histone h3

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.

Histone H3 (1-35) acetate 是组蛋白 H3 的 35 个残基肽。组蛋白 H3 是一种重要的蛋白质，在基因的动态和长期调控中发挥作用。

Histone H3 (21-44), derived from a sequence of 21-44 amino acids of histone H3, is commonly employed as a substrate, particularly for protein arginine methyltransferase assays, where methylation activity is being examined.

Histone H3 (23-34) is a peptide consisting of amino acid residues 23 to 34 of the histone H3 protein. This peptide specifically includes lysine residues at positions 23 and 27, which can undergo methylation and acetylation modifications.

Histone H3 (5-23), a derivative of histone H3 consisting of amino acids 5-23, serves as a substrate for histone acetyltransferase (HAT) assays.

Histone H3 (1-21) is a truncated form of the Histone H3 protein consisting of amino acids 1 to 21. It serves as a common substrate for methyltransferase assays targeting Histone 3 at lysine 4 and lysine 9, as well as for acetyltransferase assays targeting Histone 3 at lysine 9 and lysine 14.

Histone H3 (21-44)-GK-biotin is a peptide fragment of histone H3 that corresponds to amino acid residues 22-45 of the human histone H3.1 and 3.2 sequences and is biotinylated via a C-terminal GK linker. Histone H3 (21-44) contains a lysine residue at position 23 that is subject to acetylation, an arginine at position 26 subject to methylation, and a serine at position 28 subject to phosphorylation, as well as lysine residues at positions 27 and 36 that are subject to methylation and acetylation. Histone H3 (21-44)-GK-biotin has been used as a substrate for the primate-specific histone methyltransferase PR domain-containing protein 7 (PRDM7) to determine substrate specificity.

Histone H3 (21-44)-GK-biotin is a peptide fragment of histone H3 that corresponds to amino acid residues 22-45 of the human histone H3.3 sequence and is biotinylated via a C-terminal GK linker. Unlike histone H3.1 and H3.2, the histone H3.3 variant contains a serine residue at position 31 that is phosphorylated during late prometaphase and metaphase of mitosis. Histone H3 (21-44) also contains lysine residues at positions 23, 27, and 36 that are subject to methylation and acetylation, all of which have a role in the regulation of gene expression, and a serine residue at position 28 that is subject to phosphorylation during mitosis.

Histone H3 (1-25), amide is a N-terminal peptide fragment of histone H3 that serves as a substrate for histone methyltransferases (HMTs). It can be utilized to identify the substrate for HMTs. Compared to histone H3 (15-39) and full-length histone H3, Histone H3 (1-25), amide proves to be more efficient as a substrate for HMT G9a.

Histone H3 (116-136), C116-136 is a peptide consisting of amino acids 116 to 136, which spans the C-terminus of histone H3.

Acetyl-Histone H3 (Lys9) (C5B11) Rabbit mAb #9649R 是一种有用的有机化合物，可用于生命科学领域的相关研究，其产品编号为 T64611。

Histone H3K27Me1 (23-34) is a peptide fragment of histone H3 that corresponds to amino acid residues 24-35 of the human histone H3.1 and H3.2 sequences. Monomethylation of histone H3 at lysine 27 is associated with actively transcribed genes and positively correlates with H3K36 trimethylation. Levels of H3K27Me1 are increased in tumor tissue isolated from patients with metastatic hormone-na ve and castration-resistant prostate cancer. Histone H3K27Me1 (23-34) has been used in epitope mapping of the lupus-derived monoclonal antibody BT164.

