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Isoforms Recommended:	PI3Kα

Results for "

PI3K-α

" in MedChemExpress (MCE) Product Catalog:

By Targets:	PI3K (108) Apoptosis (22) ATM/ATR (3) Autophagy (7) Bacterial (1) Bcr-Abl (1) Casein Kinase (1) CDK (1) DNA-PK (5) Dopamine Receptor (3) Epigenetic Reader Domain (2) HDAC (3) MEK (2) mTOR (40) PARP (1) PERK (2) PI4K (1) Reactive Oxygen Species (2) Syk (1) Virus Protease (1) Wnt (1)
By Research Areas:	Cancer (108) Infection (2) Inflammation/Immunology (3) Metabolic Disease (1) Neurological Disease (4)

114

Inhibitors & Agonists

Natural
Products

Targets Recommended: PI3K

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-19763

BEBT-908 PI3Kα inhibitor 1	PI3K	Cancer
BEBT-908 (PI3Kα inhibitor 1) is a selective PI3Kα inhibitor extracted from patent US/20120088764A1, Compound 243, has an IC₅₀<0.1 μM, PI3Kα inhibitor 1 also inhibits HDAC (0.1 μM≤IC₅₀≤1 μM) .

HY-153915

PI3Kα-IN-11

PI3K Cancer

PI3Kα-IN-11 is a potent PI3Kα inhibitor with anticancer activity .

PI3Kα-IN-11	PI3K	Cancer
PI3Kα-IN-11 is a potent PI3Kα inhibitor with anticancer activity .

HY-163360

PI3Kα-IN-19	PI3K	Cancer
PI3Kα-IN-19 (Compound 1) is a PI3Kα inhibitor with a targeted binding site at the p110α catalytic subunit. PI3Kα is one of the most common dysregulated kinases used in cancer research .

HY-U00326

PI3Kα/mTOR-IN-1	PI3K mTOR	Cancer
PI3Kα/mTOR-IN-1 is a potent PI3Kα/mTOR dual inhibitor, with an IC₅₀ of 7 nM for PI3Kα in a cell assay, and K_is of 10.6 nM and 12.5 nM for mTOR and PI3Kα in a cell free assay , respectively.

HY-160458

PI3Kα-IN-17

PI3K Others

PI3Kα-IN-17 (example 4) is a potent inhibitor of PI3Kα .
HY-163361

PI3Kα-IN-20

PI3K Cancer

PI3Kα-IN-20 (compound 2) is a selective PI3Kα inhibitor .
HY-124647

PI3Kα-IN-1

PI3K Cancer

PI3Kα-IN-1 is a PI3Kα inhibitor (IC₅₀ < 0.5 nM), and also inhibits mTOR (IC₅₀: 104 nM) .

PI3Kα-IN-17	PI3K	Others
PI3Kα-IN-17 (example 4) is a potent inhibitor of *PI3K*α .

PI3Kα-IN-20	PI3K	Cancer
PI3Kα-IN-20 (compound 2) is a selective PI3Kα inhibitor .

PI3Kα-IN-1	PI3K	Cancer
PI3Kα-IN-1 is a PI3Kα inhibitor (IC₅₀ < 0.5 nM), and also inhibits mTOR (IC₅₀: 104 nM) .

HY-150618

PI3Kα-IN-9	PI3K Apoptosis	Cancer
PI3Kα-IN-9 (compound 27) is a selective, long-acting and oral active PI3Kα inhibitor with IC₅₀ values of 4.4, 128, 146 and 153 nM for PI3Kα, PI3Kγ, PI3Kδ and PI3Kβ, respectively. PI3Kα-IN-9 has antiproliferative activity and induces apoptosis. PI3Kα-IN-9 can be used for cancer research .

HY-131345

PI3Kα-IN-4

PI3K Cancer

PI3Kα-IN-4 is a potent, selective and orally active inhibitor of PI3Kα, with an IC₅₀ of 1.8 nM. PI3Kα-IN-4 has antitumor activity .

