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13

抑制剂 & 化合物

3

天然产物

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Cat. No. Product Name Target Signaling Pathways
T6357 (S)-crizotinib

ent-crizotinib

Apoptosis; DNA/RNA Synthesis; MTH1 Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair
(S)-crizotinib (ent-crizotinib) 是一种选择性MTH1(mutT 同源物)抑制剂,IC50为 330 nM。它通过抑制 MTH1 破坏核苷酸库的稳态,诱导 DNA 单链断裂的增加,激活人结肠癌细胞的 DNA 修复,在动物模型中抑制肿瘤生长。
T0369 Ethaverine hydrochloride

Consenil,Ethaquin,Papetherine,盐酸依沙维林

MAO Metabolism; Neuroscience
Ethaverine hydrochloride (Ethaquin) 是罂粟碱的同系物。
T1366 3-Pyridylacetic acid hydrochloride

DPP-4 Proteases/Proteasome
3-Pyridylacetic acid hydrochloride (3-PAA-HCl)尼克酸的高同系物,是尼古丁(和其它烟草生物碱)的分解产物,还可与胺、醇和羧酸等反应,也可在反应中作为酸催化剂。
T67929 Linoleoyl glycine

Linoleoyl glycine 是一种经过修饰的多不饱和脂肪酸,是一种内源性的亚油酰乙醇酰胺同源物。Linoleoyl glycine 可以从哺乳动物皮肤、脊髓和大脑中提取 对爪蟾卵母细胞表达的人 KCNQ1/KCNE1 (hKCNQ1/hKCNE1) 通道有激活作用,在动物实验中显示出镇痛活性。
T70163 Bizine dihydrochloride

Bizine dihydrochloride is a potent LSD1 inhibitor in vitro, being selective versus monoamine oxidases A/B and the LSD1 homologue, LSD2.
T38685 C12-Sphingosine

C12-Sphingosine

C12-Sphingosine is a short-chain homologue of Sphingosine. It effectively inhibits the activity of serine palmitoyltransferase in primary cultured cerebellar cells.
T69376 Viriditoxin

Viriditoxin is a secondary metabolite isolated from Aspergillus viridinutans that has been shown to inhibit FtsZ, the bacterial homologue of eukaryotic tubulin.
T19188 ALLO-1

Autophagy Autophagy
ALLO-1 is a crucial autophagy receptor responsible for facilitating the formation of autophagosomes around paternal organelles. It directly interacts with the worm LC3 homologue, LGG-1, through its LC3-interacting region (LIR) motif.
T81743 mTORC1-IN-1

mTOR PI3K/Akt/mTOR signaling
mTORC1-IN-1(compound T1)为一种rapalog及选择性mTORC1抑制剂,调节细胞生长和代谢,与多种疾病如癌症相关。该化合物通过与FKBP12-FRB复合物结合(对接分数−11.6 kcal/mol)来靶向mTORC1。
T82613 Danburstotug

STI-3031,IMC-001

PD-1/PD-L1 Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation
Danburstotug (IMC-001) 是一种对CD274(程序性细胞死亡 1 配体1、PDL1、B7 同源物 1、B7-H1)具有亲和力的IgG1-lambda人源化单克隆抗体。该抗体不仅能够促进免疫应答,还显示出对抗肿瘤的潜力。
T36649 AN3661

AN3661, a potent antimalarial lead compound, targets a Plasmodium falciparum cleavage and polyadenylation specificity factor homologue subunit 3 (PfCPSF3). AN3661 inhibits Plasmodium falciparum laboratory-adapted strains, Ugandan field isolates, and murine P. berghei and P. falciparum infections[1]. AN3661 is active at nanomolar (IC50=20-56 nM) concentrations against P. falciparum laboratory strains known to be sensitive (3D7) or resistant (W2, Dd2, K1, HB3, FCR3 and TM90C2B), and AN3661 is simi...
T79730 LB244

STING Immunology/Inflammation
LB244为BB-Cl-amidine的同系物,为口服有效的STING抑制剂(EC50=0.8 μM),适用于治疗STING依赖性炎症性疾病。药代动力学研究表明,LB244在小鼠中的口服活性受限。
T36798L SW2_110A acetate

Histone Methyltransferase Chromatin/Epigenetic
SW2_110A acetate 是一种选择性的,细胞渗透性的chromobox 同源蛋白CBX8抑制剂(Kd = 800 nM),结合CBX8 N 端色域(ChD)。SW2_110A acetate 对CBX8 N 有很高的亲和力,抑制CBX8与细胞染色质的关联,抑制MLL-AF9诱导的THP1白血病细胞增殖。

化合物

(S)-crizotinib
Cat.No: T6357
Synonym: ent-crizotinib
Target: Apoptosis, DNA/RNA Synthesis, MTH1
Ethaverine hydrochloride
Cat.No: T0369
Synonym: Consenil,Ethaquin,Papetherine,盐酸依沙维林
Target: MAO
3-Pyridylacetic acid hydrochloride
Cat.No: T1366
Synonym:
Target: DPP-4
Linoleoyl glycine
Cat.No: T67929
Synonym:
Target:
Bizine dihydrochloride
Cat.No: T70163
Synonym:
Target:
C12-Sphingosine
Cat.No: T38685
Synonym: C12-Sphingosine
Target:
Viriditoxin
Cat.No: T69376
Synonym:
Target:
ALLO-1
Cat.No: T19188
Synonym:
Target: Autophagy
mTORC1-IN-1
Cat.No: T81743
Synonym:
Target: mTOR
Danburstotug
Cat.No: T82613
Synonym: STI-3031,IMC-001
Target: PD-1/PD-L1
AN3661
Cat.No: T36649
Synonym:
Target:
LB244
Cat.No: T79730
Synonym:
Target: STING
SW2_110A acetate
Cat.No: T36798L
Synonym:
Target: Histone Methyltransferase
Cat. No. Product Name Target Signaling Pathways
T8103 H-HoArg-OH

Endogenous Metabolite; Phosphorylase Metabolism
H-HoArg-OH 是人骨和肝脏碱性磷酸酶(alkaline phosphatase)的强效抑制剂,是一种精氨酸的同系物。
T8100 Azetidine-2-carboxylic acid

Others Others
Azetidine-2-carboxylic acid 是脯氨酸的非蛋白原氨基酸同系物,可以在常见的甜菜中获得。 在许多物种中,它能够错误地掺入蛋白质中代替脯氨酸,是一种致毒和致畸剂。
T83531 (Rac)-Juvenile hormone III

(Rac)-Juvenile hormone III,一种自法脂酸分离的天然产物,作为幼体激素的同源物具有最广泛分布。

天然产物

H-HoArg-OH
Cat.No: T8103
Synonym:
Target: Endogenous Metabolite, Phosphorylase
Azetidine-2-carboxylic acid
Cat.No: T8100
Synonym:
Target: Others
(Rac)-Juvenile hormone III
Cat.No: T83531
Synonym:
Target:
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