuresertib 10+ Cited Publications GSK2110183; LAE002	Akt PKC ROCK	Cancer
Afuresertib (GSK2110183) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with K_is of 0.08/2/2.6 nM for Akt1/Akt2/Akt3, respectively .

HY-15727A

Afuresertib hydrochloride 10+ Cited Publications GSK2110183 hydrochloride; LAE002 hydrochloride	Akt PKC ROCK	Cancer
Afuresertib hydrochloride (GSK 2110183 hydrochloride) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with K_is of 0.08/2/2.6 nM for Akt1/Akt2/Akt3 respectively .

HY-19982

AKT-IN-6

AKT-IN-6 (Example 13) is a potent Akt inhibitor. AKT-IN-6 inhibits Akt1, Akt2 and Akt3 with IC₅₀s < 500nM, respectively. (patent WO2013056015A1).

AKT-IN-6
AKT-IN-6 (Example 13) is a potent Akt inhibitor. AKT-IN-6 inhibits Akt1, Akt2 and Akt3 with IC₅₀s < 500nM, respectively. (patent WO2013056015A1).

HY-10355

AKT inhibitor VIII 35+ Cited Publications Akti-1/2	Akt Apoptosis	Metabolic Disease Cancer
AKT inhibitor VIII (AKTi-1/2) is a cell-permeable quinoxaline compound that has been shown to potently, selectively, allosterically, and reversibly inhibit *Akt1, Akt2, and Akt3* activity with IC₅₀s of 58 nM, 210 nM, and 2119 nM, respectively.

HY-132302

Hu7691	Akt PKA PKC ROCK Ribosomal S6 Kinase (RSK) SGK	Cancer
Hu7691 is an orally active, selective Akt inhibitor with IC₅₀s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 inhibits tumor growth and enables decrease of cutaneous toxicity in mice .

HY-12059

AT7867 4 Publications Verification	Akt PKA Ribosomal S6 Kinase (RSK)	Cancer
AT7867 is a potent ATP-competitive inhibitor of *Akt1/Akt2/Akt3* and p70S6K/PKA with IC₅₀s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively.

HY-12059A

AT7867 dihydrochloride 4 Publications Verification	Akt PKA Ribosomal S6 Kinase (RSK)	Cancer
AT7867 dihydrochloride is a potent ATP-competitive inhibitor of *Akt1/Akt2/Akt3* and p70S6K/PKA with IC₅₀s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively.

HY-N0004

Oridonin 15+ Cited Publications NSC-250682; Isodonol	Akt Bacterial	Infection Inflammation/Immunology Cancer
Oridonin (NSC-250682), a diterpenoid isolated from Rabdosia rubescens, acts as an inhibitor of AKT, with IC₅₀s of 8.4 and 8.9 μM for AKT1 and AKT2; Oridonin possesses anti-tumor, anti-bacterial and anti-inflammatory effects.

HY-147937

AKT-IN-13	Akt	Cancer
AKT-IN-13 (compound 4b) is a potent Akt inhibitor with IC₅₀s of 1.6 nM, 2.4 nM and 0.3 nM for Akt1, Akt2 and Akt3, respectively. AKT-IN-13 can be used for researching anticancer .

HY-10358

MK-2206 dihydrochloride Maximum Cited Publications 286 Publications Verification MK-2206 (2HCl)	Organoid Akt Autophagy Apoptosis	Cancer
MK-2206 dihydrochloride (MK-2206 (2HCl)) is an orally active, BBB-penetrated allosteric AKT inhibitor with IC₅₀s of 5 nM, 12 nM, and 65 nM for *AKT1, AKT2, and AKT3, respectively. MK-2206 dihydrochloride induces autophagy* .

HY-132302A

Hu7691 free base	Akt PKA PKC ROCK Ribosomal S6 Kinase (RSK) SGK	Cancer
Hu7691 free base is an orally active, selective Akt inhibitor with IC₅₀s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 free base inhibits tumor growth and enables decrease of cutaneous toxicity in mice .

HY-N8122

24-Methylenecycloartanyl ferulate	Akt	Cancer
24-Methylenecycloartanyl ferulate is a γ-oryzanol compound. 24-Methylenecycloartanyl ferulate promotes parvin-beta expression in human breast cancer cells. 24-Methylenecycloartanyl ferulate is a potential ATP-competitive *Akt1* inhibitor (EC₅₀= 33.3μM) .

HY-16071

AT13148 2 Publications Verification	Akt PKA ROCK Ribosomal S6 Kinase (RSK)	Cancer
AT13148 is an orally active and ATP-competitive, multi-AGC kinase inhibitor with IC₅₀s of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively.

