PIK3CA

By Targets:	Akt (5) Apoptosis (4) Autophagy (3) MMP (1) mTOR (2) Organoid (3) p38 MAPK (1) PI3K (5) Ser/Thr Protease (1) Small Interfering RNA (siRNA) (3)
By Research Areas:	Cancer (12) Infection (1) Inflammation/Immunology (2)
Oligonucleotides:	Pre-designed siRNA Sets (3) siRNAs (3)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-100886

BAY1082439	PI3K Apoptosis	Cancer
BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibiting Pten-null prostate cancer growth .

HY-15244

Alpelisib 90+ Cited Publications BYL-719	PI3K	Cancer
Alpelisib (BYL-719) is a potent, selective, and orally active PI3Kα inhibitor. Alpelisib (BYL-719) shows efficacy in targeting PIK3CA-mutated cancer. Alpelisib (BYL-719) also inhibits p110α/p110γ/p110δ/p110β with IC₅₀s of 5/250/290/1200 nM, respectively. Antineoplastic activity ^[3].

HY-153306

RLY-2608	PI3K	Cancer
RLY-2608 is an orally active first-in-class allosteric mutant-selective inhibitor of *PI3Ka* with anti-tumor activity. RLY-2608 inhibits tumor growth in PIK3CA-mutant xenograft mice models with minimal impact on insulin ^[3].

HY-RS10523

PIK3CA Human Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
PIK3CA Human Pre-designed siRNA Set A contains three designed siRNAs for PIK3CA gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

PIK3CA Human Pre-designed siRNA Set A PIK3CA Human Pre-designed siRNA Set A

HY-RS10524

Pik3ca Mouse Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
Pik3ca Mouse Pre-designed siRNA Set A contains three designed siRNAs for Pik3ca gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

Pik3ca Mouse Pre-designed siRNA Set A Pik3ca Mouse Pre-designed siRNA Set A

HY-RS10525

Pik3ca Rat Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
Pik3ca Rat Pre-designed siRNA Set A contains three designed siRNAs for Pik3ca gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

Pik3ca Rat Pre-designed siRNA Set A Pik3ca Rat Pre-designed siRNA Set A

HY-N12726

Halociline	p38 MAPK MMP	Infection Inflammation/Immunology Cancer
Halociline, a derivative of alkaloids, that can be isolated from the marine fungus Penicillium griseofulvum. Halociline targets MAPK1, MMP-9, and PIK3CA in gastric cancer cells, potentially mediated by diverse pathways including cancer, lipid metabolism, atherosclerosis, and EGFR tyrosine kinase inhibitor resistance. Halociline possesses antimicrobial, antioxidant and biofilm inhibitory activities .

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-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 ^[3] .

HY-10357

MK-2206 free base	Organoid Akt Autophagy Apoptosis	Cancer
MK-2206 free base 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 free base. MK-2206 free base has anticancer activities .

HY-13898

Taselisib 15+ Cited Publications GDC-0032; RG-7604	PI3K	Cancer
Taselisib (GDC-0032) is a potent *PI3K* inhibitor targets PIK3CA mutations, with K_is of 0.12 nM, 0.29 nM, 0.97 nM, and 9.1 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.

HY-126077

MTI-31 1 Publications Verification LXI-15029	mTOR	Inflammation/Immunology Cancer
MTI-31 (LXI-15029) is a potent, orally active and highly selective inhibitor of mTORC1 and mTORC2. MTI-31 is selective for mTOR (K_d: 0.20 nM) versus PIK3CA, PIK3CB and PIK3G with >5,000 fold selectivity in mTOR binding assays. MTI-31 shows an IC₅₀ of 39 nM for mTOR in LANCE assay of mTOR substrate phosphorylation with 100 μM ATP. MTI-31 can be used for the research of breast cancer .

HY-116191

WJD008	PI3K mTOR	Cancer
WJD008 is a potent dual phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor with antiproliferative and anticlonogenic activity in tumor cells and transformed cells with PIK3CA mutant. WJD008 inhibits kinase activity of PI3K α and mTOR and abrogates insulin-like growth factor-I-activated PI3K-Akt-mTOR signaling cascade. WJD008 is promising for research of cancers .

