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文献引用
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PI3K inhibitor
AZD6482 是一种 PI3Kbeta 抑制剂(IC50=0.021M),用于抗血栓治疗。- Kevin J Pridham, .et al. , iScience, 2024, May 7;27(6):109921 PMID: 38812542
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PI3K/mTOR Inhibitor
BEZ235(NVP-BEZ235)通过结合到这些酶的ATP结合裂隙,抑制PI3K和mTOR激酶活性。- Lijuan Chen, .et al. , Behav Neurol, 2023, May 9;2023:6991826 PMID: 37200987
- Makoto Koyama, .et al. , Int J Oncol, 2020, Sep 2 PMID: 32901840
- Tzeng SF, .et al. , FASEB J, 2018, Jun 15:fj201800687 PMID: 29906246
- Dominik Schulz, .et al. , Am J Cancer Res, 2016, 6(9): 1963-1975 PMID: 27725902
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PI3K inhibitor
CAL-101 是一种选择性抑制 PI3K 的异构体抑制剂,能够诱导慢性淋巴细胞性白血病(CLL)细胞的凋亡。- Kevin J Pridham, .et al. , iScience, 2024, May 7;27(6):109921 PMID: 38812542
- Ming-Chun Hung, .et al. , Cell Biosci, 2022, 12: 122 PMID: 35918763
- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Pridham KJ, .et al. , Neuro Oncol, 2018, Mar 27;20(4):494-505 PMID: 29016844
- Yoshihiro Umezawa, .et al. , J Biol Chem, 2017, Dec 1; 292(48): 19639-19655 PMID: 28974577
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PI3K inhibitor
GDC-0941 是一种强效、选择性、口服生物利用度的 class I PI3 kinase (PI3K) 抑制剂,其 IC50 值(纳摩尔)分别针对 p110 α、β、δ 和 γ 亚型、DNA-PK 和 mTOR 为 3、33、3、75、1230 和 580。- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Li T, .et al. , Oncogene, 2018, Nov;37(47):6180-6194 PMID: 30013190
- Joo Sang Lee, .et al. , Nat Commun, 2018, 9: 2546 PMID: 29959327
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mTOR/PI3K Inhibitor
GSK1059615 是一种强效的、可逆的、ATP竞争性的、噻唑烷二酮类抑制剂,针对 PI3Kα(IC50 = 2 nM)。- Jing Xie, .et al. , Oncotarget, 2017, Aug 1; 8(31): 50814-50823 PMID: 28881606
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PI3K Inhibitor
LY294002 是一种 PI3k 抑制剂(细胞 IC50 约为 10 μM)和 casein kinase II 抑制剂。- Yinhua Ni, .et al. , J Agric Food Chem, 2024, Jul 31;72(30):16708-16725 PMID: 39016108
- Yinhua Ni, .et al. , J Nutr Biochem, 2024, Mar:125:109569 PMID: 38185346
- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Nahla E. El-Ashmawy, .et al. , Clin Phytosci, 2022, 8: 20
- Ming-Chun Hung, .et al. , Cell Biosci, 2022, 12: 122 PMID: 35918763
- Chien-Feng Li, .et al. , Cell Oncol (Dordr), 2021, Aug 2 PMID: 34339014
- Hiroharu Sakai, .et al. , Exp Ther Med, 2021, March 5 PMID: 33747195
- Cheng Zhou, .et al. , Cell Death Dis, 2021, Mar 3;12(3):231 PMID: 33658491
- Daniel Limonta, .et al. , J Infect Dis, 2019, 2019 PMID: 30799482
