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搜索结果：“ehop 016”

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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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BS-181

Catalog No. A10163
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CDK 抑制剂

BS-181 是作为CDK7抑制剂的潜在抗肿瘤剂。了解更多

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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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BV-6

Catalog No. A14231
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dual cIAP and XIAP 抑制剂

BV-6是一种SMAC模拟，双重cIAP和XIAP抑制剂。了解更多

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- Aneri Shah, .et al. YB-1 Mediates TNF-Induced Pro-Survival Signaling by Regulating NF-κB Activation, Cancers (Basel), 2020, Aug 5;12(8):E2188 PMID: 32764479
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Deoxygalactonojirimycin HCl

Catalog No. A14016
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Alpha-galactosidase 抑制剂

Deoxygalactonojirimycin Hydrochloride是一种有效且选择性的Alpha-gal A（Alpha-半乳糖苷酶）抑制剂。了解更多

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SR 11302

Catalog No. A14950
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AP-1 transcription factor 抑制剂

SR 11302，活化蛋白1（AP-1）转录因子活性的抑制剂，在体内表现出抗肿瘤作用。了解更多

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LY2801653 dihydrochloride

Catalog No. A15150
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MET 抑制剂

LY2801653 dihydrochloride是一种有效的，口服可生物利用的c-MET激酶小分子抑制剂（Ki = 2 nM）。了解更多

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NVP DPP 728 dihydrochloride

Catalog No. A15320
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DPP-4 抑制剂

NVP DPP 728 dihydrochloride是一种有效的活性二肽基肽酶(DPP)-IV抑制剂，Ki和IC50值分别为11 nM和14 nM。了解更多

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SU6656

Catalog No. A15518
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SRC 抑制剂

SU6656是Src激酶的选择性抑制剂，包括Src，Yes，Lyn和Fyn（分别为IC50 = 280、20、130、170 nM）。了解更多

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JH-II-127

Catalog No. A15777
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LRRK2 抑制剂

JH-II-127是一种高效，选择性和脑渗透性的LRRK2抑制剂，对于LRRK2野生型，LRRK2-G2019S和LRRK2-A2016T，IC50为6.6 nM，2.2 nM和47.7 nM。了解更多

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ETC-1002

Catalog No. A15815
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ACL 抑制剂 and AMPK 激活剂

ETC-1002是一种新颖的，一流的可以降低LDL-C的小分子；肝AMP激活的蛋白激酶（AMPK）的激活剂;对肝ATP-柠檬酸裂解酶也具有有效的抑制活性（IC50 = 29 uM）。了解更多

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ORY-1001 (RG-6016)

Catalog No. A15893
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LSD1 抑制剂

ORY-1001 (RG-6016)是一种活性的选择性赖氨酸脱甲基酶LSD1/KDM1A抑制剂，IC50 <20 nM，对相关FAD依赖性氨氧化酶具有高选择性。了解更多

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PD0166285

Catalog No. A15863
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Wee1 抑制剂

PD0166285是一种有效的Wee1和Chk1抑制剂，在纳摩尔浓度下具有活性。PD0166285是一种新型的G2检查点消除剂。了解更多

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KT 5720

Catalog No. A16016
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PKA 抑制剂

KT5720 是一种能透过细胞的、有效的、特异性的、可逆的、ATP 竞争性的蛋白酶 K (PKA) 的抑制剂，其 Ki 值为 60 nM。了解更多

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LY2801653 (Merestinib)

Catalog No. A12557
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c-MET 抑制剂

LY2801653 (Merestinib)是一种有效的，口服生物利用的小分子c-MET激酶抑制剂（Ki = 2 nM）。了解更多

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Sivelestat sodium hydrate (ONO-5046 sodium hydrate)

Catalog No. A16137
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Neutrophil elastase 抑制剂

Sivelestat sodium hydrate (ONO-5046 sodium hydrate)是人嗜中性粒细胞弹性蛋白酶的竞争性抑制剂，还抑制从兔，大鼠，仓鼠和小鼠获得的白细胞弹性蛋白酶。了解更多

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Vadadustat

Catalog No. A16794
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HIF prolyl-hydroxylase 抑制剂

Vadadustat，也称为AKB-6548和PG-1016548，是一种有效的缺氧诱导因子脯氨酸双加氧酶抑制剂。了解更多

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MIK665

Catalog No. A18362
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Mcl-1 inhibitor

MIK665 (S-64315) is a special Mcl-1 inhibitor extracted from patent WO2016207225A1, compound Preparation 13, has an IC50 of 1.81 nM. 了解更多

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Fosfomycin calcium

Catalog No. A18154
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MurA and isopentenyl mevalonate kinase inhibitor

Fosfomycin calcium is a MurA and isopentenyl mevalonate kinase inhibitor that prevents synthesis of bacterial cell walls. 了解更多

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RV01

Catalog No. A19104
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ALDH2 inhibitor

RV01 is an analogue of resveratrol, inhibits DNA damage, reduces acetaldehyde dehydrogenase 2 (ALDH2) mRNA expression induced by ethanol, and exhibits hydroxyl radical scavenging activity. RV01 decreases iNOS expression, with anti-neuroinflammatory activity. 了解更多

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UPGL00004

Catalog No. A19047
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GAC inhibitor

UPGL00004 is a potent allosteric glutaminase C (GAC) inhibitor (IC50=29 nM; Kd=27 nM). UPGL00004 strongly inhibits the proliferation of highly aggressive triple-negative breast cancer cell lines. 了解更多

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Bromodomain IN-1

Catalog No. A18845
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Bromodomain inhibitor

Bromodomain IN-1 is a Bromodomain inhibitor extracted from patent WO2016069578A1, compound 4 . 了解更多

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HPGDS inhibitor 2

Catalog No. A18390
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H-PGDS 抑制剂

HPGDS inhibitor 2 is a highly potent and selective hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with an IC50 of 9.9 nM. 了解更多

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EC330

Catalog No. A13799
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leukemia inhibitory factor (LIF) inhibitor

EC330 is a leukemia inhibitory factor (LIF) inhibitor. 了解更多

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T56-LIMKi

Catalog No. A12266
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LIMK2 inhibitor

T56-LIMKi is a selective inhibitor of LIMK2; inhibits the growth of Panc-1 cells with an IC50 of 35.2 μM. 了解更多

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Glycolic acid oxidase inhibitor 1

Catalog No. A13016
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glycolate oxidase inhibitor

Glycolic acid oxidase inhibitor 1 is a glycolate oxidase inhibitor, extracted from patent EP0021228A1, in Table IV. 了解更多

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CRA-026440

Catalog No. A12179
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HDAC inhibitor

CRA-026440 is a potent, broad-spectrum HDAC inhibitor. 了解更多

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MethADP sodium salt

Catalog No. A21603
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CD73 inhibitor

MethADP (sodium salt) is a specific CD73 inhibitor. 了解更多

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NMS-P515

Catalog No. A18449
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PARP-1 抑制剂

NMS-P515 is a potent inhibitor of PARP-1 both in biochemical (Kd: 0.016 μM) and cellular (IC50: 0.027 μM) assays. 了解更多

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EHop-016

Catalog No. A12740
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Rac GTPase Inhibitor

EHop-016 is a potent and specific inhibitor of Rac1 and Rac3 GTPase activity that inhibits Vav2 interaction with Rac, Rac-activated PAK1, lamellipodia formation, and cell migration. 了解更多

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