114
2
12
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T8548 |
Metoprine
|
Histone Methyltransferase; Antifolate; Histamine Receptor | Cell Cycle/Checkpoint; Chromatin/Epigenetic; GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Metoprine 是一种有效的组胺 N-甲基转移酶抑制剂,具有抗肿瘤活性。它是一种二氨基嘧啶衍生物,可以透过血脑屏障,并通过抑制 HMT 增加脑组胺水平。 | |||
T8381 |
Amodiaquine
|
Others; Histone Methyltransferase; Parasite | Chromatin/Epigenetic; Microbiology/Virology; Others |
Amodiaquine 是一种合成的4-氨基喹啉类抗疟剂,是一种有口服活性的组胺 N-甲基转移酶抑制剂。它也是一种Nurr1激动剂,有抗炎活性,可特异性结合Nurr1的配体结合域,EC50约为20 μM。 | |||
T2097 |
C-7280948
C7280948 |
Histone Methyltransferase | Chromatin/Epigenetic |
C-7280948 是一种选择性有效的PRMT1抑制剂,IC50值 12.75 μM。 | |||
T5322 |
BCI-121
|
Histone Methyltransferase | Chromatin/Epigenetic |
BCI-121是一种底物竞争性 SMYD3 抑制剂,可抑制癌细胞的增殖。 | |||
T3084 |
SGC707
|
Histone Methyltransferase | Chromatin/Epigenetic |
SGC707 是 PRMT3化学探针,是一种有效的、选择性的、细胞活性的 PRMT3 变构抑制剂,IC50值为 31 nM。 | |||
T1775 |
GSK503
|
Histone Methyltransferase | Chromatin/Epigenetic |
GSK503是一种高效特异性EZH2甲基转移酶抑制剂,Ki 值为3到27 nM,具有潜在的抗肿瘤活性。 | |||
T4021 |
UNC3866
|
Histone Methyltransferase | Chromatin/Epigenetic |
UNC3866 CBX7-H3 相互作用的有效拮抗剂,IC50为 66±1.2 nM。 | |||
T1905 |
EPZ005687
|
Histone Methyltransferase | Chromatin/Epigenetic |
EPZ005687 是一种选择性EZH2抑制剂,Ki 值为 24 nM,对其选择性是对 EZH1 的 50 倍,对其他 15 种甲基转移酶的 500 倍。 | |||
T9584 |
UNC6934
|
Others; Histone Methyltransferase | Chromatin/Epigenetic; Others |
UNC6934 是一种针对 NSD2 的 N 端 PWWP (PWWP1) 结构域的化学探针,可定位核仁。 | |||
T2435 |
EPZ011989
|
Histone Methyltransferase | Chromatin/Epigenetic |
EPZ011989是一种高选择性可口服的 EZH2抑制剂,对wt EZH2以及EZH2突变型Ki 值<3nM。 | |||
T15624 |
JNJ-64619178
|
Histone Methyltransferase | Chromatin/Epigenetic |
JNJ-64619178 是一种选择性的、口服活性的、假不可逆的蛋白质精氨酸甲基转移酶 5 抑制剂,IC50为 0.14 nM,有用于肺癌的研究潜力。 | |||
TQ0100 |
AZ505
|
Histone Methyltransferase | Chromatin/Epigenetic |
AZ505 是一种选择性SMYD2抑制剂,IC50值为 0.12 μM。 | |||
T15194 |
EBI-2511
|
Histone Methyltransferase | Chromatin/Epigenetic |
EBI-2511 是一种高效且具有口服活性的 EZH2 抑制剂,在 Pfeffiera 细胞系中的 IC50值为 6 nM。 | |||
T7403 |
BAY-598
|
Histone Methyltransferase | Chromatin/Epigenetic |
BAY-598 是SMYD2的选择性抑制剂,IC50值为 27 nM。 | |||
T13780 |
MS1943
|
Apoptosis; Histone Methyltransferase | Apoptosis; Chromatin/Epigenetic |
MS1943 是一种具有口服生物活性的 EZH2选择性降解剂,IC50为 120 nM。它显著降低了许多三阴性乳腺癌和其他癌及非癌细胞系中的 EZH2蛋白水平,能有效阻止多个三阴性乳腺癌和其他癌细胞系的增殖。 | |||
T15201 |
MAK683
|
Histone Methyltransferase | Chromatin/Epigenetic |
MAK683 是胚胎外胚层发育 (EED) 抑制剂。在 EED Alphascreen 结合、LC-MS 和 ELISA 测定中,IC50值为 59、89 和 26 nM。 | |||
T6900 |
MS023
|
Histone Methyltransferase | Chromatin/Epigenetic |
MS023 是一种有效的、选择性的、细胞活性的 I 型 PRMT 抑制剂,对 PRMT1、PRMT3、PRMT4、PRMT6和 PRMT8的 IC50分别为 30、119、83、4 和 5 nM。 | |||