HY-10358

MK-2206 dihydrochloride Maximum Cited Publications 332 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-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 .

Cat. No.	Product Name

HY-L015

PI3K/Akt/mTOR Compound Library	600 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 600 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.

PI3K/Akt/mTOR Compound Library

600 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 600 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-N12726

Halociline	Structural Classification Microorganisms Marine natural products Source classification Phenols Marine microorganism	p38 MAPK MMP
Halociline, a derivative of alkaloids, that can be isolated from the marine fungus Penicillium griseofulvum. Halociline targets MAPK1, MMP-9, and PIK3CA in gastric cancer cells, potentially mediated by diverse pathways including cancer, lipid metabolism, atherosclerosis, and EGFR tyrosine kinase inhibitor resistance. Halociline possesses antimicrobial, antioxidant and biofilm inhibitory activities .

Species:	Human (2)
Tag:	His (1) Strep (1) Tag Free (1)
Source:	Sf9 insect cells (2)

Cat. No.	Compare	Product Name	Species	Source

HY-P703580

	PIK3CA Protein, Human (Active, Sf9, His, Strep) Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform; Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit alpha; PtdIns-3-kinase subunit p110-alpha; p110alpha; Phosphoinositide 3-kinase alpha; Phosphoinositide-3-kinase catalytic alpha polypeptide; Serine/threonine protein kinase PIK3CA; 2.7.11.1; PIK3CA; Homo sapiens; Human; PI3-kinase subunit alpha; Kinase; Serine/threonine-protein kinase; Transferase; 2.7.1.137	Human	Sf9 insect cells
	PIK3CA Protein, Human (Active, Sf9, His, Strep) is the recombinant human-derived PIK3CA, expressed by Sf9 insect cells , with Strep, His labeled tag. ,

HY-P703583

	*PIK3R1-PIK3CA Protein, Human (Active, Sf9)* GRB1	Human	Sf9 insect cells

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HY-P81162

	*PI3 Kinase p110 alpha/PIK3CA Antibody* PI3 kinase p110 subunit alpha; caPI3K; MGC142161; MGC142163; p110 alpha; Phosphatidylinositol 3 kinase catalytic alpha polypeptide; Phosphatidylinositol 3 kinase catalytic 110 KD alpha; Phosphatidylinositol 4 5 bisphosphate 3 kinase catalytic subunit alpha isoform; Phosphoinositide 3 kinase catalytic alpha polypeptide; PI3 kinase p110 subunit alpha; PI3K; PI3KC A; PIK3C A; PK3CA; PtdIns 3 kinase p110; PI3-kinase P110α; PI3-kinase p110 subunit alpha; PI 3 Kinase catalytic subunit alpha; PK3CA_HUMAN; PI3 kinase P110α.	WB, ICC/IF, IP	Human, Mouse, Rat
	PIK3CA Antibody is an unconjugated, approximately 110 kDa, rabbit-derived, anti-PIK3CA monoclonal antibody. PIK3CA Antibody can be used for: WB, ICC/IF, IP expriments in human, mouse, rat background without labeling.

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Cat. No.	Product Name		Classification

HY-RS10523

PIK3CA Human Pre-designed siRNA Set A		siRNAs Pre-designed siRNA Sets
PIK3CA Human Pre-designed siRNA Set A contains three designed siRNAs for PIK3CA gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

HY-RS10524

Pik3ca Mouse Pre-designed siRNA Set A		siRNAs Pre-designed siRNA Sets
Pik3ca Mouse Pre-designed siRNA Set A contains three designed siRNAs for Pik3ca gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

HY-RS10525

Pik3ca Rat Pre-designed siRNA Set A		siRNAs Pre-designed siRNA Sets
Pik3ca Rat Pre-designed siRNA Set A contains three designed siRNAs for Pik3ca gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

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