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抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T16133	MRK-560	Gamma-secretase	Neuroscience; Proteases/Proteasome; Stem Cells
	MRK-560 是高效的、口服有效的 γ- 分泌酶抑制剂抑制剂，具有大脑屏障渗透性。
T6603	Nelarabine GW 506U78,Nelzarabine,奈拉滨,506U78	Apoptosis; Nucleoside Antimetabolite/Analog; DNA/RNA Synthesis	Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	Nelarabine (GW 506U78) 是一种嘌呤核苷酸类似物，为DNA 合成抑制剂，对肿瘤细胞的IC50为0.067-2.15 μM，可作用于T 细胞急性淋巴细胞白血病。
T0370	Pheniramine maleate Daneral,Inhiston,Trimetose,马来酸非尼拉敏	5-HT Receptor; Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Pheniramine maleate (Trimetose) 是一种具有抗组胺和血管扩张特性的烷基胺衍生物，可与组胺 H1 受体结合，从而抑制磷脂酶 A2 和内皮源性松弛因子一氧化氮的产生。
T72984	(Rac)-SHIN2	Others	Others
	(Rac)-SHIN2 是一种丝氨酸羟甲基转移酶 (SHMT) 抑制剂，可提高 NOTCH1 驱动的小鼠原代 T-ALL 在体内的存活率，可用于研究 T 细胞急性淋巴细胞白血病（T-ALL）。
T3448	GJ103	Others	Others
	GJ103 是通读化合物 GJ072 的活性类似物。一些 GJ072 类似物（例如，GJ103、GJ106、GJ109 和 GJ111）通过 FCATMpSer1981 和 IRIF 测定一致地证明了它们在所有三种 PTC 中的活性。 GJ103 具有与 RTC13 或 RTC14 相似的通读活性，但比 RTC13 和 RTC14 对 A-T 细胞的耐受性更高。
T36944	Ara-G	Nucleoside Antimetabolite/Analog	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	Ara-G 是一种脱氧鸟苷 (GdR) 类似物和核苷类似物，可被 T 淋巴谱系细胞迅速转化为其相应的阿拉伯糖基鸟嘌呤核苷酸三磷酸 (araGTP)，从而抑制 DNA 合成和对 T 淋巴母细胞的选择性体外毒性细胞系以及来自 T 细胞急性淋巴细胞白血病 (ALL) 患者的新鲜分离的白血病细胞。
T79377	NWP-0476
	NWP-0476为针对BCL-2/BCL-xL的抑制剂，其结构已优化以提高对BCL-xL的选择性。该化合物适用于复发性T-急性淋巴细胞白血病（T-ALL）的相关研究。
T39799	S2157 S2157
	S2157, a potent N-alkylated tranylcypromine (TCP) derivative lysine-specific demethylase 1 (LSD1) inhibitor, enhances H3K9 methylation and concurrently reduces H3K27 acetylation at super-enhancer sites. This compound triggers apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by inhibiting NOTCH3 and TAL1 gene expression. Moreover, S2157 is capable of crossing the blood-brain barrier, effectively eliminating central nervous system (CNS) leukemia in mice models implanted...
T39800	S2116
	S2116 is a powerful inhibitor of lysine-specific demethylase 1 (LSD1), and it is a derivative of N-alkylated tranylcypromine (TCP). S2116 exhibits its inhibitory effects by increasing H3K9 methylation and inducing reciprocal H3K27 deacetylation at super-enhancer regions. In TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells, S2116 triggers apoptosis by repressing the transcription of NOTCH3 and TAL1 genes. Furthermore, S2116 demonstrates significant growth retardation of T-ALL cells...
T83930	SJ 11646
	SJ11646是一种高效的LCK（淋巴细胞特异性蛋白酪氨酸激酶）降解剂（PROTAC；DC50= 0.00838 pM）。该化合物由Dasatinib作为LCK配体，以及基于苯基谷氨酰亚胺的cereblon结合体组成。它在体外对LCK激活的T细胞急性淋巴细胞白血病（T-ALL）细胞株和初级白血病样本展现出细胞毒性。在体内，SJ11646在源自患者的T-ALL异种移植模型中显示出抗白血病效果。
T60966	UCPH-102
	UCPH-102 可用于研究阿尔茨海默病、肌萎缩性侧索硬化症、慢性疼痛和强迫症等，具有良好的血脑通透性。UCPH-102 是高度选择性的 EAAT1抑制剂，IC50值为0.43 μM。UCPH-102 还对 T-ALL 细胞表现出特异性的抗增殖作用。
T36693	FD-211
	FD-211 is a δ lactone originally isolated from M. lutea with anticancer activity.1 It is cytotoxic to adriamycin-susceptible P388, T-24, HeLa, A549, and HL-60 cancer cells (IC50s = 4, 0.5, 1, 1, and 0.2 μg/ml, respectively), as well as adriamycin-resistant HL-60/ADR cells (IC50 = 0.1 μg/ml). FD-211 also inhibits DNA, RNA, and protein synthesis in HeLa cells (IC50 = 1.25 μg/ml for all). \|1. Nozawa, O., Okazaki, T., Sakai, N., et al. A novel bioactive δ lactone FD-211. Taxonomy, isolation and char...
T37553	(-)-Mycousnine
	(-)-Mycousnine is a microbial metabolite and derivative of usnic acid originally isolated fromM. nawaethat has antibacterial and antifungal activities.1,2It is active against the Gram-positive bacteriaB. subtilis,K. rhizophila, andS. aureus(MICs = 4, 8, and 4 g/ml, respectively) but not the Gram-negative bacteriaE. coli,S. typhimurium, andK. pneumoniae(MICs = >128 g/ml for all).2(-)-Mycousnine is also active against the fungiT. mentagrophytes,T. rubrum, andC. albicans(MICs = 25, 25, and 100 μg/m...
T37887	1-Heptadecanoyl-rac-glycerol
	1-Heptadecanoyl-rac-glycerol is a monoacylglycerol that contains heptadecanoic acid at the sn-1 position. It is active against the bacteria E. aerogens, E. cloacae, P. mirabilis, and S. faecalis (MIC = 78 μg/ml for all).1 1-Heptadecanoyl-rac-glycerol has been found in T. africana, I. sonorae, and wheat bran.1,2,3 \|1. Kuete, V., Metuno, R., Ngameni, B., et al. Antimicrobial activity of the methanolic extracts and compounds from Treculia africana and Treculia acuminata (Moraceae). S. Afr. J. Bot. ...
T37536	Carbazomycin A
