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Search Results for " phosphatidylinositol 3-kinase "

34

抑制剂 & 化合物

5

天然产物

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Cat. No. Product Name Target Signaling Pathways
T13386 Zandelisib

PI3K PI3K/Akt/mTOR signaling
Zandelisib 是PI3K 抑制剂,对p110δ选择性抑制,IC50为 3.5 nM。它显示出抗肿瘤作用。
T2616 PIK-93

PIK 93

ATM/ATR; DNA-PK; Virus Protease; PI3K; Carbonic Anhydrase; PI4K; mTOR; HSV DNA Damage/DNA Repair; Metabolism; Microbiology/Virology; PI3K/Akt/mTOR signaling
PIK-93 是一种合成的PI4KIIIβ抑制剂,IC50值为 19 nM,同时可抑制PI3Kγ和PI3Kα的活性,IC50值分别为 16 nM 和 39 nM。
T12469 PI4KIIIbeta-IN-9

PI3K; PI4K PI3K/Akt/mTOR signaling
PI4KIIIbeta-IN-9 是一种 PI4KIIIβ抑制剂,其 IC50=7 nM。它也抑制 PI3Kδ (IC50:125 nM) 和 PI3Kγ (IC50:1046 nM)。
T19840 GSK-F1

PI4KA inhibitor-F1

PI4K PI3K/Akt/mTOR signaling
GSK-F1 (PI4KA inhibitor-F1) 是一种新型强效 PI4KA 抑制剂。
T4079 LY-294002 hydrochloride

SF 1101,LY 294002,NSC 697286

PI3K PI3K/Akt/mTOR signaling
LY-294002 hydrochloride (NSC 697286) 是一种合成的 PI3Kα/δ/β 分子抑制剂(IC50:0.5/0.57/0.97 μM,在无细胞试验中);在溶液中比 Wortmannin 更稳定,也是自噬体形成的阻断剂。
T28416 PIK-108

PIK 108,PIK108

PI3K PI3K/Akt/mTOR signaling
PIK-108 是选择性的、变构的、非 ATP 竞争性的 p110β/p110δ 抑制剂。
T12365 PARP/PI3K-IN-1

PARP; PI3K Chromatin/Epigenetic; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
PARP/PI3K-IN-1 是一种 新型双重聚(ADP-核糖)聚合酶(PARP)和磷酸肌醇 3-激酶(PI3K)双重抑制剂,具有抗癌、抗肿瘤和抗癌细胞增殖活性,可用于研究乳腺癌、胰腺癌和肺癌。
T1999 Taselisib

RG-7604,GDC-0032

PI3K; Carbonic Anhydrase Metabolism; PI3K/Akt/mTOR signaling
Taselisib (GDC-0032) 是 PI3K 抑制剂,靶向作用于突变 PI3KCA。它能够抑制 PI3Kα (IC50:0.29 nM),PI3Kβ (IC50:0.91 nM) 和 PI3Kγ (IC50:0.97 nM)。
T16528 PI-828

LY 294002, 4gamma-NH2

Casein Kinase; PI3K Metabolism; PI3K/Akt/mTOR signaling; Stem Cells
PI-828 是磷脂酰肌醇3-激酶(PI3K)抑制剂,广泛用于研究 PI3K 的生理功能,也可促进干细胞向中胚层分化。
T1861 Omipalisib

GSK458,GSK2126458

PI3K; mTOR; Autophagy Autophagy; PI3K/Akt/mTOR signaling
Omipalisib (GSK2126458) 是一种磷脂酰肌醇 3-激酶(PI3K) 的小分子吡啶磺酰胺抑制剂,具有抗肿瘤活性。它抑制 p110α/β/δ/γ,mTORC1/2 的活性,Ki 值分别为 0.019 nM/0.13 nM/0.024 nM/0.06 nM 和 0.18 nM/0.3 nM。
T67703 mTOR inhibitor 9b

mTOR PI3K/Akt/mTOR signaling
mTOR inhibitor 9b 是一种酶抑制剂,对蛋白激酶mTOR 和磷脂酰肌醇 3-激酶 PIK3CA 具有抑制作用,IC50分别为 0.76nm 和1.262 µM。mTOR inhibitor 9b 具有抗癌活性,可用来研究白血病、皮肤癌、乳腺癌、肺癌和结肠癌。
T6168 ZSTK474

