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BKM120 (NVP-BKM120, Buparlisib)

Catalog No. A11016
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PI3K 抑制剂?

BKM120 (NVP-BKM120,Buparlisib)是生物可利用的口服泛I类磷脂酰肌醇3激酶（PI3K）激酶抑制剂，在无细胞试验中作用于p110α/β/δ/γ的。对VPS34，mTOR，DNAPK的作用效果下降，而对 PI4Kβ几乎没有活性。了解更多

Product Citations (11)

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- Giri R. Gnawali, .et al. Synthesis of 2-oxoquinoline derivatives as dual pim and mTORC protein kinase inhibitors, Medicinal Chemistry Research, 2022, 31: 1154-1175
- Yusuke Murase, .et al. Antitumor activity of the dual PI3K/mTOR inhibitor gedatolisib and the involvement of ABCB1 in gedatolisib resistance in canine tumor cells, Oncol Rep, 2022, Apr;47(4):61 PMID: 35088890
- Jeremiah J Bearss, .et al. EDC3 phosphorylation regulates growth and invasion through controlling P-body formation and dynamics, EMBO Rep, 2021, Apr 7;22(4):e50835 PMID: 33586867
- Takaaki Fujimura, .et al. Enhanced antitumor effect of alectinib in combination with cyclin-dependent kinase 4/6 inhibitor against RET-fusion-positive non-small cell lung cancer cells, Cancer Biol Ther, 2020, Sep 1;21(9):863-870 PMID: 32835580
- Nachi Namatame, .et al. Antitumor profile of the PI3K inhibitor ZSTK474 in human sarcoma cell lines, Oncotarget, 2018, Oct 12; 9(80): 35141-35161 PMID: 30416685
- Jin H. Song, .et al. Mechanisms Behind Resistance to PI3K Inhibitor Treatment Induced by the PIM Kinase, Mol Cancer Ther, 2018, Dec;17(12):2710-2721 PMID: 30190422
- Saijo A, .et al. Bone marrow-derived fibrocytes promote stem cell-like properties of lung cancer cells, Cancer Lett, 2018, May 1;421:17-27 PMID: 29448000
- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Pridham KJ, .et al. PIK3CB/p110β is a selective survival factor for glioblastoma, Neuro Oncol, 2018, Mar 27;20(4):494-505 PMID: 29016844
- Charles-André Philip, .et al. Inhibition of PI3K-AKT-mTOR pathway sensitizes endometrial cancer cell lines to PARP inhibitors, BMC Cancer, 2017, 17: 638 PMID: 28886696
- Rogers HA, .et al. PI3K pathway activation provides a novel therapeutic target for pediatric ependymoma and is an independent marker of progression-free survival., Clin Cancer Res., 2013, Dec 1;19(23):6450-60 PMID: 24077346
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Bortezomib (Velcade)

Catalog No. A10160
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Proteasome 抑制剂

Bortezomib (Velcade)是26S蛋白酶体的高度选择性，可逆抑制剂。了解更多

Product Citations (13)