PI3Kα-IN-4	PI3K	Cancer
PI3Kα-IN-4 is a potent, selective and orally active inhibitor of PI3Kα, with an IC₅₀ of 1.8 nM. PI3Kα-IN-4 has antitumor activity .

HY-147983

PI3Kα-IN-8	PI3K Reactive Oxygen Species Apoptosis	Cancer
PI3Kα-IN-8 (Compound 9g) is a selective PI3Kα inhibitor with an IC₅₀ of 0.012 μM. PI3Kα-IN-8 increases intracellular reactive oxygen species level, decreases mitochondrial membrane potential and induces apoptosis .

HY-161373

PI3Kα-IN-22	PI3K	Cancer
PI3Kα-IN-22 (Compound 17) is an orally active, potent and selective inhibitor of PI3Kα ^H1047R, with an IC₅₀ of 1 nM for pAKT T47D AlphaLISA. PI3Kα-IN-22 can induce tumor regressions in the HCC1954 tumor model in mice .

HY-147767

PI3Kα-IN-6	PI3K Apoptosis Reactive Oxygen Species	Cancer
PI3Kα-IN-6 (Compound 5b) is a PI3Kα inhibitor. PI3Kα-IN-6 exhibits anticancer potential and no toxicity in normal cells. PI3Kα-IN-6 increases generation of ROS, reduces mitochondrial membrane potential (MMP) and induces apoptosis .

HY-149000

PI3Kα-IN-7	PI3K Apoptosis	Cancer
PI3Kα-IN-7 (Compound A12) is a potent PI3Kα inhibitor. PI3Kα-IN-7 also inhibits PI3Kβ. PI3Kα-IN-7 decreases cancer cells mitochondrial membrane potential and induces apoptosis .

HY-161140

PI3Kα-IN-16	PI3K Wnt	Cancer
PI3Kα-IN-16 (Z86) is a novel PI3Kα inhibitor with an IC₅₀ value of 4.28 μM. PI3Kα-IN-16 has potent inhibitory efficiency on PI3K-mediated CRCs growth and migration. PI3Kα-IN-16 also inhibits the Wnt signaling pathway .

HY-149427

PI3Kα-IN-12	PI3K	Cancer
PI3Kα-IN-12 (compound 13) is a highly selective PI3Kα inhibitor (IC₅₀: 1.2 nM). PI3Kα-IN-12 inhibits HCT-116 and U87-MG with IC₅₀s values of 0.83 and 1.25 μM, respectively. PI3Kα-IN-12 (40 mg/kg; IP) causes tumor regression in a U87-MG cell line xenograft mouse model .

HY-156018

PI3Kα-IN-13	PI3K	Cancer
PI3Kα-IN-13 (Compound 18a) is a PI3Kα inhibitor (IC₅₀: 2.5 nM). PI3Kα-IN-13 induces tumor cell apoptosis. PI3Kα-IN-13 inhibits cancer cell proliferation with IC₅₀s of 0.75 μM (MCF-7), 3.79 μM (HCT-116), 13.71 μM (MDA-MB-231), 9.85 μM (SW620), respectively. PI3Kα-IN-13 inhibits tumor cell colony formation, migration and invasion .

HY-157125

PI3Kα-IN-14	PI3K Apoptosis	Cancer
PI3Kα-IN-14 (compound F8) is a selective PI3Kα inhibitor with an IC₅₀ of 0.14 nM. PI3Kα-IN-14 induces a great decrease in mitochondrial membrane which caused cell cycle arrest at G1 phase and apoptosis in U87-MG cells. PI3Kα-IN-14 shows significant anti-proliferative activities against three tumor-derived cell lines (PC-3: IC₅₀ of 0.28 μM; HCT-116: IC₅₀ of 0.57 μM; and U87-MG: IC₅₀ of 1.37 μM) .

