Search Result

Pathways Recommended:	PI3K/Akt/mTOR

Results for "

AKT Kinase Inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (35) Ack1 (2) AMPK (3) Anaplastic lymphoma kinase (ALK) (1) Apoptosis (24) Aurora Kinase (3) Autophagy (9) Bcl-2 Family (1) Bcr-Abl (2) c-Kit (3) c-Met/HGFR (5) Casein Kinase (1) Caspase (2) CDK (4) EGFR (5) ERK (2) FAK (1) FGFR (1) FLT3 (1) Formyl Peptide Receptor (FPR) (1) IGF-1R (1) Integrin (1) Isotope-Labeled Compounds (1) JNK (2) mTOR (2) Myosin (2) NF-κB (1) NO Synthase (1) p38 MAPK (1) Parasite (1) PARP (2) PDGFR (2) PDK-1 (1) Phosphodiesterase (PDE) (1) PI3K (4) Pim (1) PKA (4) PKC (5) Polo-like Kinase (PLK) (2) Reactive Oxygen Species (1) RET (1) Ribosomal S6 Kinase (RSK) (1) ROCK (3) ROR (1) ROS Kinase (1) Ser/Thr Protease (1) SphK (1) Src (4) STAT (3) Syk (1) VEGFR (2) Wnt (1)
By Research Areas:	Cancer (57) Inflammation/Immunology (6) Metabolic Disease (3)

By Targets:

Akt (35)

Ack1 (2)

AMPK (3)

Anaplastic lymphoma kinase (ALK) (1)

Apoptosis (24)

Aurora Kinase (3)

Autophagy (9)

Bcl-2 Family (1)

Bcr-Abl (2)

c-Kit (3)

c-Met/HGFR (5)

Casein Kinase (1)

Caspase (2)

CDK (4)

EGFR (5)

ERK (2)

FAK (1)

FGFR (1)

FLT3 (1)

Formyl Peptide Receptor (FPR) (1)

IGF-1R (1)

Integrin (1)

Isotope-Labeled Compounds (1)

JNK (2)

mTOR (2)

Myosin (2)

NF-κB (1)

NO Synthase (1)

p38 MAPK (1)

Parasite (1)

PARP (2)

PDGFR (2)

PDK-1 (1)

Phosphodiesterase (PDE) (1)

PI3K (4)

Pim (1)

PKA (4)

PKC (5)

Polo-like Kinase (PLK) (2)

Reactive Oxygen Species (1)

RET (1)

Ribosomal S6 Kinase (RSK) (1)

ROCK (3)

ROR (1)

ROS Kinase (1)

Ser/Thr Protease (1)

SphK (1)

Src (4)

STAT (3)

Syk (1)

VEGFR (2)

Wnt (1)

By Research Areas:

Cancer (57)

Inflammation/Immunology (6)

Metabolic Disease (3)

Inhibitors & Agonists

Screening Libraries

Biochemical Assay Reagents

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Akt

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-10249A

AKT Kinase Inhibitor

10+ Cited Publications

Akt Cancer

AKT Kinase Inhibitor is an Akt kinase inhibitor with anti-tumor activity .

**AKT Kinase Inhibitor** 10+ Cited Publications	Akt	Cancer
AKT Kinase Inhibitor is an *Akt* kinase inhibitor with anti-tumor activity .

HY-10249D

AKT Kinase Inhibitor hydrochloride 10+ Cited Publications	Akt	Cancer
AKT Kinase Inhibitor hydrochloride is an *Akt* kinase inhibitor with anti-tumor activity . AKT Kinase Inhibitor (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-10721

PF-AKT400 AKT protein Kinase Inhibitor	Akt	Cancer
PF-AKT400 is a broadly selective, potent, ATP-competitive Akt inhibitor, displays 900-fold greater selectivity for PKBα (IC₅₀=0.5 nM) than PKA (IC₅₀=450 nM).

HY-15431

Capivasertib Maximum Cited Publications 46 Publications Verification 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-133850

10-DEBC

Pim Cancer

10-DEBC is a selective Akt inhibitor. 10-DEBC shows strong inhibitory activity against Moloney murine leukemia virus (Pim) kinase-1 (IC₅₀=1.28 μM) .

10-DEBC	Pim	Cancer
10-DEBC is a selective Akt inhibitor. 10-DEBC shows strong inhibitory activity against Moloney murine leukemia virus (Pim) kinase-1 (IC₅₀=1.28 μM) .

