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Search Results for " histones "

22

抑制剂 & 化合物

1

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Cat. No.	Product Name	Target	Signaling Pathways
T7378	BRD9539	Histone Methyltransferase	Chromatin/Epigenetic
	BRD9539 是一种组蛋白甲基转移酶G9a 抑制剂，IC50为 6.3 μM，还抑制PRC2活性。
T11563	Histone Acetyltransferase Inhibitor II	Epigenetic Reader Domain; Histone Acetyltransferase	Chromatin/Epigenetic
	Histone Acetyltransferase Inhibitor II 是一种选择性的细胞渗透性 p300 组蛋白乙酰转移酶抑制剂，IC50值为 5 µM。它在哺乳动物细胞中具有抗乙酰化酶活性，可用于癌症研究。
T15784	LP99	Epigenetic Reader Domain	Chromatin/Epigenetic
	LP99 是一种表观遗传探针，可破坏 BRD7 和 BRD9 与细胞中染色质的结合。它是一种选择性的 BRD7 和 BRD9 溴结构域抑制剂，对 BRD9 的 Kd 为 99 nM。
T10717	Inobrodib CBP-IN-1	Epigenetic Reader Domain	Chromatin/Epigenetic
	Inobrodib (CBP-IN-1) 是一种口服活性的强选择性p300/CBP 抑制剂，与 p300 和 CBP 结合，Kd 值为 1.3 和 1.7 nM。它抑制前列腺癌细胞系的细胞增殖并降低雄激素受体和 C-MYC 调节的基因表达。
T0975	Chlorambucil CB-1348,Chloroambucil,苯丁酸氮芥,WR-139013	DNA Alkylator/Crosslinker; DNA Alkylation	DNA Damage/DNA Repair
	Chlorambucil (CB-1348) 是一种口服活性的氮芥类双功能烷基化剂，具有抗肿瘤活性，可用于研究淋巴细胞白血病、卵巢癌和乳腺癌以及霍奇金病。
T19717	Cyclo-L-Trp-L-Trp	Antifungal	Microbiology/Virology
	Cyclo-L-Trp-L-Trp 是一种广谱抗真菌剂。它还诱导组蛋白的高度乙酰化。
T3661	Citarinostat ACY241,HDAC-IN-2	HDAC	Chromatin/Epigenetic; DNA Damage/DNA Repair
	Citarinostat (ACY241) 是一种强效、选择性和口服组蛋白脱乙酰酶 (HDAC) 抑制剂，具有抗肿瘤活性，对 HDAC1、HDAC2、HDAC3、HDAC6 和 HDAC8 的 IC50分别为 35、45、46、2.6 和 137 nM。
T21505	Suberoyl bis-hydroxamic acid SBHA,软木肟酸,Suberohydroxamic acid	Apoptosis; HDAC	Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair
	Suberoyl bis-hydroxamic acid (SBHA) 是一种竞争性且可透过细胞的HDAC1和HDAC3抑制剂，ID50值分别为 0.25 μM 和 0.30 μM。它使肿瘤细胞易于凋亡并促进线粒体凋亡途径，可研究甲状腺髓样癌。
T3712	Mivebresib ABBV-075,米维布塞	Apoptosis; Epigenetic Reader Domain	Apoptosis; Chromatin/Epigenetic
	Mivebresib (ABBV-075) 是一种有效的，口服活性的溴结构域和末端结构域 (BET) 抑制剂，结合BRD4的Ki 值是 1.5 nM。
T74485	STC314	Others	Others
	STC314 具有抗感染作用，通过中和胞外组蛋白和中性粒细胞诱捕网来逆转机体过度免疫反应造成的器官损伤，可用于研究脓毒症和急性呼吸窘迫综合征(ARDS)。STC314 可保护脂质双层的稳定性，抑制血小板活化和红细胞损伤。
T36392	TCEP-biotin
	TCEP-biotin is biotinylated form of the reducing agent TCEP and an affinity probe for protein lysine crotonylation. Covalent addition of the TCEP moiety to crotonylated lysine residues results in adduct formation that allows for detection or immobilization of crotonylated proteins through interaction with the biotin ligand. It has been used in the detection and isolation of crotonylated histones in HEK293 cells.
TP1903	PKG inhibitor peptide cGMP Dependent Kinase Inhibitor Peptide
	Competitive inhibitor of cGMP-dependent protein kinase (PKG); analog of a substrate peptide corresponding to a phosphorylation site of histone H2B. Competes with synthetic substrates (Ki = 86 mM) but does not inhibit phosphorylation of intact histones by
T35411	(+)-Biotin 4-Amidobenzoic Acid (sodium salt)
	(+)-Biotin 4-amidobenzoic acid is a substrate of biotinidase, which cleaves biotin amide to give biotin in vivo. Biotin is an essential coenzyme for certain carboxylases and is used to modify histones and regulate gene transcription. Biotinidase has key roles in intestinal absorption of biotin, the transport of biotin in plasma, and in the regulation of histone biotinylation. (+)-Biotin 4-amidobenzoic acid is hydrolyzed by biotinidase to release 4-aminobenzoic acid (PABA), which can be quantifie...