PI3K; Autophagy Autophagy; PI3K/Akt/mTOR signaling
ZSTK474 是 ATP 竞争性的泛 I 类PI3K 抑制剂,抑制 PI3Kα、PI3Kβ、PI3Kδ 和 PI3Kγ,IC50分别为 16 nM、44 nM、4.6 nM 和 49 nM。它是一种可口服的 s-三嗪衍生物,具有抗肿瘤活性。
T36083 DS-7423

PI3K; mTOR PI3K/Akt/mTOR signaling
DS-7423 是PI3K 和mTOR 的有效抑制剂,抑制PI3Kα 和 mTOR 的IC50分别为15.6 nM 和 34.9 nM。DS-7423表现出抗癌活性。
T67702 mTOR inhibitor 9d

PI3K; mTOR PI3K/Akt/mTOR signaling
mTOR inhibitor 9d 是一种蛋白激酶 mTOR 和PI3K 双重抑制剂,对mTOR 的IC50值为0.31nm,可用于治疗白血病、皮肤癌、乳腺癌、肺癌和结肠癌。
T69912 AS2541019

AS2541019 is a selective Phosphatidylinositol-3-kinase p110δ (PI3Kδ) inhibitor.
T39581 PI3K-IN-19 hydrochloride

PI3K-IN-19 hydrochloride

PI3K-IN-19 hydrochloride (WO2017153220, step 5) acts as a phosphatidylinositol-3-kinase (PI3K) inhibitor.
T24637 PI3K inhibitor C 96

PI3K IN C96,PI3K-IN-C96

PI3K inhibitor C 96 is an inhibitor of phosphatidylinositol 3-kinase. It shows effective activity against multiple myeloma in vitro and in vivo.
T71798 Demethoxyviridiol

Demethoxyviridiol is a mycotoxin that inhibits phosphatidylinositol 3-kinase (PI3K).
T28627 RV-1729

RV1729

RV-1729, a phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K) inhibitor, is used potentially for the treatment of asthma.
T27526 Halenaquinone

Halenaquinone is a phosphatidylinositol 3-kinase inhibitor. Halenaquinone specifically inhibits the secondary DNA binding of RAD51. Halenaquinone inhibits RANKL-induced osteoclastogenesis. Halenaquinone induces apoptosis in PC12 cells.
T29159 WJD008

WJD-008,WJD 008

WJD008 is a dual inhibitor of phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin. WJD008 prevents PI3K signaling and inhibits the proliferation of transformed cells with oncogenic PI3K mutant. WJD008 has antiproliferative and anticlonogeni
T27157 Dezapelisib

INCB-040093,INCB 040093,INCB040093

Dezapelisib is an orally bioavailable, selective inhibitor of the delta isoform of the 110 kDa catalytic subunit of class I phosphoinositide-3 kinases (PI3K). INCB040093 prevents both the production of the second messenger phosphatidylinositol-3,4,5-trisp
T72071 WAY-299017

Antibacterial Microbiology/Virology
WAY-299017是一种强效且具有选择性的UPPS 抑制剂,可用于治疗细菌感染。
T70352 PH11

PH11 is a novel Focal Adhesion Kinase (FAK) inhibitor. PH11 restores TRAIL apoptotic pathway in PANC-1 cells through down-regulation of c-FLIP via inhibition of FAK and the phosphatidylinositol-3 kinase (PI3K)/AKT pathways. Tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) emerges as one of the most-promising experimental cancer therapeutic drugs and is currently being tested in clinical trials. However, both intrinsic and acquired resistance of human cancer cells to TRAIL...
T62273 Vulolisib