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- Yoshitaka Sato, .et al. Epstein-Barr virus tegument protein BGLF2 in exosomes released from virus-producing cells facilitates de novo infection, Cell Commun Signal, 2022, Jun 21;20(1):95 PMID: 35729616
- Shin-Ichi Makino, .et al. Impairment of Proteasome Function in Podocytes Leads to CKD, J Am Soc Nephrol, 2021, Mar;32(3):597-613 PMID: 33510039
- Yusuke Yamashita, .et al. Targeting Adaptive IRE1α Signaling and PLK2 in Multiple Myeloma: Possible Anti-Tumor Mechanisms of KIRA8 and Nilotinib, Int J Mol Sci, 2020, Sep; 21(17): 6314 PMID: 32878237
- Nandini Verma, .et al. Synthetic lethal combination targeting BET uncovered intrinsic susceptibility of TNBC to ferroptosis, Sci Adv, 2020, 6 : eaba8968
- A Hayano, .et al. Cell-type-specific sensitivity of bortezomib in the methotrexate-resistant primary central nervous system lymphoma cells, Int J Clin Oncol, 2019, 1-10 PMID: 30993483
- Hiroshi Fukamachi, .et al. A subset of diffuse-type gastric cancer is susceptible to mTOR inhibitors and checkpoint inhibitors, J Exp Clin Cancer Res, 2019, 38:127 PMID: 30866995
- Y Sato, .et al. S-like phase CDKs stabilize the Epstein-Barr virus BDLF4 protein to temporally control late gene transcription, J Virol, 2019, Jan 30. pii: JVI.01707-18 PMID: 30700607
- Takashi Azuma, .et al. Removal of pharmaceuticals in water by introduction of ozonated microbubbles, SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Wenhan Deng, .et al. Variable Responses of MYC Translocation Positive Lymphoma Cell Lines To Different Combinations of Novel Agents: Impact of BCL2 Family Protein Expression, Transl Oncol, 2018, Oct; 11(5): 1147-1154 PMID: 30055346
- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Hokyung K. Chung, .et al. Tunable and reversible drug control of protein production via a self-excising degron, Nat Chem Biol, 2015, Sep; 11(9): 713-720 PMID: 26214256
- S Raz, .et al. Severe hypoxia induces complete antifolate resistance in carcinoma cells due to cell cycle arrest, Cell Death Dis., 2014, 5(2): e1067 PMID: 24556682
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BTZ043 (BTZ038, BTZ044) Racemate

Catalog No. A10165
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DprE1 抑制剂

BTZ043 (BTZ038,BTZ044) Racemate 抑制癸二烯基磷酸基-β-d-核糖2α-表异构酶，它是一种产生致病细菌结核分枝杆菌细胞壁的酶。了解更多

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BSI-201 (Iniparib)

Catalog No. A10164
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PARP 抑制剂

BSI-201 (Iniparib)是一种有效的PARP-1抑制剂，已被证明可以穿越血脑屏障。了解更多

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- Jianwei Dou, .et al. Development and evaluation of poly adenosine 5'-diphosphate-ribose polymerase 1 immobilization-based receptor chromatography, J Sep Sci, 2020, Dec 4 PMID: 33275824
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YM201636

Catalog No. A11064
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PI3K 抑制剂

YM201636是PIKfyve的细胞渗透性和选择性抑制剂（IC50 = 33 nM）。了解更多

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- Krishna Chintaluri, .et al. The PH domain from the Toxoplasma gondii PH-containing protein-1 (TgPH1) serves as an ectopic reporter of phosphatidylinositol 3-phosphate in mammalian cells, PLoS One, 2018, 13(6): e0198454 PMID: 29870544
- Dayam RM, .et al. The Lipid Kinase PIKfyve Coordinates the Neutrophil Immune Response through the Activation of the Rac GTPase, J Immunol, 2017, Sep 15;199(6):2096-2105 PMID: 28779020
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Brivanib alaninate (BMS-582664)

Catalog No. A10162
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VEGFR 抑制剂

Brivanib alaninate (BMS-582664)是VEGFR和FGFR信号转导的双重酪氨酸激酶抑制剂。了解更多

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Bosutinib (SKI-606)

Catalog No. A10161
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Src 抑制剂

Bosutinib (SKI-606)是一种酪氨酸激酶抑制剂。了解更多

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- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
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SB939 ( Pracinostat )

Catalog No. A10830
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HDAC 抑制剂

SB939 (Pracinostat)是HDAC的口服抑制剂，对I，II和IV类HDAC具有选择性，在体外HDAC1活性测定中显示IC50值为77 nM。了解更多

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- Giovanni Bocci, .et al. Virtual and In Vitro Antiviral Screening Revive Therapeutic Drugs for COVID-19, ACS Pharmacol Transl Sci, 2020, Oct 14
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KX2-391

Catalog No. A11177
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Src 抑制剂

KX2-391是新型的非ATP竞争底物口袋定向SRC抑制剂。了解更多

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