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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T6364 |
Desfesoterodine
5-HMT,(R)-5-Hydroxymethyl Tolterodine,(R)-5-羟甲基托特罗定,PNU-200577,5-HM,5-hydroxymethyl Tolterodine |
AChR | Neuroscience |
Desfesoterodine (5-HMT) 是选择性毒蕈碱受体拮抗剂,Kb 和pA2分别为 0.84 nM 和 9.14。它可改善大鼠脑梗死诱导膀胱过度活动,是 Tolterodine 和 Fesoterodine 的主要药理活性代谢产物。 | |||
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。 | |||
T9419 |
Fesoterodine
(R) Fesoterodine,弗斯特罗定 |
AChR | Neuroscience |
Fesoterodine ((R) Fesoterodine) 是可口服的,非亚型选择性的竞争性毒蕈碱受体拮抗剂,用于膀胱过度活动症,对 M1、M2、M3、M4 和 M5 受体的pKi 值分别为 8.0、7.7、7.4、7.3 和 7.5。 | |||
T1475 |
Fesoterodine fumarate
Toviaz,SPM 907,富马酸非索罗定 |
AChR | Neuroscience |
Fesoterodine fumarate (Toviaz) 是可口服的,非亚型选择性的竞争性毒蕈碱受体拮抗剂,用于膀胱过度活动症,对 M1、M2、M3、M4 和 M5 受体的pKi 值分别为 8.0、7.7、7.4、7.3 和 7.5。 | |||
T62404 |
SHMT-IN-2
|
Others | Others |
SHMT-IN-2 (compound 2) 是一种特异性人 SHMT1/2 小分子抑制剂,能够作用于 SHMT1 (IC50: 13 nM) 和 SHMT2 (IC50: 66 nM)。SHMT-IN-2 对许多人类癌细胞的生长具有抑制作用,对 B 细胞淋巴瘤具有敏感性。 | |||
T62512 |
IHMT-MST1-58
|
Hippo pathway | Stem Cells |
IHMT-MST1-58 是一种 STE20-like protein 1 kinase (MST1) 抑制剂(IC50 :23 nM),具有高效性、选择性和口服活性。IHMT-MST1-58 可用于研究 1 型或 2 型糖尿病。 | |||
T35530 |
IHMT-PI3Kδ-372
IHMT-PI3Kδ-372 |
PI3K | PI3K/Akt/mTOR signaling |
IHMT-PI3Kδ-372 是一种选择性的 PI3Kδ 抑制剂,IC50 为 14 nM,可用于慢性阻塞性肺病的研究。 | |||
T12902 |
SHMT-IN-1
|
Others | Others |
SHMT-IN-1 是有效的血浆丝氨酸羟甲基转移酶 (SHMT) 抑制剂。SHMT-IN-1 具有抗肿瘤活性。 | |||
T60196 |
IHMT-PI3Kδ-372 S-isomer
|
PI3K | PI3K/Akt/mTOR signaling |
IHMT-PI3Kδ-372 S-isomer 是一种有效的选择性 PI3Kδ 抑制剂,IC50 为 14 nM。IHMT-PI3Kδ-372 S-isomer 对 PI3Kδ 的选择性高于其他 I 类 PI3K (56-83 倍) 和其他蛋白激酶。IHMT-PI3Kδ-372 S-isomer 可用于慢性阻塞性肺疾病 (COPD )的研究。 | |||
T78758 |
IHMT-IDH1-053
|
Isocitrate Dehydrogenase (IDH) | Metabolism |
IHMT-IDH1-053(compound 16)为高选择性不可逆IDH1R132H突变抑制剂,IC50值仅为4.7 nM。对IDH1wt和IDH2wt/突变体活性低。该化合物在IDH1R132H突变293T细胞中显著抑制2-羟基戊二酸(2-HG)生成,IC50为28 nM。IHMT-IDH1-053通过与IDH1R132H蛋白的Cys269残基形成共价键,结合至NADPH结合袋附近的变构袋。此外,它能够抑制携带IDH1R132突变的HT1080细胞系及原代AML细胞增殖。 | |||
TP1460 |
NH2-KLGADTDGEQDQHMTYGGQ-COOH
|
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NH2-QGGYTMHQDQEGDTDAGLK-COOH is a synthetic peptide chain consisting of a primary amine group attached to lysine and a carboxyl group attached to glutamine. | |||
T78836 |
IHMT-PI3K-455
|
PI3K | PI3K/Akt/mTOR signaling |
IHMT-PI3K-455(Compound 15u)为一种高效、选择性且具口服活性的PI3Kγ/δ双重抑制剂,其针对PI3Kγ与PI3Kδ的IC50值分别为7.1 nM和0.57 nM。该化合物能够抑制AKT磷酸化,并通过促进CD8+杀伤性T细胞的招募与激活,抑制肿瘤生长,适用于肿瘤学研究领域。 | |||
T63076 |
IHMT-TRK-284
|
||
IHMT-TRK-284 (Compound 34) 是一种有效的、口服具有活力的 type II TRK kinase 抑制剂,能够作用于 TRKA (IC50: 10.5 nM)、TRKB (IC50: 0.7 nM)、TRKC (IC50: 2.6 nM)。IHMT-TRK-284 在激酶组中表现出良好的选择性,体内具有良好的抗肿瘤作用。 | |||
T11167 |
EHMT2-IN-2
|
Others | Others |
EHMT2-IN-2 Used in the research of blood disease or cancer. EHMT2-IN-2 is a potent EHMT inhibitor, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2. | |||
T11166 |
EHMT2-IN-1
|
Others | Others |
EHMT2-IN-1 is a potent EHMT inhibitor, . Used in the research of blood disorder or cancer.with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2. | |||