HY-151504

ALM301 1 Publications Verification	Akt	Cancer
ALM301 is an orally active highly specific AKT inhibitor with IC₅₀ values of 0.13 µM, 0.09 µM and 2.75 µM for AKT1, AKT2 and AKT3, respectively. ALM301 inhibits AKT phosphorylation and modulates downstream signalling in vitro. ALM301 can inhibit cancer cell proliferation and tumor growth .

HY-100501

M2698 MSC2363318A
M2698 (MSC2363318A) is an orally active, ATP competitive, selective p70S6K and Akt dual-inhibitor with IC₅₀s of 1 nM for p70S6K, Akt1 and Akt3. M2698 can cross the blood-brain barrier and has anti-cancer activity .

HY-19934A

Pifusertib hydrochloride TAS-117 hydrochloride	Akt Apoptosis Autophagy	Cancer
Pifusertib (TAS-117) hydrochloride is a potent, selective, orally active allosteric Akt inhibitor (with IC₅₀s of 4.8, 1.6, and 44 nM for Akt1, 2, and 3, respectively). Pifusertib hydrochloride triggers anti-myeloma activities and enhances fatal endoplasmic reticulum (ER) stress induced by proteasome inhibition. Pifusertib hydrochloride induces apoptosis and autophagy .

HY-19934

Pifusertib TAS-117	Akt Apoptosis Autophagy	Cancer
Pifusertib (TAS-117) is a potent, selective, orally active allosteric Akt inhibitor (with IC₅₀s of 4.8, 1.6, and 44 nM for Akt1, 2, and 3, respectively). Pifusertib triggers anti-myeloma activities and enhances fatal endoplasmic reticulum (ER) stress induced by proteasome inhibition. Pifusertib induces apoptosis and autophagy .

HY-10249

GSK-690693 25+ Cited Publications	Akt AMPK Autophagy	Cancer
GSK-690693 is an ATP-competitive pan-Akt inhibitor with IC₅₀s of 2 nM, 13 nM, 9 nM for *Akt1, Akt2* and Akt3, respectively. GSK-690693 is also an AMPK inhibitor, affects Unc-51-like autophagy activating kinase 1 (ULK1) activity and robustly inhibits STING-dependent IRF3 activation .

HY-133120

INY-03-041	PROTACs Akt	Cancer
INY-03-041 is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor Ipatasertib (HY-15186) conjugated to Lenalidomide (HY-A0003, Cereblon ligand). INY-03-041 inhibits *AKT1, AKT2* and AKT3 with IC₅₀s of 2.0, 6.8 and 3.5 nM, respectively .

HY-133120A

INY-03-041 trihydrochloride	PROTACs Akt	Cancer
INY-03-041 trihydrochloride is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor Ipatasertib (HY-15186) conjugated to Lenalidomide (HY-A0003, Cereblon ligand). INY-03-041 trihydrochloride inhibits *AKT1, AKT2* and AKT3 with IC₅₀s of 2.0, 6.8 and 3.5 nM, respectively .

HY-108232

MK-2206	Organoid Akt Autophagy Apoptosis	Cancer
MK-2206 is an orally active, highly potent and selective allosteric Akt inhibitor, with IC₅₀s of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. Many breast cancer cell lines, and PIK3CA-mutant and cell lines with PTEN loss are sensitive to MK-2206. MK-2206 has anticancer activities .

HY-15186

Ipatasertib 30+ Cited Publications GDC-0068; RG7440	Organoid Akt Apoptosis	Cancer
Ipatasertib (GDC-0068) is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC₅₀ values of 5, 18, 8 nM for *Akt1/2/3, respectively. Ipatasertib synchronously activates FoxO3a and NF-κB through inhibition of Akt* leading to p53-independent activation of PUMA. Ipatasertib also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models .

HY-119016

SK1-I 1 Publications Verification BML-258	SphK	Cancer
SK1-I (BML-258), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a K_i value of 10 µM . SK1-I shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I enhances autophagy and has antitumor activity .

HY-119016A

SK1-I hydrochloride 1 Publications Verification BML-258 hydrochloride	SphK	Cancer
SK1-I hydrochloride (BML-258 hydrochloride), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a K_i value of 10 µM . SK1-I hydrochloride shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I hydrochloride enhances autophagy and has antitumor activity .

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Akt1 Inhibitors

Inhibitors & Agonists

Screening Libraries

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Click Chemistry

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