- Lv H, .et al. , J Cell Physiol, 2018, Oct 26 PMID: 30362547
- Hui Liang, .et al. , Sci Rep, 2017, 7: 40361 PMID: 28098170
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PI3K Inhibitor
PI-103 是一种强效的、细胞渗透性的、ATP竞争性抑制剂,针对磷脂酰肌醇3激酶(PI3K)家族成员具有选择性,特别是对 DNA-PK、PI3K (p110α) 和 mTOR。- Diane Yang, .et al. , Diabetes, 2021, Oct;70(10):2419-2429 PMID: 34344789
- Byungki Jang, .et al. , Int J Mol Sci, 2017, Nov; 18(11): 2258 PMID: 29077055
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PI3K Inhibitor
PIK-75 是一种咪唑吡啶类化合物,能够选择性地抑制 p110α,其 IC50 值为 5.8 nM。它对 p110γ 和 p110β 的抑制效果相对较弱,其 IC50 值分别为 0.076 μM 和 1.3 μM。- Pridham KJ, .et al. , Neuro Oncol, 2018, Mar 27;20(4):494-505 PMID: 29016844
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MAO-B inhibitor
Quercetin 抑制多种酶系统,包括酪氨酸蛋白激酶、磷脂酶A2、磷酸二酯酶、线粒体ATP酶、PI 3-激酶和蛋白激酶C。 -
MAO-B inhibitor
槲皮素能够抑制多种酶系统,包括酪氨酸蛋白激酶、磷脂酶A2、磷酸二酯酶、线粒体ATP酶、PI 3-激酶和蛋白激酶C。 -
PI3K/mTOR inhibitor
Desmethyl-VS-5584 是 VS-5584 的去甲基类似物,VS-5584 是一种新型且高度选择性的 PI3K/mTOR 激酶抑制剂,用于治疗癌症。 -
PI3K Inhibitor
TGX-221 是一种强效、选择性且能渗透细胞的 PI3K p110β 抑制剂。- Kevin J Pridham, .et al. , iScience, 2024, May 7;27(6):109921 PMID: 38812542
- Mostafa Khater, .et al. , J Biol Chem, 2021, Jan-Jun, 296:100805 PMID: 34022220
- Mostafa Khater, .et al. , J Biol Chem, 2021, Jan 22;296:100325 PMID: 33493514
- Pridham KJ, .et al. , Neuro Oncol, 2018, Mar 27;20(4):494-505 PMID: 29016844
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PI3K Inhibitor
XL147 是一种强效、选择性且可口服生物利用的小分子抑制剂,针对 I类磷脂酰肌醇3激酶(PI3K),具有潜在的抗肿瘤活性。- Yushi Hayashida, .et al. , Int J Cancer, 2016, Aug 1;139(3):700-11 PMID: 26989815
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PI3K inhibitor
ZSTK474 是一种 ATP-竞争性抑制剂,针对 class I 磷脂酰肌醇 3 激酶 各种亚型。- Pridham KJ, .et al. , Neuro Oncol, 2018, Mar 27;20(4):494-505 PMID: 29016844
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PI3K Inhibitor?€?
BKM120(NVP-BKM120)是一种生物可利用的特异性口服全类别I磷脂酰肌醇3激酶(PI3K)激酶抑制剂。- Kevin J Pridham, .et al. , iScience, 2024, May 7;27(6):109921 PMID: 38812542
- Danielle H Oh, .et al. , PNAS, 2023, Sep 5;120(36):e2306414120 PMID: 37643213
- Giri R. Gnawali, .et al. , Medicinal Chemistry Research, 2022, 31: 1154-1175
- Yusuke Murase, .et al. , Oncol Rep, 2022, Apr;47(4):61 PMID: 35088890
- Jeremiah J Bearss, .et al. , EMBO Rep, 2021, Apr 7;22(4):e50835 PMID: 33586867
- Takaaki Fujimura, .et al. , Cancer Biol Ther, 2020, Sep 1;21(9):863-870 PMID: 32835580
- Nachi Namatame, .et al. , Oncotarget, 2018, Oct 12; 9(80): 35141-35161 PMID: 30416685
- Jin H. Song, .et al. , Mol Cancer Ther, 2018, Dec;17(12):2710-2721 PMID: 30190422
