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19

抑制剂 & 化合物

1

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T9575	MRTX9768	Histone Methyltransferase	Chromatin/Epigenetic
	MRTX-9768 是一种有效的、选择性的、具有口服活性的 PRMT5-MTA 复合体抑制剂，可选择性靶向 MTAP/CDKN2A 缺失的肿瘤。
T14141	AGI-24512	Others; Methionine Adenosyltransferase (MAT)	Chromatin/Epigenetic; Others
	AGI-24512 是一种甲硫氨酸腺苷转移酶 2A 抑制剂，在体外能够阻断 MTAP 缺失的癌细胞的生长，可用于研究癌症。
TQ0008	MT-DADMe-ImmA Methylthio-DADMe-Immucillin A,MTDIA	Others	Others
	MT-DADMe-ImmA (MTDIA) 是一种人5'-甲硫基腺苷磷酸化酶的抑制剂 (MTAP)(Ki:90 pM)。
T73494	TNG908
	TNG908 是一种可通过血脑屏障的 MTAP-协同PRMT5抑制剂，TNG908 对 MTAP 细胞系的选择性比 MTAPWT 细胞系高 15倍，可用于癌症研究。
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。
T31672	Erythrofuranosyladenine 9-β-D-Erythrofuranosyladenine,ETA
	Erythrofuranosyladenine(9-beta-D-Erythrofuranosyladenine, ETA) is a nontoxic MTAP substrate. Erythrofuranosyladenine is an effective salvage agent for methylthioadenosine phosphorylase–selective therapy of T-cell acute lymphoblastic leukemia with L-alanos
T33517	MTDIA HCl MTDIA,Methylthio-DADMe-Immucillin A,MT-DADMe-ImmA,MT-DADMe-ImmA HCl
	MTDIA (MT-DADMe-ImmA and methylthio-DADMe-Immucillin A) is an MTAP inhibitor.
T10259	AGI-25696	Others; Methionine Adenosyltransferase (MAT)	Chromatin/Epigenetic; Others
	AGI-25696 是甲硫氨酸腺苷转移酶 2A (MATA2) 的抑制剂。 AGI-25696 在体内阻断 MTAP 缺失肿瘤的生长，可用于癌症治疗的研究。
T79873	TNG-462	Histone Methyltransferase	Chromatin/Epigenetic
	TNG-462(化合物1143)作为一种口服有效的PRMT5抑制剂，适用于研究MTAP缺失型及/或MTA累积型癌症。
T36630	MRTX9768 hydrochloride
	MRTX9768 hydrochloride is a potent, orally active PRMT5 inhibitor. MRTX9768 hydrochloride is a synthetic lethal-based inhibitor binding the PRMT5-MTA complex[1]. MRTX9768 inhibits SDMA and cell proliferation in HCT116 MTAP-del cells (SDMA IC50 3 nM; prolif. IC50 11 nM) with marked selectivity over HCT116 MTAP-WT cells (SDMA IC50 544 nM; prolif. IC50 861 nM)[1].MRTX9768 selectively targets MTAP/CDKN2A-deleted tumors[2][1]. In xenograft studies, oral administration of MRTX9768 demonstrates dose-de...
T79350	MAT2A-IN-12	Methionine Adenosyltransferase (MAT)	Chromatin/Epigenetic
	MAT2A Allosteric inhibitor 2是一种有效的、选择性MAT2A变构抑制剂，具有5 nM的IC50值。在增殖试验（MTAP-/-细胞系）中，MAT2A Allosteric inhibitor 2表现出纳摩尔级别的活性，IC50为5 μM。
T69811	AGI25696
	AGI-25696 is a MATA2 inhibitor that are useful as therapeutic agents for treating malignancies. AGI-25696 showed in vivo activity in MTAP null tumors. Note: The correct structure of AGI-25696 is CAS#2201065-84-9. Many vendors mistakenly listed CAS#2201066-35-3 as its AGI25696. J. Med. Chem. 2021, 64, 8, 4430–4449 published AGI25696 structure (it is CAS#2201065-84-9).
T62100	MAT2A-IN-6
	MAT2A-IN-6 是一种 MAT2A 的有效抑制剂。其中 MAT2A 在几种类型的肿瘤中（包括胃癌、结肠癌、肝癌和胰腺癌）的表达水平异常升高。MAT2A-IN-6 能够减少 MTAP 缺陷癌细胞的增殖活性。MAT2A-IN-6 对癌症疾病表现出潜在的研究价值。
T63603	MAT2A-IN-3
	MAT2A-IN-3 是 MAT2A 的有效抑制剂。其中 MAT2A 的表达水平在包括胃癌、结肠癌、肝癌和胰腺癌在内的几种类型的肿瘤中显著升高。MAT2A-IN-3 能够抑制 MTAP 缺陷型癌细胞的增殖活性。MAT2A-IN-3 对癌症疾病表现出研究潜力。
T15691	L-Alanosine NSC-153353,丙氨菌素	Others	Others
	L-Alanosine inhibits adenylosuccinate synthetase. L-Alanosine is an antibiotic from Streptomyces alanosinicus with antineoplastic activity. L-Alanosine blocks the common de novo purine biosynthesis pathway and, thereby, inhibit tumor cells with MTAP defic
T63975	MAT2A-IN-1
	MAT2A-IN-1 是 MAT2A 的有效抑制剂，能够 MTAP 缺陷型癌细胞的增殖活性。其中 MAT2A 在几种类型肿瘤中表达水平异常高，包括胃癌、结肠癌、肝癌和胰腺癌。MAT2A-IN-1 对癌症疾病表现出研究潜力。
T61672	MAT2A-IN-7
	MAT2A-IN-7, a potent inhibitor of the enzyme MAT2A, demonstrates efficacy in targeting the abnormally elevated expression of MAT2A observed in gastric, colon, liver, and pancreatic cancers. Furthermore, MAT2A-IN-7 effectively reduces the proliferative activity specifically in MTAP-deficient cancer cells, thus highlighting its potential for cancer research applications [1].
T61243	MAT2A-IN-5
	MAT2A-IN-5, a potent inhibitor of MAT2A, effectively targets the abnormally elevated expression of MAT2A found in various tumor types such as gastric, colon, liver, and pancreatic cancers. By reducing the proliferative activity of MTAP-deficient cancer cells, MAT2A-IN-5 exhibits potential in cancer research applications [1].
T62984	MAT2A-IN-2
	MAT2A-IN-2 是一种 MAT2A 的有效抑制剂。其中 MAT2A 的表达水平在几种类型的肿瘤（包括胃癌、结肠癌、肝癌和胰腺癌）中异常高。MAT2A-IN-2 能够减少 MTAP 缺陷型癌细胞的增殖活性。MAT2A-IN-2 具有潜力进行癌症疾病的研究。