T7089 |
SGC2085
|
Histone Methyltransferase | Chromatin/Epigenetic |
SGC2085是一种高效选择性CARM1抑制剂,IC50值为50 nM。 | |||
T10205 |
A-395
|
Histone Methyltransferase | Chromatin/Epigenetic |
A-395 是一种多梳抑制复合物 2 (PRC2) 蛋白质-蛋白质相互作用的拮抗剂,可有效抑制三聚体 PRC2 复合物 (EZH2-EED-SUZ12),IC50为 18 nM。 | |||
T3057 |
UNC1999
|
Histone Methyltransferase; Autophagy | Autophagy; Chromatin/Epigenetic |
UNC1999 是一种可口服的,选择性和 SAM-竞争性的 EZH2和 EZH1抑制剂,IC50分别为 <10 nM 和 45 nM。 | |||
T1841 |
UNC0379
|
Histone Methyltransferase | Chromatin/Epigenetic |
UNC0379 是一种选择性的、底物竞争性的赖氨酸甲基转移酶 SETD8 抑制剂,IC50值为 7.3 μM,也选择性抑制其他 15 种甲基转移酶。 | |||
T4343 |
A-196
A 196 |
Histone Methyltransferase | Chromatin/Epigenetic |
A-196 是一种选择性有效的 SUV420H1和 SUV420H2抑制剂,IC50值分别为 0.025 和 0.144 μM。它是一种 SUV4-20的化学探针,以底物竞争性方式抑制 SUV4-20,用于研究组蛋白甲基转移酶在基因组完整性中的作用。 | |||
T3081 |
EPZ004777
|
Apoptosis; Histone Methyltransferase | Apoptosis; Chromatin/Epigenetic |
EPZ004777 是一种选择性 DOT1L 抑制剂,IC50为 0.4 nM。 | |||
T6879 |
LLY-507
LLY507,LLY 507 |
Histone Methyltransferase | Chromatin/Epigenetic |
LLY-507 是一种有效的、细胞活性的、特异性的蛋白质赖氨酸甲基转移酶 SMYD2 抑制剂。它是一种化学探针,用于解析 SMYD2 在癌症和其他生物过程中的功能。它有抑制 SMYD2 甲基化 p53 肽的能力,IC50小于 15 nM。 | |||
T6059 |
GSK343
|
Histone Methyltransferase; Autophagy | Autophagy; Chromatin/Epigenetic |
GSK343 是一种特异性且有效的 EZH2 抑制剂,IC50为 4 nM。它对 EZH1 的特异性活性是 60 倍。 | |||
T36631 |
BAY-6035
|
MEK; Histone Methyltransferase | Chromatin/Epigenetic; MAPK |
BAY-6035 是 SET 和 MYND 结构域蛋白 3 (SMYD3) 的抑制剂。 BAY-6035 的选择性比其他组蛋白甲基转移酶高 100 倍以上。 | |||
T3099 |
Pinometostat
EPZ-5676 |
Histone Methyltransferase | Chromatin/Epigenetic |
Pinometostat (EPZ-5676) 是有效的DOT1L 组蛋白甲基转移酶抑制剂,Ki 为 80 pM。它可用于研究多种白血病治疗的实验。 | |||
T3257 |
UNC0638
|
Influenza Virus; Histone Methyltransferase; Autophagy | Autophagy; Chromatin/Epigenetic; Microbiology/Virology |
UNC0638 是 β-蛋白赖氨酸甲基转移酶 G9a 和 GLP 的抑制剂,选择性抑制表观遗传和非表观遗传靶标。 | |||
T3458 |
EED226
|
Histone Methyltransferase | Chromatin/Epigenetic |
EED226 是多梳抑制复合物 2 抑制剂,是一种有效的、选择性的、可口服的胚胎外胚层发育 (EED) 抑制剂,IC50 为 22 nM,具有强抗肿瘤活性。当 H3K27me0 肽用作体外酶法测定的底物时,它抑制 PRC2的 IC50为 23.4 nM。 | |||
T14841 |
BVT948
|
Phosphatase; P450; Histone Methyltransferase | Chromatin/Epigenetic; Metabolism |
BVT948 是一种蛋白酪氨酸磷酸酶抑制剂,还可以抑制赖氨酸甲基转移酶 SETD8 (KMT5A) 和几种细胞色素 P450 (P450) 同工型。 | |||
T4166 |
UNC0642
UNC-0642,UNC 0642 |
Histone Methyltransferase | Chromatin/Epigenetic |
UNC0642是有效选择性赖氨酸甲基转移酶G9a 和GLP 抑制剂, 抑制G9a 的IC50值小于2.5 nM。 | |||
T40254 |
MRTX-1719
|
Histone Methyltransferase | Chromatin/Epigenetic |
MRTX-1719 是有效的PRMT5/MTA 复合体选择性抑制剂,其对PRMT5/MTAMTAPDELSDMA 细胞系的IC50值为 <10 nM。 | |||
T13954 |
UNC6852
|
Histone Methyltransferase; Ligands for Target Protein for PROTAC; PROTACs | Chromatin/Epigenetic; PROTAC |