HY-157319

PI3Kα-IN-15	PI3K	Cancer
PI3Kα-IN-15 is a potent PI3Kα inhibitor with an IC₅₀ of 0.15?μM. PI3Kα-IN-15 also has acceptable anti-proliferative activity (inhibits SKOV-3, T47D, NCI-H1975, NCI-H460, and MCF-7 growth with IC₅₀ values of 26.6?μM, 7.9?μM,? 32.1?μM,? 17.7??μM, and 9.4??μM, respectively. PI3Kα-IN-15 can be used for cancer research .

HY-155211

mTOR inhibitor-13	mTOR PI3K	Cancer
mTOR inhibitor-13 (compound 9g), an aryl ureido compound, is a potent and selective mTOR inhibitor with an IC₅₀ of 0.29 nM. mTOR inhibitor-13 also inhibits *PI3K-α* with an IC₅₀ of 119 nM .

HY-10683

PKI-402 5 Publications Verification	PI3K mTOR	Cancer
PKI-402 is a selective, reversible, ATP-competitive inhibitor of *PI3K, including PI3K-α mutants, and mTOR* (IC₅₀=2, 3, 7,14 and 16 nM for PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ).

HY-11080

PKI-179	PI3K mTOR	Cancer
PKI-179 is a potent and orally active dual *PI3K/mTOR* inhibitor, with IC₅₀s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for *PI3K-α, PI3K-β, PI3K-γ, PI3K-δ* and mTOR, respectively. PKI-179 also exhibits activity over E545K and H1047R, with IC₅₀s of 14 nM and 11 nM, respectively. PKI-179 shows anti-tumor activity in vivo .

HY-11080A

PKI-179 hydrochloride	PI3K mTOR	Cancer
PKI-179 hydrochloride is a potent and orally active dual *PI3K/mTOR* inhibitor, with IC₅₀s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for *PI3K-α, PI3K-β, PI3K-γ, PI3K-δ* and mTOR, respectively. PKI-179 hydrochloride also exhibits activity over E545K and H1047R, with IC₅₀s of 14 nM and 11 nM, respectively. PKI-179 hydrochloride shows anti-tumor activity in vivo .

HY-162023

mTOR inhibitor-10	mTOR PI3K	Cancer
mTOR inhibitor-10 (Compound 9c) is a selective inhibitor for mTOR. mTOR inhibitor-10 inhibits mTOR and *PI3K-α, with IC₅₀* of 0.7 and 825 nM. mTOR inhibitor-10 inhibits proliferation of LNCaP with IC₅₀ of 87 nM .

HY-162025

mTOR inhibitor-17	mTOR PI3K	Cancer
mTOR inhibitor-17 (Compound 9e) is a selective inhibitor for mTOR. mTOR inhibitor-10 inhibits mTOR and *PI3K-α, with IC₅₀* of 0.68 and 1359 nM. mTOR inhibitor-10 inhibits proliferation of LNCaP with IC₅₀ of 40 nM .

HY-162024

mTOR inhibitor-16	mTOR PI3K	Cancer
mTOR inhibitor-16 (Compound 9f) is a selective inhibitor for mTOR. mTOR inhibitor-10 inhibits mTOR and *PI3K-α, with IC₅₀* of 1.25 and 82 nM. mTOR inhibitor-10 inhibits proliferation of LNCaP with IC₅₀ of 140 nM .

HY-109633

PI3K-IN-18	mTOR PI3K	Cancer
PI3K-IN-18 (Compound 1) is a *PI3K* inhibitor, and can also effectively inhibit the homologous enzymemTOR. The IC₅₀ values of PI3K-IN-18 for mTOR and PI3K-α were 49 nM and 41 nM, respectively .

HY-150034

PI3K-IN-38	PI3K	Inflammation/Immunology Cancer
PI3K-IN-38 (compound 123) is an orally active *PI3K* inhibitor with IC₅₀ of 0.541 µM (PI3K-α). PI3K-IN-38 shows activities of anticancer and anti-inflammatory, which inhibis tumor growth in vivo .

