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Isoforms Recommended:	PI3Kα

Results for "

PI3Kα

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (5) Bacterial (1) CDK (2) GSK-3 (1) HDAC (4) mTOR (13) PARP (1) PI3K (42) Reactive Oxygen Species (2) Wnt (1)
By Research Areas:	Cancer (41) Infection (1) Inflammation/Immunology (1)

Inhibitors & Agonists

Natural
Products

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-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 .
HY-160458

PI3Kα-IN-17

PI3K Others

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

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

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-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-156091

PI3Kα/HDAC6-IN-1	PI3K HDAC	Cancer
PI3Kα/HDAC6-IN-1 (compound 21j) is a dual PI3Kα/HDAC6 inhibitor with IC₅₀ of 2.9 and 26 nM, respectively. PI3Kα/HDAC6-IN-1 also inhibits AKT(Ser473) phosphorylation and induces the accumulation of acetylated α-tubulin without affecting acetylated histones H3 and H4. PI3Kα/HDAC6-IN-1 efficiently inhibits L-363 cell line (IC₅₀=0.17 μM) and has good anti-cancer activity .

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-144295

PI3Kα-IN-5	PI3K mTOR	Cancer
PI3Kα-IN-5 (compound 6 ab) is a potent PI3Kα/mTOR inhibitor, with an IC₅₀ of 0.7 nM and 3.3 nM, respectively. PI3Kα-IN-5 can be used for the research of colorectal cancer .

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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-124760

hSMG-1 inhibitor 11e	mTOR PI3K CDK	Cancer
hSMG-1 inhibitor 11e is a potent and selective hSMG-1 kinase inhibitor with an IC₅₀ of <0.05 nM. hSMG-1 inhibitor 11e shows >900-fold selectivity over mTOR (IC₅₀ of 45 nM), PI3Kα/γ (IC₅₀s of 61 nM and 92 nM) and CDK1/CDK2 (IC₅₀s of 32 μM and 7.1 μM) .

HY-13514

TG 100713

2 Publications Verification

PI3K Cancer

TG 100713 is an inhibitor of PI3K, with IC₅₀s of 24, 50, 165, and 215 nM for PI3Kδ, γ, α and β isoforms respectively .

TG 100713 2 Publications Verification	PI3K	Cancer
TG 100713 is an inhibitor of *PI3K, with IC₅₀s of 24, 50, 165, and 215 nM for PI3*Kδ, γ, α and β isoforms respectively .

HY-143403

PI3K-IN-31	PI3K	Cancer
PI3K-IN-31 (Compound 6b) is a potent *PI3K* inhibitor with IC₅₀s of 3.7 nM, 74 nM, 14.6 nM, and 9.9 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ, respectively. PI3K-IN-31 has anticancer effects .

HY-143404

PI3K-IN-30

PI3K Cancer

PI3K-IN-30 (compound 6d) is a potent PI3K inhibitor with IC₅₀s of 5.1, 136, 30.7 and 8.9 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively .

PI3K-IN-30	PI3K	Cancer
PI3K-IN-30 (compound 6d) is a potent *PI3K* inhibitor with IC₅₀s of 5.1, 136, 30.7 and 8.9 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively .

HY-128333

PI3K/mTOR Inhibitor-4	PI3K mTOR	Cancer
PI3K/mTOR Inhibitor-4 is an orally active pan-class I *PI3K/mTOR* inhibitor. PI3K/mTOR Inhibitor-4 has enzymatic inhibition activity for PI3Kα, PI3Kγ, PI3Kδ and mTOR with IC₅₀ values of 0.63 nM, 22 nM, 9.2 nM and 13.85 nM, respectively. PI3K/mTOR Inhibitor-4 can be used for the research of cancer .

HY-13440

AMG 511 2 Publications Verification	PI3K	Cancer
AMG 511 is a potent and orally available pan inhibitor of class I *PI3Ks, with K_is of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα, β, δ and γ, respectively. AMG 511 significantly suppresses PI3*K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 exhibits anti-tumor activity in mouse glioblastoma xenograft model .