- Saijo A, .et al. , Cancer Lett, 2018, May 1;421:17-27 PMID: 29448000
- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Pridham KJ, .et al. , Neuro Oncol, 2018, Mar 27;20(4):494-505 PMID: 29016844
- Charles-André Philip, .et al. , BMC Cancer, 2017, 17: 638 PMID: 28886696
- Rogers HA, .et al. , Clin Cancer Res., 2013, Dec 1;19(23):6450-60 PMID: 24077346
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mTOR/PI3K Inhibitor
GDC-0980 (RG7422) 是一种选择性的、高效的、口服生物利用度的抑制剂,针对 Class I PI3激酶 和 mTOR激酶 (TORC1/2),在体外的半抑制浓度(IC50)分别为 p110 α、β、δ 和 γ 亚型的 5、27、7 和 14 nM。- Kasun Wanigasooriya, .et al. , Front Oncol, 2022, Jul 4;12:920444 PMID: 35860583
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PI3K/mTOR Inhibitor
PF-04691502 是一种 PI3K/mTOR 激酶抑制剂,同时也是针对 磷脂酰肌醇3激酶(PI3K) 和 哺乳动物雷帕霉素靶蛋白(mTOR) 的药物,作用于 PI3K/mTOR 信号通路。- Yusuke Murase, .et al. , Oncol Rep, 2022, Apr;47(4):61 PMID: 35088890
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mTOR/PI3K Inhibitor,
GSK2126458 是一种高效、口服生物利用度的 PI3Kα 和 mTOR 抑制剂,在体内药效动力学和肿瘤生长效能模型中均显示活性。 -
PI3K Inhibitor
YM201636 是一种细胞渗透性和选择性的 PIKfyve 抑制剂(IC50 = 33 nM)。- Krishna Chintaluri, .et al. , PLoS One, 2018, 13(6): e0198454 PMID: 29870544
- Dayam RM, .et al. , J Immunol, 2017, Sep 15;199(6):2096-2105 PMID: 28779020
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PI3K/mTOR inhibitor
PKI-587 是一种高效的 PI3K/mTOR 激酶抑制剂,能够抑制 PI3K-α, β, γ, δ 各种亚型和 mTOR,其半抑制浓度(IC50)分别为 0.4, 6.0, 5.4, 6.0 和 1.6 nM。- Yusuke Murase, .et al. , Oncol Rep, 2022, Apr;47(4):61 PMID: 35088890
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DNA-PK inhibitor
NU-7441 (KU-57788) 是一种强效且选择性的 DNA依赖性蛋白激酶(DNA-PK)抑制剂。其半抑制浓度(IC50)值分别为 DNA-PK 14 nM、mTOR 1700 nM、PI 3-K 5000 nM、ATM >100000 nM 和 ATR >100000 nM。- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Ryo Sakasai, .et al. , Biochem Biophys Res Commun, 2023, Aug 6;668:42-48 PMID: 37244033
- Shahar Biechonski, .et al. , Sci Rep, 2018, Apr 17 PMID: 29666389
- Ihara M, .et al. , J Radiat Res, 2018, Nov 23 PMID: 30476230
- Chwastek J, .et al. , Int J Biochem Cell Biol, 2017, Jun;87:38-53 PMID: 28341201
- Masaaki Yanai, .et al. , Yonago Acta Med, 2017, Mar; 60(1): 9-15 PMID: 28331416
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Autophagy/PI3K Inhibitor
3-甲基腺嘌呤是III类磷脂酰肌醇3激酶(PI 3-激酶)的抑制剂。- Yu-Chih Hsu, .et al. , Int J Med Sci, 2023, 20(4): 444-454 PMID: 37057216
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PI3K/HDAC inhibitor
CUDC-907(Fimepinostat)是一种小分子抑制剂,能够同时针对PI3K和HDAC。CUDC-907比单一的PI3K抑制剂、HDAC抑制剂或这两种单一药物的最大耐受剂量组合更有效。- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Caner Gunayd?n, .et al. , Immunopharmacol Immunotoxicol, 2022, Jun;44(3):447-455 PMID: 35291899