Vulolisib 是一种口服具有活力、有效的磷脂酰肌醇 3 激酶 (PI3K) 抑制剂,能够作用于 PI3Kα (IC50: 0.2 nM)、PI3Kβ (IC50: 168 nM)、PI3Kγ (IC50: 90 nM)、 PI3Kδ (IC50: 49 nM)。Vulolisib 具有抗肿瘤活性,对癌细胞表现出抗增殖活性。
T37029 PtdIns-(3,4,5)-P3-biotin (sodium salt)

PtdIns-(3,4,5)-P3-biotin (sodium salt)

The PtdIn phosphates play an important role in the generation and transduction of intracellular signals. PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.
T60980 PIKfyve-IN-1

PIKfyve-IN-1 是具有细胞活性的、高效的化学探针,可用于病毒学中 PIKfyve 的研究。PIKfyve-IN-1 可抑制 3 磷酸磷脂酰肌醇 5-激酶 (PIKfyve) (IC50 = 6.9 nM)。
T35525 PI3-Kinase α Inhibitor 2

PI3-Kinase α Inhibitor 2

Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of the 3' hydroxyl position of PIs to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3. PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits, whereas PI3Kγ is a class 1B PI3K composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit. PI3Kα inhibitor 2 is a selective inhibitor of PI3Kα with IC50 values of 2, 16, 660, and 220 nM for the α, β, γ, and 2Cβ isoforms, respectively. It...
T36349 CGP 74514 dihydrochloride

Potent cdk1 inhibitor (IC50 = 25 nM). Reduces Akt phosphorylation and increases mitochondrial damage in leukemia cells in vitro in combination with LY 294002. Yu et al (2013) The lethal effects of pharmacological cyclin-dependent kinase inhibitors in human leukemia cells proceed through a phosphatidylinositol 3-kinase/Akt-dependent process. Cancer Res. 63 1822 PMID:12702569 |Furet et al (2000) Structure-based design of potent CDK1 inhibitors derived from olomoucine. J.Comput.Aided Mol.Des. 14 40...
T36844 Inostamycin A

Inostamycin A is a bacterial metabolite that has been found inStreptomycesand has anticancer activity.1It is an inhibitor of CDP-diacylglycerol:inositol 3-phosphatidyltransferase (IC50= 0.02 μg/ml in A431 cell membranes) and is selective for CDP-diacylglycerol:inositol 3-phosphatidyltransferase over phospholipase C (PLC) and phosphatidylinositol kinase at 10 μg/ml.2Inostamycin A decreases viability of YCU-T892, KCC-TC873, KB, HSC-4, and YCU-T891 oral squamous cell carcinoma (OSCC) cells in a con...
T37691 Phosphatidic Acids (egg) (ammonium salt)

Phosphatidic acid is a phospholipid and an intermediate in glycerolipid biosynthesis. It is a transient intermediate in the synthesis of various phospholipid species that is synthesized de novo in cells via multiple routes, including the glycerol-3 phosphate and dihydroxyacetone phosphate pathways, enzymatic conversion of phosphatidylcholine by phospholipase D, and acetylation of lysophosphatidic acid by lysoPA-acyltransferase, among others. It has roles in shaping cellular membranes, cellular ...
T35933 D-myo-Inositol-1,4,5,6-tetraphosphate (sodium salt)

D-myo-Inositol-1,4,5,6-tetraphosphate (sodium salt),Ins(1,4,5,6)-P4

D-myo-Inositol-1,4,5,6-tetrahosphate (sodium salt) (Ins(1,4,5,6)-P4) is one of several different inositol oligophosphate isomers implicated in signal transduction. Production of Ins(1,4,5,6)-P4 by intestinal epithelial cells increases approximately 2-14 fold, depending on the strain and incubation time, following infection with Salmonella.[1] D-myo-Inositol-1,4,5,6-tetraphosphate (sodium salt) (Ins(1,4,5,6)-P4) is one of several different inositol oligophosphate isomers implicated in signal tran...
T35491 3,5-dimethyl PIT-1

PtdIns-(3,4,5)-P3 (PIP3) serves as an anchor for the binding of signal transduction proteins bearing pleckstrin homology (PH) domains such as phosphatidylinositol 3-kinase (PI3K) or PTEN. Protein binding to PIP3 is important for cytoskeletal rearrangement and membrane trafficking and initiates an intricate signaling cascade that has been implicated in cancer. 3,5-dimethyl PIT-1 is a dimethyl analog of PIT-1, the selective inhibitor of PIP3/Akt PH domain binding, that is designed for more favorab...
T36084 PKI-179

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[1][2]. PKI-179 inhibits the cell proliferation, with IC50s of 22 nM and 29 nM for MDA361 and PC3 cells, respectively[1].PKI-179 shows inhibitory activity against a panel of 361 other ...