UNC6852 包含一个 EED 配体 (IC50 = 247 nM) 和一个 von Hippel-Lindau 配体,是一种基于 PROTAC 的特异性多梳抑制复合物 2 (PRC2) 降解剂。 | |||
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。 | |||
T27133 |
DCLX069
DCLX 069,DCLX-069 |
Histone Methyltransferase | Chromatin/Epigenetic |
DCLX069 是一种选择性蛋白精氨酸甲基转移酶 1 抑制剂,IC50值为 17.9 µM,对 PRMT4 和 PRMT6 的活性较低。它可有效阻断乳腺癌、肝癌和急性髓性白血病细胞系中的细胞增殖。 | |||
T7305 |
JQEZ5
|
Histone Methyltransferase | Chromatin/Epigenetic |
JQEZ5 是一种选择性EZH2赖氨酸甲基转移酶抑制剂,具有抗肿瘤作用。它以 SAM 竞争性方式抑制PRC2的酶功能,IC50为 80 nM。 | |||
T2379 |
UNC1215
|
Apoptosis; Epigenetic Reader Domain; Histone Methyltransferase | Apoptosis; Chromatin/Epigenetic |
UNC1215 是一种选择性 L3MBTL3甲基赖氨酸结构域的拮抗剂,IC50为40 nM,Kd 为 120 nM。它可研究恶性脑瘤。 | |||
T7194 |
CM-272
|
Apoptosis; DNA Methyltransferase; Histone Methyltransferase | Apoptosis; Chromatin/Epigenetic |
CM-272 是一种可逆底物竞争性双重G9a/DNA 甲基转移酶选择性抑制剂,具有抗肿瘤活性。它抑制细胞增殖并促进细胞凋亡,诱导干扰素刺激的基因和免疫原性细胞死亡。它抑制G9a、DNMT1、DNMT3A、DNMT3B 和GLP,IC50分别为 8 nM、382 nM、85 nM、1200 nM 和 2 nM。 | |||
T12428L |
PF-06726304
|
Histone Methyltransferase | Chromatin/Epigenetic |
PF-06726304 是选择性EZH2有效抑制剂,具有强抗肿瘤生长活性。它抑制野生型和 Y641N 突变型 EZH2,Ki 分别为 0.7 和 3.0 nM。 | |||
T28996 |
TP-064
TP 064 |
Histone Methyltransferase | Chromatin/Epigenetic |
TP-064 是选择性蛋白精氨酸甲基转移酶 4 抑制剂 ,IC50小于10 nM,具有抗癌活性。它抑制 BAF155 和 MED12 的二甲基化,IC50为 340 和 43 nM。它对于 PRMT6 的 IC50为 1.3 μM。 | |||
T13279L |
Valemetostat
DS-3201 |
Histone Methyltransferase | Chromatin/Epigenetic |
Valemetostat (DS-3201) 是一种EZH1/2抑制剂,可用于研究复发/难治性周围 T 细胞淋巴瘤。 | |||
T5605 |
EZM 2302
GSK3359088 |
Histone Methyltransferase | Chromatin/Epigenetic |
EZM 2302 (GSK3359088) 是选择性口服精氨酸甲基转移酶 CARM1 抑制剂,IC50值为 6 nM。 | |||
T4378 |
MS049
|
Histone Methyltransferase | Chromatin/Epigenetic |
MS049 是一种有效的、选择性的和细胞活性的 PRMT4 和 PRMT6 双重抑制剂,IC50 分别为 34 和 43 nM。它可降低 HEK293 细胞的 Med12me2a 和 H3R2me2a 水平。 | |||
T11486 |
GSK2807 Trifluoroacetate
|
Histone Methyltransferase | Chromatin/Epigenetic |
GSK2807 Trifluoroacetate 是一种选择性和 SAM 竞争性的 SMYD3 抑制剂,IC50为 130 nM,Ki 值为 14 nM。 | |||
T2352 |
AMI-1
|
Histone Methyltransferase | Chromatin/Epigenetic |
AMI1 是一种有效的、可逆的、细胞渗透性的蛋白精氨酸 N-甲基转移酶 (PRMTs) 抑制剂,对人 PRMT1 和酵母 Hmt1p 作用的 IC50值分别为 8.8 和 3.0 μM。它通过阻断肽-底物结合对 PRMTs 发挥抑制作用。 | |||
T17204 |
UNC0321
|
Histone Methyltransferase | Chromatin/Epigenetic |
UNC0321 是一种有效的组蛋白甲基转移酶 G9a 抑制剂,在 ECSD 和 CLOT 测定中,Ki 为 63 pM,IC50 分别为 9 nM 和 6 nM。 UNC0321 抑制 GLP,在 ECSD 和 CLOT 试验中 IC50 分别为 15 nM 和 23 nM。 | |||
T2079 |
GSK126
GSK2816126A,EZH2 inhibitor |
Histone Methyltransferase | Chromatin/Epigenetic |
GSK126 (GSK2816126A) 是一种 EZH2 甲基转移酶抑制剂 (IC50=9.9 nM),具有有效性和选择性。GSK126 具有抗肿瘤活性,可以抑制肿瘤细胞增殖、抑制血管生成。 | |||
T2354 |
UNC 0631
UNC0631 |
Histone Methyltransferase | Chromatin/Epigenetic |