T38766	Histone H3 (1-35) Histone H3 (1-35)
	Histone H3 (1-35) is a 35-residue peptide derived from histone H3, which is a key member of the five main histones participating in the formation of chromatin within eukaryotic cells.
T70748	Bisthianostat
	Bisthianostat, also known as CF367 or CF367;-C, is a novel Orally Efficacious Pan-HDAC Inhibitor. Bisthianostat selectively binds to and inhibits HDACs, which inhibits deacetylation of histone proteins and leads to the accumulation of highly acetylated histones. This may result in an induction of chromatin remodeling, the inhibition of tumor oncogene transcription, and the selective transcription of tumor suppressor genes. This prevents cell division, induces cell cycle arrest and apoptosis. Thi...
TP2257	Histone-H2A-(107-122)-Ac-OH	Others	Others
	Histone-H2A-(107-122)-Ac-OH is a peptide with the sequence Ac-Gly-Val-Leu-Pro-Asn-Ile-Gln-Ala-Val-Leu-Leu-Pro-Lys-Lys-Thr-Glu-OH, MW= 1762.1. Histone H2A is one of the five main histone proteins involved in the structure of chromatin in eukaryotic cells.
T79710	PI3Kα/HDAC6-IN-1	HDAC	Chromatin/Epigenetic; DNA Damage/DNA Repair
	PI3Kα/HDAC6-IN-1（化合物21j）是一种针对PI3Kα/HDAC6的双重抑制剂，其IC50值分别为2.9 nM和26 nM。该化合物还能抑制AKT(Ser473)的磷酸化，诱导α-微管蛋白的积累，并促进其乙酰化，但对乙酰化组蛋白H3和H4无显著影响。在L-363细胞系中，PI3Kα/HDAC6-IN-1显示了高效的抑制活性（IC50=0.17 μM），表现出良好的抗癌潜力。
T80550	N-myristoyl-RKRTLRRL	PKC	Chromatin/Epigenetic; Cytoskeletal Signaling
	N-myristoyl-RKRTLRRL 抑制 PKC 底物结合，亦阻碍 Ca2+ 和磷脂酰丝氨酸（PS）依赖性组蛋白磷酸化，其中 IC50 为 5 μM；同样，N-myristoyl-RKRTLRRL 对组蛋白磷酸化的抑制作用中，IC50 为 80 μM。
T70210	FT-1101 free base
	FT-1101 is an orally bioavailable, potent and selective BET inhibitor. FT-1101 binds to the acetylated lysine recognition motifs in the bromodomain sites of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histones. This disrupts chromatin remodeling and gene expression. Prevention of the expression of certain growth-promoting genes may lead to the inhibition of tumor cell growth. BET proteins, comprised of BRD2, BRD3, BRD4 and BRDT, are transcriptional r...
T71110	Nanatinostat TFA
	Nanatinostat, also known as Tractinostat, CHR-3996 and VRx-3996, is an orally bioavailable, second-generation hydroxamic acid-based inhibitor of histone deacetylase (HDAC) with potential antineoplastic activity. HDAC inhibitor CHR-3996 inhibits HDAC, resulting in an accumulation of highly acetylated histones, the induction of chromatin remodeling, and the selective transcription of tumor suppressor genes; these events may result in the inhibition of tumor cell division and the induction of tumor...
T35567	BIX01294 (hydrochloride hydrate)
	The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development. BIX01294 (hydrochloride hydrate) is a selective inhibitor of G9a HMTase (IC50 = 1.7 μM). It less effectively inhibits the HMTase G9a-like protein (GLP; IC50 = 38 μM) and has no effect on other ...
T79714	HDAC3-IN-2	HDAC	Chromatin/Epigenetic; DNA Damage/DNA Repair
	HDAC3-IN-2 (compound 4i) 是一种具有纳摩尔级效力的吡嗪酰肼基HDAC3抑制剂，IC50值为14 nM，针对三阴性乳腺癌细胞表现出高效抑制作用。该化合物在细胞内毒性测定中显示，对4T1细胞株的IC50为0.55 μM，对MDA-MB-231细胞株的IC50为0.74 μM。HDAC3-IN-2通过增加乙酰化水平（如H3K9、H3K27和H4K12），促进细胞凋亡（涉及caspase-3、caspase-7和细胞色素c的水平提升），并抑制细胞增殖相关蛋白（如Bcl-2、CD44、EGFR和Ki-67）的表达，从而在荷瘤小鼠模型中表现出显著的体内抗肿瘤作用。