T79780 |
IHMT-EZH2-426
|
Histone Methyltransferase | Chromatin/Epigenetic |
IHMT-EZH2-426(compound 38)是一种针对EZH2野生型及其A687V和Y641F/Y641N/Y641S突变体高效的共价降解剂,其IC50值分别为1.3 nM、1.2 nM以及1.7-3.5 nM。该化合物通过下调H3K27me3和EZH2蛋白表达水平,显著抑制B细胞淋巴瘤和三阴性乳腺癌(TNBC)细胞系的增殖。 | |||
T67947 |
WDR5-0102
|
Histone Methyltransferase | Chromatin/Epigenetic |
WDR5-0102为针对WDR5-MLL1的抑制剂(Kdis=7 μM, Kd=4 μM)。该化合物有效抑制MLL1活性,而对人类H3K4甲基转移酶SETD7及其他六种HMT(G9a、EHMT1、SUV39H2、SETD8、PRMT3、PRMT5)不表现出抑制作用。 | |||
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。 | |||
T8768 |
MM-102 TFA
HMTase Inhibitor IX TFA |
Histone Methyltransferase | Chromatin/Epigenetic |
MM-102 TFA (HMTase Inhibitor IX TFA) 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。 | |||
T13334 | WDR5-IN-1 | Others | Others |
WDR5-IN-1 is a potent and selective inhibitor of WD repeat domain 5 (WDR5) (Kd <0.02 nM), and also inhibits MLL1 histone methyltransferase (HMT) activity (IC50: 2.2 nM). | |||
T38784 |
Histone H3 (1-25), amide
Histone H3 (1-25), amide |
||
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. | |||
T12091 |
MM-589
|
JAK | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
MM-589 is a potent WD repeat domain 5 (WDR5) inhibitor and mixed lineage leukemia (MLL) protein-protein interaction. | |||
T12091L |
MM-589 TFA
|
JAK | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
MM-589 TFA is a potent WD repeat domain 5 (WDR5)inhibitor and mixed lineage leukemia (MLL) protein-protein interaction. |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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 |
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TMPY-02340 |
HNMT Protein, Human, Recombinant (GST)
HMT,HNMT-S1,HNMT-S2,histamine N-methyltransferase |
Human | E. coli |
HNMT (Histamine N-methyltransferase) is a Protein Coding gene. This gene encodes the first enzyme which is found in the cytosol and uses S-adenosyl-L-methionine as the methyl donor. HNMT, the major enzyme for the metabolism of histamine in the rat brain, is potently inhibited by 9-amino-1,2,3,4-tetrahydroacridine (tacrine). Methylation is an important pathway in the biotransformation of many drugs, neurotransmitters, and xenobiotic compounds. Histamine N-methyltransferase (HNMT) catalyzes the N ... | |||
TMPY-02386 |
PTP4A2 Protein, Human, Recombinant (GST)
HNMT-S2,PRL-2,HNMT-S1,protein tyrosine phosphatase type IVA,... |
Human | E. coli |
PRL-2 (Protein-tyrosine phosphatase of regenerating liver 2), also known as PTP4A2 (Protein tyrosine phosphatase type IVA, member 2), is a member of PTP family and has an important function in controlling cell growth. PRL-2 phosphatases may be multifunctional enzymes with diverse roles in a variety of tissue and cell types. The phosphatase of regenerating liver (PRL) family, comprising PRL-1, PRL-2 and PRL-3, is a group of prenylated phosphatases that are candidate cancer biomarkers and therapeu... | |||
TMPK-01552 |
HLA-A*02:01&B2M&P53 R175H (HMTEVVRHC) Monomer Protein, Human, MHC (His & Avi), Biotinylated
TP53,TRP53,HLA-A,MHC,Antigen NY-CO-13,BCC7,LFS1,P53,FLJ92943 |