化合物

Zandelisib
Cat.No: T13386
Synonym:
Target: PI3K
PIK-93
Cat.No: T2616
Synonym: PIK 93
Target: ATM/ATR, DNA-PK, Virus Protease, PI3K, Carbonic Anhydrase, PI4K, mTOR, HSV
PI4KIIIbeta-IN-9
Cat.No: T12469
Synonym:
Target: PI3K, PI4K
GSK-F1
Cat.No: T19840
Synonym: PI4KA inhibitor-F1
Target: PI4K
LY-294002 hydrochloride
Cat.No: T4079
Synonym: SF 1101,LY 294002,NSC 697286
Target: PI3K
PIK-108
Cat.No: T28416
Synonym: PIK 108,PIK108
Target: PI3K
PARP/PI3K-IN-1
Cat.No: T12365
Synonym:
Target: PARP, PI3K
Taselisib
Cat.No: T1999
Synonym: RG-7604,GDC-0032
Target: PI3K, Carbonic Anhydrase
PI-828
Cat.No: T16528
Synonym: LY 294002, 4gamma-NH2
Target: Casein Kinase, PI3K
Omipalisib
Cat.No: T1861
Synonym: GSK458,GSK2126458
Target: PI3K, mTOR, Autophagy
mTOR inhibitor 9b
Cat.No: T67703
Synonym:
Target: mTOR
ZSTK474
Cat.No: T6168
Synonym:
Target: PI3K, Autophagy
DS-7423
Cat.No: T36083
Synonym:
Target: PI3K, mTOR
mTOR inhibitor 9d
Cat.No: T67702
Synonym:
Target: PI3K, mTOR
AS2541019
Cat.No: T69912
Synonym:
Target:
PI3K-IN-19 hydrochloride
Cat.No: T39581
Synonym: PI3K-IN-19 hydrochloride
Target:
PI3K inhibitor C 96
Cat.No: T24637
Synonym: PI3K IN C96,PI3K-IN-C96
Target:
Demethoxyviridiol
Cat.No: T71798
Synonym:
Target:
RV-1729
Cat.No: T28627
Synonym: RV1729
Target:
Halenaquinone
Cat.No: T27526
Synonym:
Target:
WJD008
Cat.No: T29159
Synonym: WJD-008,WJD 008
Target:
Dezapelisib
Cat.No: T27157
Synonym: INCB-040093,INCB 040093,INCB040093
Target:
WAY-299017
Cat.No: T72071
Synonym:
Target: Antibacterial
PH11
Cat.No: T70352
Synonym:
Target:
Vulolisib
Cat.No: T62273
Synonym:
Target:
PtdIns-(3,4,5)-P3-biotin (sodium salt)
Cat.No: T37029
Synonym: PtdIns-(3,4,5)-P3-biotin (sodium salt)
Target:
PIKfyve-IN-1
Cat.No: T60980
Synonym:
Target:
PI3-Kinase α Inhibitor 2
Cat.No: T35525
Synonym: PI3-Kinase α Inhibitor 2
Target:
CGP 74514 dihydrochloride
Cat.No: T36349
Synonym:
Target:
Inostamycin A
Cat.No: T36844
Synonym:
Target:
Phosphatidic Acids (egg) (ammonium salt)
Cat.No: T37691
Synonym:
Target:
D-myo-Inositol-1,4,5,6-tetraphosphate (sodium salt)
Cat.No: T35933
Synonym: D-myo-Inositol-1,4,5,6-tetraphosphate (sodium salt),Ins(1,4,5,6)-P4
Target:
3,5-dimethyl PIT-1
Cat.No: T35491
Synonym:
Target:
PKI-179
Cat.No: T36084
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T3399 Psoralidin

