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Epigenetics

Epigenetics

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MGCD0103 (Mocetinostat)

Catalog No. A10586
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HDAC 抑制剂

MGCD0103 (Mocetinostat)是一种苯甲酰胺组蛋白脱乙酰基酶抑制剂，主要抑制组蛋白脱乙酰基酶1（HDAC1），但也抑制HDAC2，HDAC3和HDAC11。了解更多

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- Mari Ishigami-Yuasa, .et al. Class IIb HDAC Inhibition Enhances the Inhibitory Effect of Am80, a Synthetic Retinoid, in Prostate Cancer, Biol Pharm Bull, 2019, 42, 448-452
- Guang Bai, .et al. Chapter 1 - Epigenetic Tools in Chronic Pain Studies, Epigenetics of Chronic Pain, 2019, Pages 1-48
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CI994 (Tacedinaline)

Catalog No. A11964
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HDAC 抑制剂

CI994 (Tacedinaline)是一种组蛋白脱乙酰基酶（HDAC）抑制剂，可在活细胞中诱导组蛋白超乙酰化。了解更多

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Resminostat hydrochloride

Catalog No. A15220
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HDAC 抑制剂

Resminostat hydrochloride是HDAC1/3/6的有效抑制剂（IC50 = 43-72 nM）；对HDAC8的效力较低，IC50为877 nM。了解更多

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HDAC-IN-7

Catalog No. A21252
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HDAC1/2/3/10 inhibitor

HDAC-IN-7 (Chidamide impurity) is an impurity of Chidamide. Chidamide is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor. 了解更多

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Trichostatin-A (TSA)

Catalog No. A10947
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HDAC 抑制剂

Trichostatin-A (TSA)是抑制HDAC 1、3、4、6和10，IC50值约为20 nM。了解更多

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- Goudreault M, .et al. Afadin couples RAS GTPases to the polarity rheostat Scribble, Research Square, 2021, 22 Nov
- Hiroyuki Imuta, .et al. Histone methylation and demethylation are implicated in the transient and sustained activation of the interleukin-1β gene in murine macrophages, Heart Vessels, 2020, Jul 16 PMID: 32676696
- M??ndez-Blanco C, .et al. Stabilization of Hypoxia-Inducible Factors and BNIP3 Promoter Methylation Contribute to Acquired Sorafenib Resistance in Human Hepatocarcinoma Cells, Cancers (Basel), 2019, Dec 9;11(12). pii: E1984 PMID: 31835431
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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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RG2833 (RGFP109)

Catalog No. A13139
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HDAC 抑制剂

RG2833 (RGFP109)是一种脑渗透性HDAC抑制剂，IC50为60 nM，HDAC1和HDAC3为50 nM。了解更多

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PCI-24781 (Abexinostat)

Catalog No. A10700
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HDAC 抑制剂

PCI-24781 (Abexinostat)是一种广谱苯基异羟肟酸HDAC抑制剂。了解更多

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Romidepsin (FK228 ,Depsipeptide)

Catalog No. A11920
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HDAC 抑制剂

Romidepsin (FK228,Depsipeptide)抑制HDAC1和HDAC2，IC50分别为1.6 nM和3.9 nM，但相对较弱地分别抑制HDAC4和HDAC6，IC50值为25 nM和79 nM。了解更多

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- Yu-Fang Liu, .et al. Effects of dexmedetomidine on cognitive dysfunction andneuroinflammation via the HDAC2/HIF?\1α/PFKFB3 axis in amurine model of postoperative cognitive dysfunction, J Biochem Mol Toxicol, 2022, Jun;36(6):e23044 PMID: 35499365
- David Diaz-Carballo, .et al. Enhanced antitumoral activity of TLR7 agonists via activation of human endogenous retroviruses by HDAC inhibitors, Commun Biol, 2021, Mar 3;4(1):276 PMID: 33658617
- Eva Hesping, .et al. An ELISA method to assess HDAC inhibitor-induced alterations to P. falciparum histone lysine acetylation, Int J Parasitol Drugs Drug Resist, 2020, 14: 249-256
- Shariful Islam, .et al. Resistance to histone deacetylase inhibitors confers hypersensitivity to oncolytic reovirus therapy, Blood Adv, 2020, 4(20): 5297-5310 PMID: 33108458
- Elena Netchiporouk, .et al. Analysis of CTCL cell lines reveals important differences between mycosis fungoides/Sézary syndrome vs. HTLV-1+ leukemic cell lines, Oncotarget, 2017, Nov 10; 8(56): 95981-95998 PMID: 29221181
- Ivan V. Litvinov, .et al. Ectopic expression of cancer testis antigens in Cutaneous T-Cell Lymphoma (CTCL) patients, Clin Cancer Res, 2014, 20(14): 3799-3808 PMID: 24850846
- Ivan V Litvinov, .et al. Analysis of STAT4 expression in cutaneous T-cell lymphoma (CTCL) patients and patient-derived cell lines, Cell Cycle., 2014, 15; 13(18): 2975-2982 PMID: 25486484
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KD 5170

Catalog No. A15354
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HDAC 抑制剂

KD 5170是一种新型的基于巯基酮的组蛋白脱乙酰基酶抑制剂，在体外和体内均表现出广谱的抗肿瘤活性。了解更多

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LBH589 (Panobinostat)