化合物

Cat.No: T9575

Target: Histone Methyltransferase

Cat.No: T14141

Target: Others, Methionine Adenosyltransferase (MAT)

Cat.No: TQ0008

Synonym: Methylthio-DADMe-Immucillin A,MTDIA

Target: Others

Cat.No: T73494

Cat.No: T40254

Target: Histone Methyltransferase

Erythrofuranosyladenine

Cat.No: T31672

Synonym: 9-β-D-Erythrofuranosyladenine,ETA

Cat.No: T33517

Synonym: MTDIA,Methylthio-DADMe-Immucillin A,MT-DADMe-ImmA,MT-DADMe-ImmA HCl

Cat.No: T10259

Target: Others, Methionine Adenosyltransferase (MAT)

Cat.No: T79873

Target: Histone Methyltransferase

MRTX9768 hydrochloride

Cat.No: T36630

Cat.No: T79350

Target: Methionine Adenosyltransferase (MAT)

Cat.No: T69811

Cat.No: T62100

Cat.No: T63603

Cat.No: T15691

Synonym: NSC-153353,丙氨菌素

Target: Others

Cat.No: T63975

Cat.No: T61672

Cat.No: T61243

Cat.No: T62984

Cat. No.	Product Name	Target	Signaling Pathways
T8227	5'-Methylthioadenosine Methylthioadenosine,5-脱氧-5-甲硫腺苷,5'-(Methylthio)-5'-deoxyadenosine,5'-Deoxy-5'-(methylthio)adenosine,5'-S-Methyl-5'-thioadenosine	Endogenous Metabolite	Metabolism
	5'-Methylthioadenosine (Methylthioadenosine) 是由 S-腺苷蛋氨酸在多胺合成过程中生成的核苷，通过抑制肿瘤细胞增殖、侵袭和诱导细胞凋亡来抑制肿瘤，同时控制肿瘤组织的炎症微环境。

天然产物

5'-Methylthioadenosine

Cat.No: T8227

Synonym: Methylthioadenosine,5-脱氧-5-甲硫腺苷,5'-(Methylthio)-5'-deoxyadenosine,5'-Deoxy-5'-(methylthio)adenosine,5'-S-Methyl-5'-thioadenosine

Target: Endogenous Metabolite

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