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-122913

Borussertib

Akt Cancer

Borussertib is a covalent-allosteric and first-in-class inhibitor of protein kinase Akt, with an IC₅₀ of 0.8 nM and a K_i of 2.2 nM for Akt ^wt .

Borussertib	Akt	Cancer
Borussertib is a covalent-allosteric and first-in-class inhibitor of protein kinase *Akt, with an IC₅₀* of 0.8 nM and a K_i of 2.2 nM for Akt ^wt .

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-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-147513

AKT-IN-12	Akt Apoptosis	Cancer
AKT-IN-12 (compound 3e) is a potent **Akt kinase** inhibitor with an IC₅₀ value of 0.55 μM. AKT-IN-12 induces G0/G1 cell cycle arrest and apoptosis. AKT-IN-12 also inhibits p-AKT, p-ERK, and activates p-JNK, JNK. AKT-IN-12 can be used for researching leukemia .

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-144059

AKT-IN-9	Akt	Cancer
AKT-IN-9 is a potent inhibitor of *AKT. Protein kinase* B (PKB, also known as AKT) is central to PI3K/AKT/mTOR signaling in cells, and its function is important for cell growth, survival, differentiation and metabolism. AKT-IN-9 has the potential for the research of breast and prostate cancer (extracted from patent WO2021185238A1, compound 1) .

HY-144060

AKT-IN-10	Akt	Cancer
AKT-IN-10 is a potent inhibitor of *AKT. Protein kinase* B (PKB, also known as AKT) is central to PI3K/AKT/mTOR signaling in cells, and its function is important for cell growth, survival, differentiation and metabolism. AKT-IN-10 has the potential for the research of breast and prostate cancer (extracted from patent WO2021185238A1, compound 4) .

HY-126257

AKT-IN-3	Akt Apoptosis	Cancer
AKT-IN-3 (compound E22) is a potent, orally active low hERG blocking *Akt* inhibitor, with 1.4 nM, 1.2 nM and 1.7 nM for Akt1, Akt2 and Akt3, respectively. AKT-IN-3 (compound E22) also exhibits good inhibitory activity against other AGC family kinases, such as PKA, PKC, ROCK1, RSK1, P70S6K, and SGK. AKT-IN-3 (compound E22) induces apoptosis and inhibits metastasis of cancer cells .

HY-12059B

AT7867 hydrochloride

Akt Cancer

AT7867 hydrochloride is a potent and orally active inhibitor of AKT and p70 S6 kinase. AT7867 hydrochloride has anticancer effect .

AT7867 hydrochloride	Akt	Cancer
AT7867 hydrochloride is a potent and orally active inhibitor of *AKT* and p70 S6 kinase. AT7867 hydrochloride has anticancer effect .

HY-137458

Vevorisertib ARQ 751	Akt Ser/Thr Protease	Cancer
Vevorisertib (ARQ 751) is an orally active, potent and selective *pan-AKT* serine/threonine kinase inhibitor against *AKT1* (IC₅₀=0.55 nM), *AKT2* (IC₅₀=0.81 nM), and *AKT3* (IC₅₀=1.31 nM). Vevorisertib, as a single agent or in combination with other anti-cancer agents, can be used for the research of solid tumors with PIK3CA / AKT / PTEN mutations .

HY-15369

FPA-124	Akt Apoptosis	Cancer
FPA-124, a cell-permeable copper complex, is a selective *Akt* inhibitor with an IC₅₀ of 0.1 μM. FPA-124 interacts with both the pleckstrin homology (PH) and the kinase domains of Akt. FPA-124 induces apoptosis .

HY-13260

CCT128930 3 Publications Verification	Akt Autophagy Apoptosis	Cancer
CCT128930 is a ATP-competitive and selective inhibitor of *AKT* (IC₅₀=6 nM for AKT2). CCT128930 has 28-fold selectivity over the closely related PKA kinase (IC₅₀=168 nM) through the targeting of Met282 of AKT (Met173 of PKA-AKT chimera), as well as 20-fold selectivity over p70S6K (IC₅₀=120 nM). Antitumor activity.

HY-161351

STAT3/AKT-IN-1	Akt STAT Apoptosis	Cancer
STAT3/AKT-IN-1 is a dual inhibitor for the signal transducer and activator of transcription 3 (STAT3) and protein kinase B (AKT) signalling pathway, exhibits antitumor activity against gastric cancer and induces cell apoptosis in SGC-7901 cells .