Catalog No. A10518
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HDAC 抑制剂

LBH589是异羟肟酸，用作非选择性HDAC抑制剂，HDAC1的IC5o为0.23 nM。了解更多

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- Jalila Chagraoui, .et al. UM171 Preserves Epigenetic Marks that Are Reduced in Ex Vivo Culture of Human HSCs via Potentiation of the CLR3-KBTBD4 Complex, Cell Stem Cell, 2021, Jan 7;28(1):48-62.e6 PMID: 33417871
- Gils Jose, .et al. Co-Delivery of CPT-11 and Panobinostat with Anti-GD2 Antibody Conjugated Immunoliposomes for Targeted Combination Chemotherapy, Cancers (Basel), 2020, Oct 31;12(11):E3211 PMID: 33142721
- Shariful Islam, .et al. Resistance to histone deacetylase inhibitors confers hypersensitivity to oncolytic reovirus therapy, Blood Adv, 2020, 4(20): 5297-5310 PMID: 33108458
- Giovanni Bocci, .et al. Virtual and In Vitro Antiviral Screening Revive Therapeutic Drugs for COVID-19, ACS Pharmacol Transl Sci, 2020, Oct 14
- Justin Kale, .et al. Phosphorylation switches Bax from promoting to inhibiting apoptosis thereby increasing drug resistance, EMBO Rep, 2018, Sep; 19(9): e45235 PMID: 29987135
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Parthenolide ((-)-Parthenolide)

Catalog No. A10698
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Parthenolide ((-)-Parthenolide), Nuclear Factor-κB抑制剂，可特异性地耗尽HDAC1蛋白，而不影响其他I/II类 HDACs。促进MDM2的泛素化并激活p53的细胞功能。了解更多

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MS-275 (Entinostat)

Catalog No. A10611
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HDAC 抑制剂

MS-275 (Entinostat)是一种有效的HDAC抑制剂，对HDAC1和HDAC3的IC50分别为0.3和8uM。了解更多

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- Vivek Bora, .et al. Systemic study of selected histone deacetylase inhibitors in cardiac complications associated with cancer cachexia, Can J Physiol Pharmacol, 2021, 6 October
- Taito Kashio, .et al. HDAC inhibitor, MS-275, increases vascular permeability by suppressing Robo4 expression in endothelial cells, Tissue Barriers, 2021, May 6;1911195 PMID: 33955828
- Ting-Yu Chang, .et al. A novel histone deacetylase inhibitor MPT0L184 dysregulates cell-cycle checkpoints and initiates unscheduled mitotic signaling, Biomed Pharmacother, 2021, Jun;138:111485 PMID: 33740521
- Arshdeep Singh, .et al. CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition, Eur J Med Chem, 2021, Apr 5;215:113169 PMID: 33588178
- Minoru Ueda, .et al. The Distinct Roles of Class I and II RPD3-Like Histone Deacetylases in Salinity Stress Response, Plant Physiol, 2017, Dec; 175(4): 1760-1773 PMID: 29018096
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Pyroxamide (NSC 696085)

Catalog No. A10764
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HDAC 抑制剂

Pyroxamide (NSC 696085)是亲和纯化的HDAC1的有效抑制剂，可导致乙酰化核心组蛋白在用该试剂培养的MEL细胞中积累。了解更多

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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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Valproic acid

Catalog No. A17323
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HDAC inhibitor

Valproic acid is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2; Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches. 了解更多

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- Dan Zhao, .et al. From crypts to enteroids: establishment and characterization of avian intestinal organoids, Poult Sci, 2022, Mar; 101(3): 101642 PMID: 35016046
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SR-4370

Catalog No. A16899
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HDAC 抑制剂

SR-4370是HDAC抑制剂。SR-4370对HDAC1，HDAC2和HDAC3的IC50值分别为0.5 uM，0.1 uM和0.06 uM。了解更多

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UF010

Catalog No. A15781
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HADC 抑制剂

UF010是一种有效的选择性HADC抑制剂，对于HDAC 3、2、1和8分别具有IC50?0.06 uM，0.1 uM，0.5 uM和1.5 uM。它的选择性是其他HDAC的6倍以上。了解更多

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CM-675

Catalog No. A18741
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PDE5/HDAC-1 inhibitor

CM-675 is a dual phosphodiesterase 5 (PDE5) and class I histone deacetylases-selective inhibitor, with IC50 values of 114 nM and 673 nM for PDE5 and HDAC1, respectively. CM-675 has potential to treat Alzheimer??s disease. 了解更多

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Tinostamustine (EDO-S101)

Catalog No. A18342
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HDAC inhibitor

EDO-S101 is a pan HDAC inhibitor; inhibits HDAC1, HDAC2 and HDAC3 with IC50 values of 9, 9 and 25 nM, respectively. 了解更多

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Domatinostat (4SC-202)

Catalog No. A14354
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HDAC 抑制剂

4SC-202是生物利用的苯甲酰胺和人I类组蛋白脱乙酰基酶（HDACs）同工酶1、2和3的抑制剂，具有潜在的抗肿瘤活性。了解更多

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BRD-6929

Catalog No. A12511
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HDAC1/HDAC2 inhibitor

BRD-6929 (Cpd-60) is a brain-penetrant, selective inhibitor of HDAC1 and HDAC2 (IC50=?1 and 8 nM), extracted from patent US2018360927. 了解更多

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BG45

Catalog No. A11361
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HDAC 抑制剂

BG45是一种HDAC I类抑制剂，对HDAC3具有选择性（IC50 = 289 nM）。它抑制HDAC1，HDAC2和HDAC6的效力大大降低（IC50分别为2、2和> 20μM）。了解更多

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TC-H 106

Catalog No. A15357
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HDAC 抑制剂

TC-H 106是一种慢速，紧密结合的I类HDAC（组蛋白脱乙酰基酶）抑制剂。了解更多

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