- Chie Ishikawa, .et al. , Eur J Haematol, 2020, Eur J Haematol PMID: 32780889
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PI3K inhibitor
Wortmannin 是一种强效、选择性、细胞渗透性和不可逆的磷脂酰肌醇3激酶(PI 3-kinase)抑制剂(IC50 = 2 - 4 nM),同时也强效抑制polo样激酶1(PLK1)(IC50 = 5.8 nM)。- Weili Chen, .et al. , Communications Biology, 2024, 7:488
- Hirotake Ishida, .et al. , J Neurosci, 2021, Oct 13;41(41):8494-8507 PMID: 34452938
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PI3K inhibitor
PX-866 是一种小分子沃特曼宁类似物,能够抑制磷脂酰肌醇3激酶(PI3K)的α、γ和δ亚型,具有潜在的抗肿瘤活性。 -
dual PI3K and mTOR kinase inhibitor
Dactolisib Tosylate (BEZ235 Tosylate) 是一种双重 PI3K 和 mTOR 激酶抑制剂,其 IC50 值分别针对 PI3Kα, β, γ, δ 为 4, 75, 7, 5 nM。Dactolisib Tosylate (BEZ235 Tosylate) 抑制 mTORC1 和 mTORC2。 -
PI3K Inhibitor
BLY719 是一种口服生物利用度的磷脂酰肌醇3激酶(PI3K)抑制剂,具有潜在的抗肿瘤活性。- Natasa Stojanovic Guzvic, .et al. , Mol Oncol, 2024, Oct 5 PMID: 39367702
- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
- Kevin J Pridham, .et al. , iScience, 2024, May 7;27(6):109921 PMID: 38812542
- Elaheh S Abutorabi, .et al. , Mol Biol Rep, 2023, May;50(5):4073-4082 PMID: 36877344
- Lisann Pelzl, .et al. , J Thromb Haemost, 2022, Feb;20(2):387-398 PMID: 34752677
- J Wei, .et al. , bioRxiv, 2018, 2018
- Pridham KJ, .et al. , Neuro Oncol, 2018, Mar 27;20(4):494-505 PMID: 29016844
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PI3K inhibitor
CZC24832 是一种选择性的 PI 3-激酶γ抑制剂(在 PI 3-Kγ依赖的 fMLP 诱导的中性粒细胞迁移实验中,IC50 = 1.0 μM)。- Kevin J Pridham, .et al. , iScience, 2024, May 7;27(6):109921 PMID: 38812542
- Yoshihiro Umezawa, .et al. , J Biol Chem, 2017, Dec 1; 292(48): 19639-19655 PMID: 28974577
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PI3Kα/δ inhibitor
Pictilisib 二甲磺酸盐(GDC-0941 二甲磺酸盐)是一种强效的 PI3Kα/δ 抑制剂,其 IC50 为 3 nM,对 p110β(11倍)和 p110γ(25倍)具有适度的选择性。 -
PI3K/PDK-1 Inhibitor
NVP-BAG956 作为一种强效、可逆的、与ATP竞争的 PI 3-K/PDK1 双激酶抑制剂,对 VEGFR1 的抑制效力较低(IC50 = 2.56 uM),对其他15种激酶的活性几乎没有或完全没有(IC50 >10 uM)。 -
PI3K inhibitor
BAY 80-6946 是一种具有潜在抗肿瘤活性的磷脂酰肌醇3激酶(PI3K)抑制剂。- Shin SM, .et al. , Sci Adv, 2020, Jan 15;6(3):eaay2174 PMID: 31998840
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PI3K Inhibitor
GSK2636771 是一种强效的、口服生物利用度高的、PI3K beta选择性抑制剂。- Sarah E Conduit, .et al. , Nat Commun, 2024, Aug 21;15(1):7181 PMID: 39168978
- Pridham KJ, .et al. , Neuro Oncol, 2018, Mar 27;20(4):494-505 PMID: 29016844
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PI3K-δ/PI3K-γ inhibitor
IPI-145,亦称为 INK-1197,是一种口服生物利用度高、选择性强且效力高的小分子抑制剂,针对磷脂酰肌醇-3激酶(PI3K)的 delta 和 gamma 亚型,具有潜在的免疫调节和抗肿瘤活性。