HY-15290

AIM-100 3 Publications Verification	Ack1	Cancer
AIM-100 is a potent and selective Ack1 inhibitor with an IC₅₀ of 21.58 nM. AIM-100 also inhibits Tyr ²⁶⁷ phosphorylation. AIM-100 does not inhibits other kinases including PI3-kinase and AKT subfamily members. AIM-100 has an anticancer effect .

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-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-18676

OSU-T315 5+ Cited Publications	Integrin Autophagy Apoptosis	Cancer
OSU-T315 (ILK-IN-1) is a small Integrin-linked kinase (ILK) inhibitor with an IC₅₀ of 0.6 μM, inhibiting PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain) . OSU-T315 abrogates AKT activation by impeding AKT localization in lipid rafts and triggers caspase-dependent apoptosis in an ILK-independent manner . OSU-T315 causes cell death through apoptosis and autophagy .

HY-15985

CTX-0294885 2 Publications Verification	Akt	Metabolic Disease Inflammation/Immunology Cancer
CTX-0294885 is a broad spectrum **kinase inhibitor** that can capture 235 kinases from MDA-MB-231 cells, and can capture all members of the *AKT* family. CTX-0294885 is a powerful reagent for analysis of kinome signaling networks that can be used for the research of diseases like inflammation, diabetes, and cancer .

HY-15985A

CTX-0294885 hydrochloride 2 Publications Verification	Akt	Metabolic Disease Inflammation/Immunology Cancer
CTX-0294885 hydrochloride is a broad spectrum **kinase inhibitor** that can capture 235 kinases from MDA-MB-231 cells, and can capture all members of the *AKT* family. CTX-0294885 hydrochloride is a powerful reagent for analysis of kinome signaling networks that can be used for the research of diseases like inflammation, diabetes, and cancer .

HY-100932

ML-9 2 Publications Verification	Myosin	Cancer
ML-9 is a selective and potent inhibitor of **Akt kinase*, inhibits* myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity . ML-9 inhibits inhibits MLCK, PKA and PKC activity with K_i values of 4, 32 and 54 μM, respectively . ML-9 induces autophagy by stimulating autophagosome formation and inhibiting their degradation .

HY-150026

Multi-kinase-IN-2	VEGFR PDGFR FGFR c-Kit Akt Src Apoptosis	Cancer
Multi-kinase-IN-2 (compound 7h) is an orally active and potent angiokinase inhibitor. Multi-kinase-IN-2 exhibits excellent inhibitory activity against angiokinases including VEGFR-1/2/3, PDGFRα/β, and FGFR-1, as well as LYN and c-KIT kinases. Multi-kinase-IN-2 significantly attenuates phosphorylation of *AKT* and ERK proteins. Multi-kinase-IN-2 induces cell apoptosis. Multi-kinase-IN-2 shows anticancer activity .

HY-149989

Ack1 inhibitor 1	Ack1 Akt	Cancer
Ack1 inhibitor 1 is a potent, selective, and orally active inhibitor of ACK1 kinase with an IC₅₀ value of 2.1 nM. Ack1 inhibitor 1 inhibits the phosphorylation of ACK1 and activation of downstream *AKT. Ack1 inhibitor* 1 has anti-tumor activity .

HY-119751

Hematein 1 Publications Verification	Casein Kinase Akt Wnt Apoptosis	Cancer
Hematein is a oxidation product of hematoxylin acted as a dye . Hematein is an allosteric *casein kinase* II** inhibitor with an IC₅₀ of 0.74 μM. Hematein inhibits Akt/PKB Ser129 phosphorylation, the Wnt/TCF pathway and increases apoptosis in lung cancer cells .

HY-13260A

CCT128930 hydrochloride 3 Publications Verification	Akt Autophagy Apoptosis	Cancer
CCT128930 hydrochloride is a potent and selective inhibitor of *AKT* (IC₅₀=6 nM). CCT128930 hydrochloride has 28-fold selectivity over the closely related PKA kinase (IC₅₀=168 nM) through the targeting of Met282 of AKT (Met173 of PKA-AKT chimera), as well as 20-fold selectivity over p70S6K (IC₅₀=120 nM). CCT128930 hydrochloride induces cell cycle arrest, DNA damage, and autophagy. Antitumor activity .

