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搜索结果：“jwh 250”

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(-)-Epigallocatechin gallate

Catalog No. A10005
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Antioxidant, antiangiogenic, antitumor agent

(-)-Epigallocatechin gallate是一种从绿茶中分离出来的强效抗氧化剂多酚类黄酮。了解更多

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- Wafa Dridi, .et al. Influence of polysaccharide concentration on polyphenol-polysaccharide interactions, Carbohydr Polym, 2021, 274:118670 PMID: 34702486
- A S D'Costa, .et al. Inhibition of starch digestion by flavonoids: Role of flavonoid-amylase binding kinetics, Food Chem, 2020, Oct 1;341(Pt 2):128256 PMID: 33035827
- Fenteany G, .et al. Multilevel structure-activity profiling reveals multiple green tea compound families that each modulate ubiquitin-activating enzyme and ubiquitination by a distinct mechanism, Sci Rep, 2019, Sep 5;9(1):12801 PMID: 31488855
- LiliSun, .et al. Comparative Effect of Black, Green, Oolong and White Tea Intake on Body Weight Gain and Bile Acid Metabolism, Nutrition, 2019, pii:S0899-9007(18)31140-7
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VX-680 (MK-0457, Tozasertib)

Catalog No. A10981
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Aurora Kinase 抑制剂

VX-680 (MK-0457,Tozasertib)是一种有效的选择性Aurora激酶小分子抑制剂。了解更多

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- Sakamoto K, .et al. Recurrent 8q24 rearrangement in blastic plasmacytoid dendritic cell neoplasm: association with immunoblastoid cytomorphology, MYC expression, and drug response, Leukemia, 2018, May 23 PMID: 29795241
- W. Joost Lesterhuis, .et al. Network analysis of immunotherapy-induced regressing tumours identifies novel synergistic drug combinations, Sci Rep, 2015, 5: 12298 PMID: 26193793
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EX 527 (Selisistat)

Catalog No. A10377
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SIRT1 抑制剂

EX 527 (Selisistat)是一种有效的选择性SIRT1 III类组蛋白脱乙酰基酶抑制剂，在无细胞分析中的IC50为38 nM。了解更多

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- Takeshi Nakamura, .et al. Effects of NAD+ Synthesis Levels on Sirtuin 1 Deacetylase Activity in Mammalian Cells, Shimane Journal of Medical Science, 2022, 38 (2), 59-66
- Bugga Paramesha, .et al. Sirt1 and Sirt3 Activation Improved Cardiac Function of Diabetic Rats via Modulation of Mitochondrial Function, Antioxidants (Basel), 2021, Feb 24;10(3):338 PMID: 33668369
- Wenhui Yao, .et al. Icariin ameliorates endothelial dysfunction in type 1 diabetic rats by suppressing ER stress via the PPARα/Sirt1/AMPKα pathway, J Cell Physiol, 2020, 07 August
- Guang Bai, .et al. Chapter 1 - Epigenetic Tools in Chronic Pain Studies, Epigenetics of Chronic Pain, 2019, Pages 1-48
- Yoshikawa A, .et al. Deletion of Atf6α impairs astroglial activation and enhances neuronal death following brain ischemia in mice, J Neurochem, 2015, Feb;132(3):342-53 PMID: 25351847
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Ascomycin

Catalog No. A12592
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calcineurin 抑制剂

Ascomycin是一种有效的免疫抑制剂，可用作自身免疫性疾病的潜在治疗剂。了解更多

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Tranylcypromine hydrochloride

Catalog No. A13358
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LSD1/BHC110 & MAO 抑制剂

Tranylcypromine hydrochloride是一种非选择性的MAO-A/B抑制剂。了解更多

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Cyclosporine

Catalog No. A15434
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Calcineurin 抑制剂

Cyclosporine是一种钙调磷酸酶磷酸酶途径抑制剂，用作免疫抑制剂以防止器官移植中的排斥反应。了解更多

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Amodiaquine dihydrochloride dihydrate

Catalog No. A16405
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Amodiaquine dihydrochloride dihydrate是人红细胞中组胺N-甲基转移酶的有效，非竞争性抑制剂，也用作抗疟疾和抗炎药。了解更多

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SGI-1776 (free base)

Catalog No. A10838
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PIM1 抑制剂

SGI-1776 (free base)是Pim1的一种新型ATP竞争性抑制剂，在无细胞试验中的IC50为7 nM，选择性是Pim2和Pim3的50倍和10倍，对Flt3和haspin也有效。阶段1。了解更多

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- Ishikawa C, .et al. Expression and significance of Pim-3 kinase in adult T-cell leukemia, Eur J Haematol, 2017, Dec;99(6):495-504 PMID: 28833639
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CCT137690

Catalog No. A11081
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Aurora Kinase 抑制剂