化合物

Cat.No: T7378

Target: Histone Methyltransferase

Histone Acetyltransferase Inhibitor II

Cat.No: T11563

Target: Epigenetic Reader Domain, Histone Acetyltransferase

Cat.No: T15784

Target: Epigenetic Reader Domain

Cat.No: T10717

Synonym: CBP-IN-1

Target: Epigenetic Reader Domain

Cat.No: T0975

Synonym: CB-1348,Chloroambucil,苯丁酸氮芥,WR-139013

Target: DNA Alkylator/Crosslinker, DNA Alkylation

Cyclo-L-Trp-L-Trp

Cat.No: T19717

Target: Antifungal

Cat.No: T3661

Synonym: ACY241,HDAC-IN-2

Target: HDAC

Suberoyl bis-hydroxamic acid

Cat.No: T21505

Synonym: SBHA,软木肟酸,Suberohydroxamic acid

Target: Apoptosis, HDAC

Cat.No: T3712

Synonym: ABBV-075,米维布塞

Target: Apoptosis, Epigenetic Reader Domain

Cat.No: T74485

Target: Others

Cat.No: T36392

PKG inhibitor peptide

Cat.No: TP1903

Synonym: cGMP Dependent Kinase Inhibitor Peptide

(+)-Biotin 4-Amidobenzoic Acid (sodium salt)

Cat.No: T35411

Histone H3 (1-35)

Cat.No: T38766

Synonym: Histone H3 (1-35)

Cat.No: T70748

Histone-H2A-(107-122)-Ac-OH

Cat.No: TP2257

Target: Others

PI3Kα/HDAC6-IN-1

Cat.No: T79710

Target: HDAC

N-myristoyl-RKRTLRRL

Cat.No: T80550

Target: PKC

FT-1101 free base

Cat.No: T70210

Nanatinostat TFA

Cat.No: T71110

BIX01294 (hydrochloride hydrate)

Cat.No: T35567

Cat.No: T79714

Target: HDAC

Cat. No.	Product Name	Target	Signaling Pathways
T6270	Trichostatin A 曲古柳菌素A,曲古抑菌素A,TSA	HDAC	Chromatin/Epigenetic; DNA Damage/DNA Repair
	Trichostatin A (TSA) 属于二烯异羟肟酸类的天然衍生物。Trichostatin A 是一种组蛋白去乙酰化酶抑制剂 (IC50=1.8 nM)，具有可逆性和特异性。Trichostatin A 导致核心组蛋白过度乙酰化，从而调节染色质结构。

天然产物

Cat.No: T6270

Synonym: 曲古柳菌素A,曲古抑菌素A,TSA

Target: HDAC

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