Ilorasertib (ABT-348) 是一种 ATP 竞争性多靶点激酶抑制剂，可抑制 Aurora A、Aurora B 和Aurora C，IC50值为120 nM、7 nM 和1 nM。它还抑制 RET 酪氨酸激酶、PDGFRβ 和 Flt1，IC50为7 nM、3 nM 和 32 nM。

Crebinostat 是一种有效的组蛋白去乙酰化酶 (HDAC) 抑制剂，对 HDAC1、HDAC2、HDAC3 和 HDAC6 有抑制作用， IC50 分别为 0.7 nM、1.0 nM、2.0 nM 和 9.3 nM。Crebinostat 可增加在体外神经元的突触蛋白 1 斑点沿树突 (synapsin-1 punctae along dendrites) 的密度。Crebinostat 可调节染色质介导的神经可塑性，增强小鼠的记忆。Crebinostat 可诱导组蛋白 H3 和组蛋白 H4 乙酰化，并增强 cAMP 反应元件结合蛋白 (CREB) 靶基因 Egr1 的表达。

Procaine (Vitamin H3) 是DNA 脱甲基剂，是一种酯类局部麻醉剂。它起效缓慢，作用持续时间短，主要用于浸润麻醉、周围神经阻滞和脊髓阻滞。

4-tert-Octylphenol 是一种干扰内分泌的化学物质及雌激素药物，能诱导子代小鼠脑神经元祖细胞的凋亡，并通过减少溴脱氧尿苷（BrdU）、有丝分裂标志物Ki67以及磷酸组蛋白H3（p-Histone-H3）的表达，导致神经元祖细胞的增殖减少。这种物质不仅会干扰小鼠的大脑发育，还会影响其行为。

HDAC-IN-7 是 Tucidinostat (Chidamide) 的类似物，是一种 HDAC 抑制剂。HDAC-IN-7 通过抑制组蛋白 H3 的乙酰化作用，诱导人类结肠癌细胞系的凋亡[1]。

UNC3866 TFA(1872382-47-2 free base) 是由 AlphaScreen 确定的 CBX7-H3 相互作用的有效拮抗剂。

LSD1-IN-5 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1. LSD1-IN-5 is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 121 nM.

LSD1-IN-6 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1. LSD1-IN-6 is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 123 nM.

CG-200745 is a potent inhibitor of HDAC. CG200745 induces apoptosis and also inhibits the deacetylation of histone H3 and tubulin.

PF-7006，一种Mps1激酶抑制剂，具有Ki值0.27 nM，IC50值2.5 nM。该化合物通过抑制Mps1催化活性影响细胞周期检查点，同步降低组蛋白 H3 的表达并缩短有丝分裂时长，促使癌细胞发生凋亡 (Apoptosis)。当与Palbociclib联合使用时，可增强对PF-7006的耐药性。该化合物主要用于乳腺癌的研究应用。

HH-2853是一种针对EZH1 2的高效抑制剂，具有显著的抗肿瘤活性。在野生型和突变型EZH2上，HH2853的IC50值在2.21-5.36 nM之间，与tazemetostat相当。此外，该化合物对EZH1的抑制作用更强，IC50为9.26 nM，较tazemetostat的IC50 58.43 nM为低。然而，HH2853在高达10 μM的浓度下，对36种组蛋白修饰酶仅表现出轻微的抑制活性。在细胞层面，HH2853在多种携带野生型或突变型EZH2的癌细胞系中，有效抑制了H3K27的单、双和三甲基化。相对地，高达10 μM的HH2853对组蛋白H3上的其他甲基化类型没有影响。此外，HH2853显著降低了携带EZH2 GOF突变或SWI SNF复合体改变的多种癌细胞系的细胞活性，并在多个肿瘤异种移植模型中展示出优于tazemetostat的抗肿瘤效果，剂量相当。

KTX-1001，亦称为NSD2 inhibitor 161，是一种新型且有效的核SET结构域含蛋白2（NSD2）抑制剂。该化合物专一性地结合NSD2，抑制其催化活性以及组蛋白H3赖氨酸36（H3K36）的单和双甲基化作用。此作用调控涉及细胞过程的基因表达，包括细胞增殖，进而可能导致癌细胞生长减缓。NSD2是NSD家族组蛋白赖氨酸甲基转移酶中的一员，该酶类在许多癌症类型中表达过量且调控失常。