HY-12037A

Rigosertib 5 Publications Verification ON-01910	Polo-like Kinase (PLK) PI3K Apoptosis	Cancer
Rigosertib (ON-01910) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle . Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 with an IC₅₀ of 9 nM .

HY-10971A

Alisertib sodium MLN 8237 sodium	Aurora Kinase Autophagy Apoptosis	Cancer
Alisertib (MLN 8237) sodium is an orally active and selective Aurora A kinase inhibitor (IC₅₀=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib sodium induces apoptosis and autophagy through targeting the *AKT/mTOR/AMPK/p38* pathway in leukemic cells. Antitumor activity .

HY-100932A

ML-9 Free Base	Myosin	Cancer
ML-9 (Free Base) is a selective and potent inhibitor of **Akt kinase*, inhibits* myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity . ML-9 (Free Base) inhibits inhibits MLCK, PKA and PKC activity with K_i values of 4, 32 and 54 μM, respectively . ML-9 (Free Base) induces autophagy by stimulating autophagosome formation and inhibiting their degradation .

HY-B0789

SU6656 10+ Cited Publications	Src FAK Akt	Cancer
SU6656 is a Src family kinases inhibitor with IC₅₀s of 280, 20, 130, 170 nM for Src, Yes, Lyn, and Fyn, respectively. SU6656 inhibits FAK phosphorylation at Y576/577, Y925, Y861 sites. SU6656 also inhibits p-AKT.

HY-10971

Alisertib 35+ Cited Publications MLN 8237	Aurora Kinase Autophagy Apoptosis	Cancer
Alisertib (MLN 8237) is an orally active and selective Aurora A kinase inhibitor (IC₅₀=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib (MLN 8237) induces apoptosis and autophagy through targeting the *AKT/mTOR/AMPK/p38* pathway in leukemic cells. Antitumor activity .

HY-101246

RPI-1
RPI-1 is a specific, orally available 2-indolinone Ret tyrosine kinase inhibitor. RPI-1 inhibits proliferation, Ret tyrosine phosphorylation, Ret protein expression, and the activation of PLCgamma, ERKs and AKT in human medullary thyroid carcinoma TT cells. Antitumor activity .

HY-13072

Cenisertib 1 Publications Verification AS-703569; R-763	Aurora Kinase Bcr-Abl Akt STAT FLT3	Cancer
Cenisertib (AS-703569) is an ATP-competitive multi-kinase inhibitor that blocks the activity of *Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits* tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia .

HY-162143

SKI-349	SphK Akt mTOR	Cancer
SKI-349 is a dual-targeted inhibitor of sphingosine kinase 1/2 (SPHK1/2) and microtubule assembly (MDA). SKI-349 has anticancer activity. SKI-349 can inhibit the vitality, invasion, and AKT/mTOR signaling pathway of liver cells .

HY-13326

ASP3026 5 Publications Verification	Anaplastic lymphoma kinase (ALK) Apoptosis ROS Kinase Caspase PARP IGF-1R STAT Akt JNK	Cancer
ASP3026 is a selective and orally active inhibitor of anaplastic lymphoma kinase (ALK). ASP3026 is a selective and oral active anaplastic lymphoma kinase (ALK) inhibitor with a IC₅₀ value of 3.5 nM. ASP3026 can inhibit the phosphorylation of IGF-1R, STAT3, *AKT* and JNK proteins, and induce the cleavage of caspase 3 and PARP. It also inhibited ROS and ACK. ASP3026 can be used in anti-tumor research .

HY-110193

SPP-86 1 Publications Verification	RET	Cancer
SPP-86 is a potent and selective cell permeable inhibitor of RET tyrosine kinase, with an IC₅₀ of 8 nM. SPP-86 inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells . SPP-86 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-107597

Halicin 1 Publications Verification SU3327	JNK	Metabolic Disease Inflammation/Immunology
Halicin (SU3327) is a potent, selective and substrate-competitive JNK inhibitor with an IC₅₀ of 0.7 μM. Halicin also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC₅₀ of 239 nM. Halicin shows less active against p38α and Akt kinase .

HY-147259

Dalmelitinib	c-Met/HGFR	Cancer
Dalmelitinib is an orally active selective c-Met kinase inhibitor (IC₅₀: 2.9 nM) that binds to the ATP-binding region of c-Met. Dalmelitinib induces the phosphorylation of MET, partially or completely inhibits the phosphorylation of AKT and ERK. Dalmelitinib potently inhibits cancer cell (c-Met oncogene amplification) proliferation, and is used for the research of cancers like human non-small cell lung cancer (NSCLC) .