CCT137690是Aurora A，Aurora B和Aurora C的高度选择性抑制剂，IC50为15 nM，25 nM和19 nM。它对hERG离子通道影响很小。了解更多

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TG-101348 (Fedratinib, SAR302503)

Catalog No. A11082
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JAK2/FLT3 抑制剂

TG-101348 (Fedratinib,SAR302503)是Janus相关激酶2的口服生物利用型，ATP竞争性和选择性抑制剂，在无细胞试验中IC50为3 nM，作用于JAK2比作用于JAK1和JAK3选择性高35和334倍,具有潜在的抗肿瘤活性。了解更多

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CUDC-907 (Fimepinostat)

Catalog No. A11153
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PI3K/HDAC 抑制剂

CUDC-907 (Fimepinostat)是针对PI3K和HDAC的单一小分子抑制剂，作用于PI3Kα和HDAC1/2/3/10，IC50分别为19 nM和1.7 nM/5 nM/1.8 nM/2.8 nM。了解更多

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- Chie Ishikawa, .et al. The role of CUDC-907, a dual phosphoinositide-3 kinase and histone deacetylase inhibitor, in inhibiting proliferation of adult T-cell leukemia, Eur J Haematol, 2020, Eur J Haematol PMID: 32780889
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Tubacin

Catalog No. A10954
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HDAC6 抑制剂

Tubacin (tubulin acetylation inducer)是一种高效且选择性强，可逆，可透过细胞的HDAC6抑制剂，IC50为4 nM。了解更多

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FK-506 (Tacrolimus)

Catalog No. A10389
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mTOR 抑制剂

FK-506 (Tacrolimus)是一种免疫抑制药物，通过结合到抑免蛋白FKBP12 (FK506 结合蛋白)产生新的复合物，从而降低T细胞中肽酰脯氨酰异构酶活性。了解更多

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- Ogawa Y, .et al. Inhibition of astrocytic adenosine receptor A2A attenuates microglial activation in a mouse model of Sandhoff disease, Neurobiol Dis, 2018, Oct;118:142-154 PMID: 30026035
- Yuko Okamoto, .et al. In vivo drug delivery efficiency of albumin-encapsulated liposomes as hydrophobic drug carriers, J Drug Deliv Sci Technol, 2018, 47: 62-66
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ACY-1215 (Rocilinostat)

Catalog No. A11940
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HDAC6 抑制剂

ACY-1215 (Rocilinostat)是一种选择性HDAC6抑制剂，从而通过Hsp90的超乙酰化作用破坏Hsp90蛋白伴侣系统，并防止随后的总蛋白降解。了解更多

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BIX 01294

Catalog No. A11763
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G9a/GLP HMT 抑制剂

BIX 01294是一种G9a样蛋白和G9a组蛋白赖氨酸甲基转移酶抑制剂。了解更多

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BMN673

Catalog No. A11243
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PARP 抑制剂

BMN-673是核酶聚（ADP-核糖）聚合酶（PARP）的口服生物利用抑制剂，无细胞试验中对PARP1的IC50为0.57 nM。它也是有效的PARP-2抑制剂，但不抑制PARG，对PTEN突变型高度敏感。具有潜在的抗肿瘤活性。了解更多

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- Subhajit Chatterjee, .et al. Combination of talazoparib and olaparib enhanced the curcumin-mediated apoptosis in oral cancer cells by PARP-1 trapping, J Cancer Res Clin Oncol, 2022, Dec;148(12):3521-3535 PMID: 35962813
- 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
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Go 6976

Catalog No. A12419
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PKC 抑制剂

Go6976是一种有效的PKC抑制剂，对PKC（大鼠脑），PKCα和PKCβ1的IC50分别为7.9 nM，2.3 nM和6.2 nM。也是JAK2和Flt3的有效抑制剂。了解更多

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EPZ-5676 (Pinometostat)

Catalog No. A12735
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DOT1L 抑制剂?

EPZ-5676 (Pinometostat)是组蛋白甲基转移酶的小分子抑制剂，具有潜在的抗肿瘤活性。了解更多

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- Yoo H, .et al. Epigenetic priming by Dot1l in lymphatic endothelial progenitors ensures normal lymphatic development and function, Cell Death Dis, 2020, Jan; 11(1): 14 PMID: 31908356
- Guang Bai, .et al. Chapter 1 - Epigenetic Tools in Chronic Pain Studies, Epigenetics of Chronic Pain, 2019, Pages 1-48
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Garcinol

Catalog No. A12814
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HAT 抑制剂

藤黄酚是从印度藤黄中分离的聚异戊二烯基二苯甲酮衍生物。在体外和体内，它都是有效的组蛋白乙酰转移酶（HATs）p300（IC50 = 7?M）和PCAF（IC50 = 5?M）抑制剂。了解更多