HY-124719

hSMG-1 inhibitor 11j 1 Publications Verification	PI3K mTOR GSK-3 CDK	Cancer
hSMG-1 inhibitor 11j, a pyrimidine derivative, is a potent and selective inhibitor of hSMG-1, with an IC₅₀ of 0.11 nM. hSMG-1 inhibitor 11j exhibits >455-fold selectivity for hSMG-1 over mTOR (IC₅₀=50 nM), PI3Kα/γ (IC₅₀=92/60 nM) and CDK1/CDK2 (IC₅₀=32/7.1 μM). hSMG-1 inhibitor 11j can be used for the research of cancer .

HY-139810

ETP-47037	PI3K	Others
ETP-47037 is a potent and inhibitor of PI3Kα isoform with an IC₅₀ value of 0.99 nM. ETP-47037 also inhibits the PI3Kβ, PI3Kδ, and PI3Kγ isoforms, with IC₅₀ values of 49.2, 7.13, and 49.1 nM, respectively. ETP-47037 has the potential for the research of chemical modulation of telomere protection .

HY-10812

GNE-490	PI3K mTOR	Cancer
GNE-490, a (thienopyrimidin-2-yl)aminopyrimidine, is a potent pan-PI3K inhibitor with IC₅₀s of 3.5 nM, 25 nM, 5.2 nM, 15 nM for PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ, respectively. GNE-490 has >200 fold selectivity for mTOR (IC₅₀=750 nM). GNE-490 shows potent suppression efficacy profile against MCF7.1 breast cancer xenograft model .

HY-157295

PI3K/HDAC-IN-3	PI3K HDAC	Cancer
PI3K/HDAC-IN-3 (36) is a *PI3K* and HDAC dual inhibitor, with IC₅₀ values of 0.23 nM and 172 nM for PI3Kα and HDAC1, respectively. PI3K/HDAC-IN-3 (36) suppresses AKT phosphorylation and increased H3 acetylation in MV4-11 cells. PI3K/HDAC-IN-3 (36) exhibits significant and dose-dependent anticancer efficacy in a MV4-11 xenograft model .

HY-123849

SN32976	PI3K mTOR	Cancer
SN32976 is a potent and selective class I *PI3K* and mTOR inhibitor with IC₅₀s of 15.1 nM, 461 nM, 110 nM, 134 nM and 194 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and mTOR, respectively. SN32976 shows high selectivity among other 442 kinases. SN32976 shows anticancer effects .

HY-162349

PARP7/HDACs-IN-1	HDAC PARP	Cancer
PARP7/HDACs-IN-1 (compound 9l) is a dual-target inhibitor targeting PARP7/HDAC with anti-tumor activity. PARP7/HDACs-IN-1 inhibits different subtypes of PARPs and HDACs with IC₅₀s of 83.3 nM (PARP1), 3.1 nM (PARP7), 35 nM (HDAC1), 30.3 nM (HDAC2), 35.4 nM (HDAC3), and 6.4 nM respectively. (HDAC6) . br/ .

HY-146159

PI3K/HDAC-IN-2	PI3K HDAC	Cancer
PI3K/HDAC-IN-2 is a potent dual *PI3K/HDAC* inhibitor with IC₅₀s of 226 nM, 279 nM, 467 nM, 29 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, respectively, and IC₅₀s of 1.3 nM, 3.4 nM, 972 nM, 17 nM, 12 nM for HDAC1, HDAC2, HDC4, HDAC6, HDAC8, respectively. PI3K/HDAC-IN-2 exhibits PI3Kδ and class I and IIb HDAC selectivity. PI3K/HDAC-IN-2 has remarkable anticancer effects .

HY-147419

Vulolisib	PI3K	Cancer
Vulolisib is a potent and orally active phosphatidylinositol 3-kinase (PI3K) inhibitor, with IC₅₀ values of 0.2 nM, 168 nM, 90 nM and 49 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. Antiproliferative and antineoplastic activity .

Brevianamide F 2 Publications Verification Cyclo(L-Pro-L-Trp)	Infection Alkaloids Structural Classification Human Gut Microbiota Metabolites Microorganisms Classification of Application Fields Source classification Endogenous metabolite Disease Research Fields Indole Alkaloids	PI3K Bacterial
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 .

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PI3Kα

Inhibitors & Agonists

NaturalProducts

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