	Carbazomycin A is a bacterial metabolite that has been found in Streptomyces and has diverse biological activities.1,2It is active againstS. aureus,T. asteroides, andT. mentagrophytes(MIC = 12.5 μg/ml for all), as well as the plant pathogenic fungusP. oryzae(MIC = 25 μg/ml). Carbazomycin A is cytotoxic to MCF-7, KB, NCI H187, and Vero cells (IC50s = 26.2, 30.1, 18.4, and 32.6 μg/ml, respectively).2 1.Sakano, K.-I., Ishimaru, K., and Nakamura, S.New antibiotics, carbazomycins A and B. I. Fermenta...
T37330	Pyridindolol
	Pyrindolol is a bacterial metabolite that has been found inS. alboverticillatus.1It inhibits neutral β-galactosidase by 50% under acidic, but not neutral, conditions when used at a concentration of 2 μg/ml. It is selective for β-galactosidase isolated from bovine liver over β-galactosidases isolated from human, bovine, pig, and rat tissues and sialidases isolated fromC. perfringens,Streptomyces, and the H3N2 strain of influenza virus (IC50s = >250 μg/ml for all).1,2 1.Aoyagi, T., Kumagai, M., Ha...
T38381	CAY17c
	CAY17c is an inhibitor of bromodomain-containing protein 4 (BRD4; IC50= 0.71 μM), as well as class I histone deacetylases (HDACs; IC50s = 0.046, 0.058, 0.075, and 0.167 μM for HDAC1, -2, -3, and -8, respectively) and class IIb HDACs (IC50s = 0.073 and 0.923 μM for HDAC6 and HDAC10, respectively).1It is selective for these enzymes over BRD2, -3, and -T (IC50s = >20 μM for all), as well as over HDAC4, -5, -7, -9, and -11 (IC50s = >10 μM for all). CAY17c inhibits the proliferation of HCT116, SW620,...
T35810	C24 dihydro Ceramide (d18:0/24:0) Cer(d18:0/24:0)
	C24 dihydro Ceramide is a sphingolipid that has been found in the stratum corneum of human skin.[1] It is found in higher concentrations in female sebum compared to male sebum.[2] C24 dihydro Ceramide levels positively correlate with cytotoxicity in CCRF-CEM, MOLT-4, COG-LL-317h, and COG-LL-332h T cell acute lymphoblastic leukemia (ALL) cell lines.[4] Levels of C24 dihydro ceramide are increased by 149.49-fold in dihydroceramide desaturase 1 (DEGS1) knockdown UM-SCC-22A human head and neck squam...
T35890	Pentosidine
	Advanced glycation end products (AGEs) are compounds formed by non-enzymatic chemical reactions following the bonding of sugars to proteins or lipids during diabetes, uremia, aging, rheumatic arthritis, and other conditions. A receptor for the AGEs (RAGE) binds certain members of this class to initiate cell signaling.[1][2] Pentosidine is a well-characterized natural AGE that is often used as a biomarker for the production of all AGEs. While pentosidine can be measured in urine, the majority of ...
T35829	CC-90005
	CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM. CC-90005 shows selectivity for PKC-θ over PKC-δ (IC50=4440 nM). CC-90005 can inhibit T cell activation by IL-2 expression[1]. CC-90005 shows the exquisite selectivity of CC-90005, with IC50s for all other family members of >3 μM[1].CC-90005 is a moderate inhibitor of both CYP2C9 (IC50=8 μM) and CYP2C19 (IC50=5.9 μM) in human liver microsomes[1].CC-90005 inhibits IL-2 expression in LRS...
T36947	Pyrithiamine (hydrobromide)
	Pyrithiamine is the pyridine analog of thiamine that prevents growth of organisms that require intact thiamine. [1] It inhibits the growth of bacterial and fungal species at a pyrithiamine:thiamine ratio of 10:1 in growth media and induces symptoms of thiamine deficiency in mice at a dietary ratio of 3:1. These effects are reversible with addition of sufficient thiamine in all species. Pyrithiamine inhibits the formation of cocarboxylase from thiamine in chicken blood in a dose-dependent manner....
T36887	8(E),10(E),12(Z)-Octadecatrienoic Acid
	8(E),10(E),12(Z)-Octadecatrienoic acid is a conjugated polyunsaturated fatty acid (PUFA) that has been found inC. officinalisseed oil and has anticancer activity.1,2,3It inhibits the growth of Caco-2 cells when used at concentrations ranging from 10 to 50 μM.28(E),10(E),12(Z)-Octadecatrienoic acid (10 μM) induces formation of thiobarbituric acid reactive substances (TBARS) and apoptosis in DLD-1 colorectal adenocarcinoma cells.3It also inhibits prostaglandin biosynthesis in sheep vesicular gland...
T37522	Teneligliptin
	Teneligliptin (MP-513) is a potent chemotype prolylthiazolidine-based DPP-4 inhibitor, which competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM. Teneligliptin (MP-513) inhibits all these DPP-4 enzymes in a concentration-dependent manner. The IC50s of Teneligliptin (MP-513) for rhDPP-4, human plasma, and rat plasma are 0.889, 1.75, and 1.35 nM, respectively. A study of enzyme inhibition kinetics is conducted for Teneligliptin (M...