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UPF 1069

Catalog No. A12750
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PARP2 抑制剂

UPF 1069是一种选择性聚（ADP-核糖）聚合酶（PARP）2抑制剂（PARP-2和PARP-1的IC50值分别为0.3和8.0μM）。了解更多

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XL019

Catalog No. A12394
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JAK2 抑制剂

XL019是janus相关激酶2 (JAK-2)的生物可利用抑制剂，具有潜在的抗肿瘤活性。了解更多

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GSK343

Catalog No. A13114
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EZH2 抑制剂

GSK343是有效的组蛋白H3-赖氨酸27（H3K27）甲基转移酶EZH2抑制剂（IC = 4 nM）。对除EZH1以外的其他HMT的选择性是1000倍（选择性是60倍）。GSK343抑制HCC1806细胞中的H3K27甲基化，IC小于200nM（通过免疫荧光测量）。了解更多

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- Nie L, .et al. CDK2-mediated site-specific phosphorylation of EZH2 drives and maintains triple-negative breast cancer, Nat Commun, 2019, Nov 8;10(1):5114 PMID: 31704972
- Yang PM, .et al. p38α/S1P/SREBP2 activation by the SAM-competitive EZH2 inhibitor GSK343 limits its anticancer activity but creates a druggable vulnerability in hepatocellular carcinoma, Am J Cancer Res, 2019, Oct 1;9(10):2120-2139 PMID: 31720078
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Reversine

Catalog No. A13250
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human A3 adenosine receptor 拮抗剂 /Aurora 抑制剂

Reversine是一种有效的人A3腺苷受体拮抗剂，Ki为0.66μM，是一种泛光A/B/C激酶抑制剂，IC50分别为12 nM/13 nM/20 nM。也用于干细胞去分化。了解更多

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- Hazheen K, .et al. BuGZ facilitates loading of spindle assembly checkpoint proteins to kinetochores in early mitosis, J Biol Chem, 2020, August 20
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Resminostat

Catalog No. A12556
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HDAC 抑制剂

Resminostat，也称为RAS2410，是一种有效的I和II类组蛋白脱乙酰基酶（HDAC）抑制剂。它结合并抑制HDAC，从而导致高度乙酰化的组蛋白的积累。选择性的抑制HDAC1/3/6，IC50为42.5 nM/50.1 nM/71.8 nM，作用于HDAC8效果弱，IC50为877 nM。了解更多

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CX-6258

Catalog No. A12896
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Pim 抑制剂

CX-6258是一种有效，选择性和口服有效的pan-Pim激酶抑制剂。了解更多

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OTX015

Catalog No. A13890
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BET 抑制剂

OTX015是口服可生物利用的BRD2，BRD3和BRD4的小分子抑制剂（EC50s = 10-19 nM）。了解更多

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MS436

Catalog No. A13749
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BRD4 抑制剂

MS436是用于BRD4溴结构域的重氮基小分子抑制剂，Ki值为30-50 nM。了解更多

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PRT 062070 (Cerdulatinib)

Catalog No. A14147
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Dual Syk and JAK 抑制剂

PRT 062070 (Cerdulatinib)是一种新型的口服双脾酪氨酸激酶（Syk）和janus激酶（JAK）抑制剂。Cerdulatinib优先抑制各种细胞类型中JAK1和JAK3依赖性细胞因子介导的信号传导和功能性反应。了解更多

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Nexturastat A

Catalog No. A14032
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HDAC6 抑制剂

Nexturastat A是一种芳基脲衍生物，可作为组蛋白脱乙酰基酶6（HDAC6）的有效且高度选择性的抑制剂（IC50 = 5.02+/-0.60 nM）。了解更多

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TMP 269

Catalog No. A14128
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HDAC 抑制剂

TMP 269是一种有效的选择性IIa类HDAC抑制剂，对HDAC4，HDAC5，HDAC7和HDAC9的IC50分别为157 nM，97 nM，43 nM和23 nM。了解更多

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TG-02 (SB1317)

Catalog No. A11962
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FLT3 抑制剂

TG-02 (SB1317)是一种新型的小分子有效CDK/JAK2/FLT3抑制剂。了解更多

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AGK2

Catalog No. A14225
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SIRT2 抑制剂

AGK2是一种有效的选择性SIRT2抑制剂，IC50为3.5μM。了解更多

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Anacardic Acid

Catalog No. A14226
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KAT5 (Tip60), p300/PCAF 抑制剂

Anacardic Acid是p300和p300/CBP相关因子组蛋白乙酰转移酶的有效抑制剂。了解更多

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Procainamide HCl

Catalog No. A14240
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Sodium channel blocker/DNMT 抑制剂