UNC 0631 是一种有效的组蛋白甲基转移酶 G9a 抑制剂,IC50值为 4 nM。它有效降低 MDA-MB-231 细胞中 H3K9me2的水平,IC50为 25 nM。 | |||
T6333 |
MM-102
MM102,HMTase Inhibitor IX |
Histone Methyltransferase | Chromatin/Epigenetic |
MM-102 (HMTase Inhibitor IX) 是一种有效的 WDR5/MLL 相互作用抑制剂,在 WDR5 结合检测中,IC50为 2.4 nM,Ki 小于 1 nM。 | |||
T6360 |
3-deazaneplanocin A HCl
|
Others; Histone Methyltransferase | Chromatin/Epigenetic; Others |
3-deazaneplanocin A HCl 是组蛋白甲基转移酶 (EZH2) 和 S-腺苷同型半胱氨酸水解酶 (AHCY) 抑制剂。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T8201 |
Gambogenic acid
|
Histone Methyltransferase | Chromatin/Epigenetic |
Gambogenic acid 是黄藤中的一种有效成分,具有抗癌活性。它是特异性EZH2抑制剂,与 EZH2-SET 结构域的 Cys668 位点共价结合,诱导 EZH2 泛素化。 | |||
T6803 |
Chaetocin
毛壳素 |
Histone Methyltransferase; Antibacterial; Antibiotic | Chromatin/Epigenetic; Microbiology/Virology |
Chaetocin 特异性抑制组蛋白甲基转移酶(HMT) SU(VAR)3-9,IC50值为0.6 μM。它还可抑制硫氧还蛋白还原酶,IC50值为4 μM。 |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPY-01708 |
DOT1L Protein, Human, Recombinant
DOT1,KMT4,DOT1-like histone H3K79 methyltransfe... |
Human | E. coli |
Histone-lysine N-methyltransferase, H3 lysine-79 specific, also known as Histone H3-K79 methyltransferase, DOT1-like protein, Lysine N-methyltransferase 4 and DOT1L, is a nucleus protein which belongs to theDOT1 family. In contrast to other lysine histone methyltransferase, DOT1L does not contain a SET domain, suggesting the existence of another mechanism for methylation of lysine residues of histones. DOT1L is an histone methyltransferase. It methylates 'Lys-79' of histone H3. Nucleosome... | |||
TMPH-02105 |
ASH2L Protein, Human, Recombinant (His & SUMO)
ASH2-like protein,ASH2L,ASH2L1,Set1/Ash2 histone |
Human | E. coli |
Transcriptional regulator. Component or associated component of some histone methyltransferase complexes which regulates transcription through recruitment of those complexes to gene promoters. Component of the Set1/Ash2 histone methyltransferase (HMT) complex, a complex that specifically methylates 'Lys-4' of histone H3, but not if the neighboring 'Lys-9' residue is already methylated. As part of the MLL1/MLL complex it is involved in methylation and dimethylation at 'Lys-4' of histone H3. May p... | |||
TMPH-01526 |
KMT2E Protein, Human, Recombinant (His & Myc)
Inactive histone-lysine N-methyltransferase |
Human | E. coli |
Associates with chromatin regions downstream of transcriptional start sites of active genes and thus regulates gene transcription. Chromatin interaction is mediated via the binding to tri-methylated histone H3 at 'Lys-4' (H3K4me3). Key regulator of hematopoiesis involved in terminal myeloid differentiation and in the regulation of hematopoietic stem cell (HSCs) self-renewal by a mechanism that involves DNA methylation. Also acts as an important cell cycle regulator, participating in cell cycle r... | |||