Human | HEK293 Cells |
p53 is a tumor suppressor protein. Under stressful conditions, p53 tightly regulates cell growth by promoting apoptosis and DNA repair. When p53 becomes mutated, it loses its function, resulting in abnormal cell proliferation and tumor progression. Depending on the p53 mutation, it has been shown to form aggregates leading to negative gain of function of the protein.p53 mutant associated aggregation has been observed in several cancer tissues and has been shown to promote tumor growth. | |||
TMPK-01442 |
HLA-A*02:01&B2M&P53 WT (HMTEVVRRC) Tetramer Protein, Human, MHC (His & Avi), PE-Labeled
HLA-A,P53,TP53,LFS1,MHC,BCC7,TRP53,FLJ92943,Antigen NY-CO-13 |
Human | HEK293 Cells |
p53 is a tumor suppressor protein. Under stressful conditions, p53 tightly regulates cell growth by promoting apoptosis and DNA repair. When p53 becomes mutated, it loses its function, resulting in abnormal cell proliferation and tumor progression. Depending on the p53 mutation, it has been shown to form aggregates leading to negative gain of function of the protein. p53 mutant associated aggregation has been observed in several cancer tissues and has been shown to promote tumor growth. | |||
TMPK-01437 |
HLA-A*02:01&B2M&P53 R175H (HMTEVVRHC) Tetramer Protein, Human, MHC (His & Avi), PE-Labeled
FLJ92943,HLA-A,TP53,Antigen NY-CO-13,TRP53,MHC,BCC7,P53,LFS1 |
Human | HEK293 Cells |
p53 is a tumor suppressor protein. Under stressful conditions, p53 tightly regulates cell growth by promoting apoptosis and DNA repair. When p53 becomes mutated, it loses its function, resulting in abnormal cell proliferation and tumor progression. Depending on the p53 mutation, it has been shown to form aggregates leading to negative gain of function of the protein.p53 mutant associated aggregation has been observed in several cancer tissues and has been shown to promote tumor growth. | |||
TMPK-01531 |
HLA-A*02:01&B2M&P53 R175H (HMTEVVRHC) Tetramer Protein, Human, MHC (His & Avi)
Antigen NY-CO-13,MHC,FLJ92943,TRP53,HLA-A,BCC7,TP53,LFS1,P53 |
Human | HEK293 Cells |
p53 is a tumor suppressor protein. Under stressful conditions, p53 tightly regulates cell growth by promoting apoptosis and DNA repair. When p53 becomes mutated, it loses its function, resulting in abnormal cell proliferation and tumor progression. Depending on the p53 mutation, it has been shown to form aggregates leading to negative gain of function of the protein.p53 mutant associated aggregation has been observed in several cancer tissues and has been shown to promote tumor growth. | |||
TMPK-01538 |
HLA-A*02:01&B2M&P53 WT (HMTEVVRRC) Monomer Protein, Human, MHC (His & Avi), Biotinylated
MHC,LFS1,Antigen NY-CO-13,HLA-A,BCC7,TP53,TRP53,FLJ92943,P53 |
Human | HEK293 Cells |
p53 is a tumor suppressor protein. Under stressful conditions, p53 tightly regulates cell growth by promoting apoptosis and DNA repair. When p53 becomes mutated, it loses its function, resulting in abnormal cell proliferation and tumor progression. Depending on the p53 mutation, it has been shown to form aggregates leading to negative gain of function of the protein. p53 mutant associated aggregation has been observed in several cancer tissues and has been shown to promote tumor growth. | |||