化合物

Cat.No: T16133

Target: Gamma-secretase

Cat.No: T6603

Synonym: GW 506U78,Nelzarabine,奈拉滨,506U78

Target: Apoptosis, Nucleoside Antimetabolite/Analog, DNA/RNA Synthesis

Pheniramine maleate

Cat.No: T0370

Synonym: Daneral,Inhiston,Trimetose,马来酸非尼拉敏

Target: 5-HT Receptor, Histamine Receptor

Cat.No: T72984

Target: Others

Cat.No: T3448

Target: Others

Cat.No: T36944

Target: Nucleoside Antimetabolite/Analog

Cat.No: T79377

Cat.No: T39799

Synonym: S2157

Cat.No: T39800

Cat.No: T83930

Cat.No: T60966

Cat.No: T36693

Cat.No: T37553

1-Heptadecanoyl-rac-glycerol

Cat.No: T37887

Cat.No: T37536

Cat.No: T37330

Cat.No: T38381

C24 dihydro Ceramide (d18:0/24:0)

Cat.No: T35810

Synonym: Cer(d18:0/24:0)

Cat.No: T35890

Cat.No: T35829

Pyrithiamine (hydrobromide)

Cat.No: T36947

8(E),10(E),12(Z)-Octadecatrienoic Acid

Cat.No: T36887

Cat.No: T37522

Cat. No.	Product Name	Target	Signaling Pathways
T36329	Terpendole I
	Terpendole I is a fungal metabolite that has been found in A. yamanashiensis.1 It is a weak inhibitor of acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 145 μM) and is active against the bacteria B. cereus and B. subtilis (MICs = 100 μg/ml for both) but not S. aureus, P. aeruginosa, or K. pneumoniae (MICs = >200 μg/ml for all) or the fungus C. albicans (MIC = 200 μg/ml).1,2 It is cytotoxic to HeLa cells with an IC50 value of 52.6 μM.3 \|1. Tomoda, H., Tabata, N., Yang, D.-J., et al. Ter...

天然产物

Cat.No: T36329

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