Procainamide HCl是钠通道阻滞剂，又是DNA甲基转移酶抑制剂。了解更多

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Santacruzamate A

Catalog No. A14236
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HDAC 抑制剂

Santacruzamate A (CAY10683)是一种有效的选择性HDAC抑制剂，对HDAC2的IC50为119 pM，选择性是其他HDAC的3600倍以上。了解更多

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LMK-235

Catalog No. A14341
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HDAC4/5 抑制剂

LMK-235是选择性组蛋白脱乙酰基酶(HDAC) 4和HDAC5抑制剂。了解更多

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INCB39110 (Itacitinib)

Catalog No. A14390
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JAK1 抑制剂

INCB39110 (Itacitinib)是一种有效的JAK1酪氨酸激酶抑制剂，目前正在II期试验中，用于治疗类风湿关节炎，骨髓纤维化，类风湿关节炎和斑块状牛皮癣。了解更多

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- Czech J, .et al. JAK2V617F but not CALR mutations confer increased molecular responses to interferon-α via JAK1/STAT1 activation, Leukemia, 2018, Nov 23 PMID: 30470838
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BMN-673 8R,9S

Catalog No. A15024
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PARP 抑制剂

BMN-673 8R,9S 是BMN-673的（8R，9S）对映异构体。BMN 673是一种新型PARP抑制剂，IC50为0.58 nM。了解更多

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NU 1025

Catalog No. A15375
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PARP 抑制剂

NU 1025是一种有效的聚（ADP-核糖）聚合酶（PARP）抑制剂，可增强L1210细胞中一系列机制多样的抗癌药的细胞毒性。了解更多

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GSK-J4

Catalog No. A12732
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Demethylase 抑制剂

GSK J4是可被细胞吞噬的前药，可被巨噬细胞酯酶快速水解为GSK-J1，GSK-J1是一种有效的选择性Jumonji H3K27脱甲基酶抑制剂。减轻脂多糖（LPS）诱导的人类原代巨噬细胞促炎细胞因子的产生（IC50 = 9 uM，抑制TNFα释放）。了解更多

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- Guang Bai, .et al. Chapter 1 - Epigenetic Tools in Chronic Pain Studies, Epigenetics of Chronic Pain, 2019, Pages 1-48
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SP2509 (HCI-2509)

Catalog No. A14443
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LSD1 抑制剂

SP2509 (HCI-2509)是一种新型组蛋白脱甲基酶LSD1（KDM1A）拮抗剂，IC50为13 nM。对MAO-A和MAO-B没有抑制作用。了解更多

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SGC 707

Catalog No. A15450
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PRMT3 抑制剂

SGC 707是PRMT3的有效变构抑制剂（IC50 = 50 nM），其选择性是其他甲基转移酶和其他非表观遗传靶标的100倍以上。了解更多

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HDAC inhibitor

Catalog No. A13405
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HDAC 抑制剂

N/A 了解更多

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A-366

Catalog No. A15969
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G9a/GLP 抑制剂

A-366是一种有效的选择性G9a/GLP组蛋白赖氨酸甲基转移酶抑制剂，IC50值为3.3 nM。了解更多

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CPI 4203

Catalog No. A16177
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KDM5 demethylases 抑制剂

CPI 4203是KDM5脱甲基酶的选择性抑制剂，在结构上与CPI 455相关，但效力低约25倍（IC50值250 nM用于抑制全长KDM5A）。了解更多

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HOI-07

Catalog No. A15970
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Aurora B 抑制剂

HOI-07是有效的Aurora B激酶抑制剂。了解更多

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GW841819X

Catalog No. A16367
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BET 抑制剂

GW841819X是(+)-JQ1的类似物，是BET溴结构域的新型抑制剂。GW841819X是单个对映异构体，但在苯并二氮杂3.环3的4位具有不确定的手性。了解更多

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Ruxolitinib Phosphate

Catalog No. A11552
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JAK 抑制剂

Ruxolitinib Phosphate是ruxolitinib的磷酸盐形式，ruxolitinib是一种口服生物可利用的Janus相关激酶(JAK)抑制剂，具有潜在的抗肿瘤和免疫调节活性。了解更多

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WM-1119

Catalog No. A16828
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lysine acetyltransferase KAT6A 抑制剂

WM-1119是赖氨酸乙酰基转移酶KAT6A的高效选择性抑制剂，IC50为0.25 uM。它对KAT6A的活性分别是对KAT5或KAT7的1100倍和250倍。了解更多

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GSK-3326595 (EPZ015938)

Catalog No. A16862
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PRMT5 抑制剂

GSK-3326595 (EPZ015938)是一种有效的，选择性的，可逆的蛋白精氨酸甲基转移酶5（PRMT5）抑制剂，IC50为6.2 nM。了解更多

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