HY-13864

PF-4989216

PI3K Apoptosis Cancer

PF-4989216 is a potent and selective PI3Kα inhibitor with a K_i of 0.6 nM.
HY-101272

GDC-0326

PI3K Cancer

GDC-0326 is a potent and selective PI3Kα inhibitor with a K_i of 0.2 nM.
HY-16596

CNX-1351

PI3K Cancer

CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor with IC₅₀ of 6.8 nM.
HY-100470

NSC781406

2 Publications Verification

PI3K mTOR Cancer

NSC781406 is a highly potent PI3K and mTOR inhibitor with an IC₅₀ of 2 nM for PI3Kα.

PF-4989216	PI3K Apoptosis	Cancer
PF-4989216 is a potent and selective PI3Kα inhibitor with a K_i of 0.6 nM.

GDC-0326	PI3K	Cancer
GDC-0326 is a potent and selective PI3Kα inhibitor with a K_i of 0.2 nM.

CNX-1351	PI3K	Cancer
CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor with IC₅₀ of 6.8 nM.

NSC781406 2 Publications Verification	PI3K mTOR	Cancer
NSC781406 is a highly potent *PI3K* and mTOR inhibitor with an IC₅₀ of 2 nM for PI3Kα.

HY-11105

Pilaralisib analogue 2 Publications Verification XL147 analogue	PI3K Apoptosis	Cancer
Pilaralisib analogue (XL147 analogue) is a representative and selective PI3Kα inhibitor extracted from patent WO2012006552A1, Compound 147 in Table 1.

HY-12340

ETP-46321

PI3K Cancer

ETP-46321 is a potent and orally bioavailable PI3Kα and PI3Kδ inhibitor with K_iapps of 2.3 and 14.2 nM, respectively.
HY-12869

AZD-8835

1 Publications Verification

PI3K Cancer

AZD8835 is a potent and selective inhibitor of PI3Kα and PI3Kδ with IC₅₀s of 6.2 and 5.7 nM, respectively.

ETP-46321	PI3K	Cancer
ETP-46321 is a potent and orally bioavailable PI3Kα and PI3Kδ inhibitor with K_iapps of 2.3 and 14.2 nM, respectively.

AZD-8835 1 Publications Verification	PI3K	Cancer
AZD8835 is a potent and selective inhibitor of PI3Kα and PI3Kδ with IC₅₀s of 6.2 and 5.7 nM, respectively.

HY-101562

Inavolisib 2 Publications Verification GDC-0077; RG6114	PI3K Apoptosis	Cancer
GDC-0077 (RG6114) is a potent, orally available, and selective PI3Kα inhibitor (IC₅₀=0.038 nM). GDC-0077 (RG6114) exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. GDC-0077 (RG6114) is more selective for mutant versus wild-type PI3Kα .

HY-131972

PF-06843195	PI3K	Cancer
PF-06843195 is a highly selective PI3Kα inhibitor with an IC₅₀ of 18 nM in Rat1 fibroblasts. The K_is of PF-06843195 for PI3Kα and PI3Kδ in biochemical kinase assay are less than 0.018 nM and 0.28 nM, respectively. PF-06843195 has great suppression of the PI3K/mTOR signaling pathway and durable antitumor efficacy .

HY-15466

Izorlisib 3 Publications Verification CH5132799	PI3K	Cancer
Izorlisib (CH5132799) is a selective class I *PI3K* inhibitor. Izorlisib inhibits class I PI3Ks, particularly PI3Kα, with an IC₅₀ of 14 nM.

HY-12338

ON 146040

PI3K Bcr-Abl Cancer

ON 146040 is a potent PI3Kα and PI3Kδ (IC₅₀≈14 and 20 nM, respectively) inhibitor. ON 146040 also inhibits Abl1 (IC₅₀<150 nM).

ON 146040	PI3K Bcr-Abl	Cancer
ON 146040 is a potent PI3Kα and PI3Kδ (IC₅₀≈14 and 20 nM, respectively) inhibitor. ON 146040 also inhibits Abl1 (IC₅₀<150 nM).

HY-100398

PF-04979064 2 Publications Verification	PI3K mTOR	Cancer
PF-04979064 is a potent and selective *PI3K/mTOR* dual kinase inhibitor with K_is of 0.13 nM and 1.42 nM for PI3Kα and mTOR, respectively.