Others; Estrogen/progestogen Receptor; Reactive Oxygen Species; Lipoxygenase; Gamma-secretase; Akt; COX; Antibacterial Cytoskeletal Signaling; Endocrinology/Hormones; Immunology/Inflammation; Metabolism; Microbiology/Virology; Neuroscience; NF-κB; Others; PI3K/Akt/mTOR signaling; Proteases/Proteasome; Stem Cells
Psoralidin 是COX-2和5-LOX 的抑制剂,有抗癌,抗菌和抗炎作用。它显著下调NOTCH1信号传导,还极大地诱导活化氧产生。
TN2019 Orobol

3'-Hydroxygenistein,3’,4’,5,7-tetrahydroxy-isoflavon,3',4',5,7-四羟基异黄酮

BCL; Caspase; PI3K Apoptosis; PI3K/Akt/mTOR signaling; Proteases/Proteasome
Orobol (3’,4’,5,7-tetrahydroxy-isoflavon) 是酪氨酸特异性蛋白激酶和磷脂酰肌醇转换的抑制剂。Orobol 抑制 PI3K,对 PI3K α/β/γ/K/δ 的 IC50 为 3.46-5.27 μM。 Orobol 具有抗皮肤老化和抗肥胖的作用。
T4S21320 ISOGINKGETIN

异银杏素,4',4'''-Dimethylamentoflavone,异银杏双黄酮

MMP; Others Others; Proteases/Proteasome
ISOGINKGETIN (4',4'''-Dimethylamentoflavone) 是一种MMP9抑制剂,也是一种Pre-mRNA Splicing 抑制剂。
T73812 Phosphatidylinositol 4,5-bisphosphate

Phosphatidylinositol 4,5-bisphosphate(L-alpha-Phosphatidylinositol-4,5-bisphosphate)为细胞膜磷脂成分,主要作为磷脂酶C(PLC)与磷酸肌醇3-激酶(PI3K)的底物,充当重要信使。
TMA0291 Dehydroglyasperin D

GSK-3; p38 MAPK; ROS; Akt; COX; PI3K; DNA/RNA Synthesis; Prostaglandin Receptor; JNK Cell Cycle/Checkpoint; Cytoskeletal Signaling; DNA Damage/DNA Repair; GPCR/G Protein; Immunology/Inflammation; MAPK; Neuroscience; PI3K/Akt/mTOR signaling; Stem Cells
Dehydroglyasperin D exhibits anticancer, anti-inflammatory, anti-obesity, antioxidant and anti-aldose reductase effects, it inhibits the proliferation of HT-29 human colorectal cancer cells through direct interaction with phosphatidylinositol 3-kinase; it also mediates suppression of both COX-2 expression and the MLK3 signalling pathway through direct binding and inhibition of MLK3. Dehydroglyasperin D shows strong ferric reducing activities and effectively scavenged DPPH, ABTS(+), and singlet o...

天然产物

Psoralidin
Cat.No: T3399
Synonym:
Target: Others, Estrogen/progestogen Receptor, Reactive Oxygen Species, Lipoxygenase, Gamma-secretase, Akt, COX, Antibacterial
Orobol
Cat.No: TN2019
Synonym: 3'-Hydroxygenistein,3’,4’,5,7-tetrahydroxy-isoflavon,3',4',5,7-四羟基异黄酮
Target: BCL, Caspase, PI3K
ISOGINKGETIN
Cat.No: T4S21320
Synonym: 异银杏素,4',4'''-Dimethylamentoflavone,异银杏双黄酮
Target: MMP, Others
Phosphatidylinositol 4,5-bisphosphate
Cat.No: T73812
Synonym:
Target:
Dehydroglyasperin D
Cat.No: TMA0291
Synonym:
Target: GSK-3, p38 MAPK, ROS, Akt, COX, PI3K, DNA/RNA Synthesis, Prostaglandin Receptor, JNK
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