HY-10230S

Midostaurin-d5 PKC412-d₅; CGP 41251-d₅	Isotope-Labeled Compounds PKC Syk Akt PKA c-Kit	Cancer
Midostaurin-d₅ is a deuterium labeled Midostaurin. Midostaurin is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM[1].

HY-116035

Nimbolide 1 Publications Verification	NF-κB CDK Apoptosis	Cancer
Nimbolide is a triterpene compound that can be isolated from neem (Azadirachta indica), possesses anticancer and antiproliferative activity. Nimbolide induces tumor cell apoptosis by inhibiting NF-κB and CDK4/CDK6 kinase. Nimbolide suppresses the Wnt, PI3K-Akt, MAPK and JAK-STAT signaling pathways .

HY-12037

Rigosertib sodium 5 Publications Verification ON-01910 sodium	Polo-like Kinase (PLK) PI3K Apoptosis	Cancer
Rigosertib sodium (ON-01910 sodium) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the *PI3K/Akt* pathway, promotes the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle . Rigosertib sodium is a selective and non-ATP-competitive inhibitor of PLK1 with an IC₅₀ of 9 nM .

HY-16558

Butein 3 Publications Verification 2’,3,4,4’-tetrahydroxy Chalcone	EGFR Autophagy Apoptosis Phosphodiesterase (PDE)	Cancer
Butein is a cAMP-specific PDE inhibitor with an IC₅₀ of 10.4 μM for PDE4 . Butein is a specific protein tyrosine kinase inhibitor with IC₅₀s of 16 and 65 μM for EGFR and p60 ^c-src in HepG2 cells . Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a . Butein is a SIRT1 activator (STAC).

HY-121629

PS210	PDK-1	Cancer
PS210 is a potent and selective PDK1 activator with a K_d of 3 μM and targets the PIF-binding pocket of PDK1. PS210 is inactive against other protein kinases, including PDK1 downstream signaling components such as S6K, PKB/Akt or GSK3. In cells, the prodrug of PS210 (PS423) acts as a substrate-selective inhibitor of PDK1, inhibiting the phosphorylation and activation of S6K .

HY-132231

FD223	PI3K Apoptosis	Cancer
FD223 is a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. FD223 displays high potency (IC₅₀=1 nM) and good selectivity over other isoforms (IC₅₀s of 51 nM, 29 nM and 37 nM, respectively for α, β and γ). FD223 exhibits efficient inhibition of the proliferation of acute myeloid leukemia (AML) cell lines by suppressing p-AKT Ser473 thus causing G1 phase arrest during the cell cycle. FD223 has potential for the research of leukemia such as AML .

HY-10230

Midostaurin 20+ Cited Publications PKC412; CGP 41251	PKC VEGFR c-Kit NO Synthase Apoptosis	Cancer
Midostaurin (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin inhibits PKCα/β/γ, Syk, Flk-1, *Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ* and VEGFR1/2 with IC₅₀s ranging from 22-500 nM . Midostaurin also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin shows powerful anticancer effects .

Cat. No.	Product Name

HY-L009

Kinase Inhibitor Library

3137 compounds

Kinase is an enzyme that adds phosphate groups to other molecules. This process is known as phosphorylation. Protein phosphorylation is a key aspect in the regulation of a large number of cellular processes including cellular division, metabolism, signal transduction, and so on. There are over 500 kinases encoded by the human genome and it has been estimated that kinases regulate approximately 50% of cellular functions. Kinases are a large group of drug targets in drug discovery. Kinase inhibitors are an important class of drugs that block certain enzymes involved in diseases such as cancer and inflammatory disorders.

Kinase inhibitor library designed by MCE contains 3137 kinase inhibitors and regulators mainly targeting protein kinases (VEGFR, EGFR, BTK, CDK, Akt, etc.), lipid kinases (PI3K, PI4K, SK, etc.) and carbohydrate kinases (Hexokinase), and is a useful tool for kinase drug discovery and related research.