TMPH-01484 |
SMYD3 Protein, Human, Recombinant (His & Myc)
Zinc finger MYND domain-containing protein 1,SMYD3,SET and M... |
Human | E. coli |
SMYD3 Protein, Human, Recombinant (His & Myc) is expressed in E. coli. | |||
TMPY-01229 |
SETD7 Protein, Human, Recombinant (His)
SET7/9,SET domain containing (lysine methyltransferase |
Human | E. coli |
Histone-lysine N-methyltransferase SETD7, also known as SET domain containing (lysine methyltransferase) 7, SET7/9, Histone H3-K4 methyltransferase SETD7, H3-K4-HMTase SETD7, and SETD7, is a member of the histone-lysine methyltransferase family and SET7 subfamily. SETD7 is widely expressed and expressed in pancreatic islets. SETD7 contains three MORN repeats and one SET domain. SETD7 plays a central role in the transcriptional activation of genes such as collagenase or insulin. As a protein lysi... | |||
TMPY-01657 |
SUV420H2 Protein, Human, Recombinant (His & GST)
suppressor of variegation 4-20 homolog 2 (Drosophila),KMT5C |
Human | E. coli |
Histone-lysine N-methyltransferase SUV42H2, also known as Suppressor of variegation 4-2 homolog 2, Su(var)4-2 homolog 2, Lysine N-methyltransferase 5C, SUV42H2 and KMT5C, is nucleus protein that belongs to the histone-lysine methyltransferase family and Suvar4-2 subfamily. SUV42H2 is a histone methyltransferase that specifically trimethylates 'Lys-2' of histone H4. H4 'Lys-2' trimethylation represents a specific tag for epigenetic transcriptional repression. SUV42H2 mainly functions in pericentr... | |||
TMPH-02227 |
ERG Protein, Human, Recombinant (His)
Transcriptional regulator ERG,Transforming protein ERG,ERG |
Human | P. pastoris (Yeast) |
Transcriptional regulator. May participate in transcriptional regulation through the recruitment of SETDB1 histone methyltransferase and subsequent modification of local chromatin structure. ERG Protein, Human, Recombinant (His) is expressed in yeast with N-6xHis tag. The predicted molecular weight is 56.6 kDa and the accession number is P11308. | |||
TMPY-01383 |
PRMT6 Protein, Human, Recombinant (His & Flag)
protein arginine methyltransferase 6,HRMT1L6 |
Human | HEK293 Cells |
Protein arginine N-methyltransferase 6, also known as Histone-arginine N-methyltransferase PRMT6, PRMT6, and HRMT1L6, is a member of the protein arginine N-methyltransferase family and PRMT6 subfamily. PRMT6 is highly expressed in kidney and testes. PRMT6 is known to catalyze the generation of asymmetric dimethylarginine in polypeptides. It has been implicated in human immunodeficiency virus pathogenesis, DNA repair, and transcriptional regulation. PRMT6 is known to methylate histone H3 Arg-2 (H... | |||