HY-118712

mTOR inhibitor WYE-23	mTOR	Cancer
mTOR inhibitor WYE-23 is a mTOR inhibitor, and IC₅₀ is 0.45 nM. It is selective to PI3Kα and IC₅₀ is 661 nM. mTOR inhibitor WYE-23 has antitumor activity .

HY-100385

Brevianamide F 2 Publications Verification Cyclo(L-Pro-L-Trp)	PI3K Bacterial	Infection
Brevianamide F (Cyclo(L-Pro-L-Trp)) is a mycotoxin isolated from Colletotrichum gloeosporioides, with antibacterial activity. Brevianamide F shows potent PI3Kα inhibitory activity with an IC₅₀ of 4.8 µM .

HY-156681

STX-478	PI3K	Cancer
STX-478 (compound 80) is an oral CNS-penetrant allosteric mutant-selective PI3Kα inhibitor. STX-478 shows robust and durable tumor regression and can be used in cancer research .

HY-154848

UCL-TRO-1938	PI3K	Cancer
UCL-TRO-1938 is a potent allosteric activator of PI3Kα with an EC₅₀ value of approximately 60 μM. UCL-TRO-1938 can induce cell proliferation and has cardioprotective and neural regeneration effects .

HY-124036

DS-7423

PI3K mTOR Cancer

DS-7423 is a dual PI3K and mTOR inhibitor, with IC₅₀ values of 15.6 nM, 34.9 nM for PI3Kα and mTOR, respectively. DS-7423 possesses anti-tumor activity .

DS-7423	PI3K mTOR	Cancer
DS-7423 is a dual *PI3K* and mTOR inhibitor, with IC₅₀ values of 15.6 nM, 34.9 nM for PI3Kα and mTOR, respectively. DS-7423 possesses anti-tumor activity .

HY-131345A

(S)-PI3Kα-IN-4	PI3K	Cancer
(S)-PI3Kα-IN-4 is a potent inhibitor of PI3Kα, with an IC₅₀ of 2.3 nM. (S)-PI3Kα-IN-4 shows 38.3-, 4.25-, and 4.93-fold selectivity for PI3Kα over PI3Kβ, PI3Kδ, and PI3Kγ, respectively. (S)-PI3Kα-IN-4 can be used for the research of cancer .

HY-12046

PIK-93 4 Publications Verification	PI4K PI3K Virus Protease	Cancer
PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC₅₀ of 19 nM, and also inhibits PI3Kγ and PI3Kα with IC₅₀ of 16 nM and 39 nM, respectively.

HY-15174

Dactolisib Tosylate 45+ Cited Publications BEZ235 Tosylate; NVP-BEZ 235 Tosylate	PI3K mTOR Autophagy	Cancer
Dactolisib Tosylate (BEZ235 Tosylate) is a dual *PI3K* and mTOR kinase inhibitor with IC₅₀ values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively. Dactolisib Tosylate (BEZ235 Tosylate) inhibits mTORC1 and mTORC2.

HY-101146

SF2523 2 Publications Verification	PI3K Epigenetic Reader Domain DNA-PK	Cancer
SF2523 is a highly selective and potent inhibitor of *PI3K* with IC₅₀s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.

HY-136198

SRX3207	Syk PI3K	Cancer
SRX3207 is an orally active and first-in-class dual *Syk/PI3K* inhibitor, with IC₅₀ values of 10.7 nM and 861 nM for Syk and PI3Kα, respectively. SRX3207 relieves tumor immunosuppression .

HY-15177

PF-04691502 5+ Cited Publications	PI3K mTOR Autophagy	Cancer
PF-04691502 is a potent and selective inhibitor of *PI3K* and mTOR. PF-04691502 binds to human PI3Kα, β, δ, γ and mTOR with K_is of 1.8, 2.1, 1.6, 1.9 and 16 nM, respectively.

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PI3K-α

Inhibitors & Agonists

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