HDAC

Inhibitory Selectivity

Catalog No.	Inhibitor Name	HDAC	HDAC1	HDAC2	HDAC3	HDAC4	HDAC5	HDAC6	HDAC7	HDAC8	HDAC9	HDAC10	HDAC11	HD1	HD2
A10979	Vorinostat	****
A10611	Entinostat		**		*
A10518	Panobinostat	****
A10947	Trichostatin A	****
A10586	Mocetinostat		**	**	*								*
A10122	Belinostat	***
A11920	Romidepsin		***	***
A10560	MC1568													*
A11042	Tubastatin A HCl		*					***
A10488	Givinostat													****	****
A10516	Dacinostat	***
A10246	CUDC-101	****	****	***	****	***	***	****	**	**	**	***
A10830	Pracinostat		***	**	***	***	***	*	**	**	**	***	**
A11152	PCI-34051		*					*		****		*
A10337	Droxinostat				*			*		*
A10700	Abexinostat		****	***	****			***		**		***
A13218	RGFP966				**
A11037	AR-42	***
A11940	Ricolinostat		**	***	***	*	*	****	*	**
A11964	Tacedinaline		*	*	*					**
A11153	CUDC-907		****	****	****	**	*	***	**		**	****	****
A11355	M344	**
A10954	Tubacin							****
A13139	RG2833		***		****
A12556	Resminostat		***		***			**
A15489	BRD73954			*				***		**
A11361	BG45		*	*	**
A14354	4SC-202		*	*	*
A16431	CAY10603		**					****
A14341	LMK-235					***	****
A14032	Nexturastat A							****
A14128	TMP269					**	**		***		***
A14197	HPOB		*	*	*			***		*		*
A12722	Scriptaid
A12616	Tasquinimod
A11042	Tubastatin A							***

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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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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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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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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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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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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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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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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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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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

Product Citations (3)

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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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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

Product Citations (7)

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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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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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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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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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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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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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