TMPK-01509 |
HLA-A*02:01&B2M&P53 WT (HMTEVVRRC) Monomer Protein, Human, MHC (His & Avi)
TRP53,HLA-A,TP53,LFS1,P53,MHC,FLJ92943,BCC7,Antigen NY-CO-13 |
Human | HEK293 Cells |
p53 is a tumor suppressor protein. Under stressful conditions, p53 tightly regulates cell growth by promoting apoptosis and DNA repair. When p53 becomes mutated, it loses its function, resulting in abnormal cell proliferation and tumor progression. Depending on the p53 mutation, it has been shown to form aggregates leading to negative gain of function of the protein. p53 mutant associated aggregation has been observed in several cancer tissues and has been shown to promote tumor growth. | |||
TMPK-01532 |
HLA-A*02:01&B2M&P53 R175H (HMTEVVRHC) Monomer Protein, Human, MHC (His & Avi)
Antigen NY-CO-13,BCC7,FLJ92943,HLA-A,LFS1,P53,TP53,TRP53,MHC |
Human | HEK293 Cells |
p53 is a tumor suppressor protein. Under stressful conditions, p53 tightly regulates cell growth by promoting apoptosis and DNA repair. When p53 becomes mutated, it loses its function, resulting in abnormal cell proliferation and tumor progression. Depending on the p53 mutation, it has been shown to form aggregates leading to negative gain of function of the protein.p53 mutant associated aggregation has been observed in several cancer tissues and has been shown to promote tumor growth. | |||
TMPJ-00484 |
SHMT1 Protein, Human, Recombinant (His)
Serine Methylase,Glycine Hydroxymethyltransferase,Serine Hyd... |
Human | HEK293 Cells |
Serine Hydroxymethyltransferase Cytosolic (SHMT1) is a member of the SHMT family. SHMT1 is a cytoplasmic protein and exists as a homotetramer. SHMT1 catalyzes the reversible conversion of serine and tetrahydrofolate to glycine and 5,10-methylene tetrahydrofolate. This reaction provides one carbon unit for the synthesis of methionine, thymidylate, and purines in the cytoplasm. A reduction in SHMT1 levels would result in less glycine that could affect the nervous system by acting as an agonist to ... | |||
TMPK-01508 |
HLA-A*02:01&B2M&P53 WT (HMTEVVRRC) Tetramer Protein, Human, MHC (His & Avi)
TP53,Antigen NY-CO-13,P53,MHC,HLA-A,BCC7,LFS1,FLJ92943,TRP53 |
Human | HEK293 Cells |
p53 is a tumor suppressor protein. Under stressful conditions, p53 tightly regulates cell growth by promoting apoptosis and DNA repair. When p53 becomes mutated, it loses its function, resulting in abnormal cell proliferation and tumor progression. Depending on the p53 mutation, it has been shown to form aggregates leading to negative gain of function of the protein. p53 mutant associated aggregation has been observed in several cancer tissues and has been shown to promote tumor growth. | |||
TMPH-02105 |
ASH2L Protein, Human, Recombinant (His & SUMO)
ASH2-like protein,ASH2L,ASH2L1,Set1/Ash2 histone methyltrans... |
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... |