HY-L164

Serine/Threonine Kinase Inhibitor Library

1267 Compounds compounds

Protein serine/threonine kinases (PSKs) are protein kinases that use ATP as a high-energy donor molecule to transfer phosphate groups to serine/threonine residues of target protein. As an important signal transduction regulator, serine/threonine kinases can affect the function of target proteins by disrupting enzyme activity or binding of target proteins to other proteins. Serine/threonine kinases are involved in the regulation of immune response, cell proliferation, differentiation, apoptosis and other physiological processes. Serine/threonine kinase inhibitors are an important class of compounds that have been widely studied in cancer, chronic inflammation, autoimmune diseases, aging and other diseases.

MCE designs a unique collection of 1267 serine/threonine kinase inhibitors, mainly targeting the receptor PKA, Akt, PKC, MAPK/ERK, etc, which is an effective tool for development and research of anti-cancer, anti-chronic inflammatory diseases, anti-autoimmune diseases and anti-aging compounds.

HY-L015

PI3K/Akt/mTOR Compound Library

568 compounds

The PI3K/Akt/mTOR pathway controls many cellular processes that are important for the formation and progression of cancer, including apoptosis, transcription, translation, metabolism, angiogenesis, and cell cycle progression. Every major node of this signaling network is activated in a wide range of human tumors. Mechanisms for the pathway activation include activation of receptor tyrosine kinases (RTKs) upstream of PI3K, mutation or amplification of PIK3CA encoding p110α catalytic subunit of PI3K, mutation or loss of PTEN tumor suppressor gene, and mutation or amplification of Akt1. Once the pathway is activated, signaling through Akt can stimulate a series of substrates including mTOR which is involved in protein synthesis. Thus, inhibition of this pathway is an attractive concept for cancer prevention and/or therapy. Currently some mTOR inhibitors are approved for several indications, and there are several novel PI3K/Akt/mTOR inhibitors in clinical trials.

MCE owns a unique collection of 568 compounds that can be used for PI3K/Akt/mTOR pathway research. PI3K/Akt/mTOR Compound Library also acts as a useful tool for anti-cancer drug discovery.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-116035

Nimbolide 1 Publications Verification	Triterpenes Structural Classification Classification of Application Fields Terpenoids Source classification Plants Azadirachta indica A. Juss. Disease Research Fields Meliaceae Cancer	NF-κB CDK Apoptosis
Nimbolide is a triterpene compound that can be isolated from neem (Azadirachta indica), possesses anticancer and antiproliferative activity. Nimbolide induces tumor cell apoptosis by inhibiting NF-κB and CDK4/CDK6 kinase. Nimbolide suppresses the Wnt, PI3K-Akt, MAPK and JAK-STAT signaling pathways .

HY-16558

Butein 3 Publications Verification 2’,3,4,4’-tetrahydroxy Chalcone	Structural Classification Chalcones Flavonoids other families Classification of Application Fields Anti-aging Source classification Phenols Polyphenols Plants Disease Research Fields Cancer	EGFR Autophagy Apoptosis Phosphodiesterase (PDE)
Butein is a cAMP-specific PDE inhibitor with an IC₅₀ of 10.4 μM for PDE4 . Butein is a specific protein tyrosine kinase inhibitor with IC₅₀s of 16 and 65 μM for EGFR and p60 ^c-src in HepG2 cells . Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a . Butein is a SIRT1 activator (STAC).

HY-N0281

Daphnetin 2 Publications Verification 7,8-Dihydroxycoumarin	Classification of Application Fields Daphne Thymelaeaceae Source classification Coumarins Phenols Polyphenols Phenylpropanoids Plants Disease Research Fields Cancer	EGFR PKA PKC Autophagy Apoptosis AMPK Akt mTOR Reactive Oxygen Species Caspase Bcl-2 Family PARP Parasite
Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC₅₀s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1ß, ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research .

HY-W744699

Larixol (+)-Larixol	Larix decidua Miller Structural Classification Natural Products Pinaceae Source classification Plants	Src ERK Akt
Larixol is an fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Larixol can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Larixol inhibits fMLP (0.1 μM)-induced superoxide anion production (IC₅₀: 1.98 μM), cathepsin G release (IC₅₀: 2.76 μM), and chemotaxis. Larixol improves neutrophil hyperactivation and reduces inflammation or tissue damage. A series of Larixol derivatives were found to have inhibitory effects on FSGS-related TRPC6 functional mutants .

Cat. No.	Product Name	Chemical Structure

HY-10230S

Midostaurin-d5
Midostaurin-d₅ is a deuterium labeled Midostaurin. Midostaurin is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM[1].

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