TMPY-01268 |
SMYD3 Protein, Human, Recombinant (GST)
SET and MYND domain containing 3,ZMYND1,KMT3E,ZNFN3A1,bA74P1... |
Human | Baculovirus Insect Cells |
SET and MYND domain-containing protein 3, also known as Zinc finger MYND domain-containing protein 1, SMYD3, and ZMYND, is a member of the histone-lysine methyltransferase family. SMYD3 contains one MYND-type zinc finger and one SET domain. SMYD3 is a histone H3 lysine-4-specific methyltransferase. It is expressed in skeletal muscles and testis. It is overexpressed in a majority of colorectal carcinoma (CRC) and hepatocellular carcinoma (HCC). SMYD3 plays an important role in transcriptional reg... | |||
TMPY-04403 |
NLK/Nemo Like Kinase Protein, Human, Recombinant (His & GST)
nemo-like kinase,LAK1 |
Human | Baculovirus Insect Cells |
Nemo-like kinase contains 1 protein kinase domain and belongs to the protein kinase superfamily, CMGC Ser/Thr protein kinase family, and MAP kinase subfamily. It also contains a TQE activation loop motif in which autophosphorylation of the threonine residue (Thr-298) is sufficient for kinase activation. As a serine/threonine-protein kinase, Nemo-like kinase regulates some transcription factors with key roles in cell fate determination. It is a positive effector of the non-canonical Wnt signaling... | |||
TMPJ-01040 |
MAX Protein, Human, Recombinant (His)
Protein Max,MAX,bHLHd4,Myc-Associated Factor X,Class D Basic... |
Human | E. coli |
Myc-Associated Factor X (MAX) is a member of the basic helix-loop-helix leucine zipper (bHLHZ) family of transcription factors. It contains 1 basic helix-loop-helix (bHLH) domain. It is found in the brain, heart, and lung at high levels while lower levels are seen in the liver, kidney, and skeletal muscle. MAX forms a sequence-specific DNA-binding protein complex with MYC or MAD which recognizes the core sequence 5'-CAC[GA]TG-3'. The MYC-MAX complex is a transcriptional activator, whereas the MA... | |||
TMPY-02888 |
MAX Protein, Human, Recombinant (His & GST)
MYC associated factor X,bHLHd4 |
Human | Baculovirus Insect Cells |
MYC associated factor X contains 1 basic helix-loop-helix (bHLH) domain and belongs to the MAX family. It is highly expressed in the brain, heart, and lung while lower levels are seen in the liver, kidney, and skeletal muscle. MYC associated factor X can form homodimers and heterodimers with other family members, which include Mad, Mxi1, and Myc. Myc is an oncoprotein implicated in cell proliferation, differentiation, and apoptosis. The homodimers and heterodimers compete for a common DNA target... |