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26

抑制剂 & 化合物

2

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Cat. No. Product Name Target Signaling Pathways
T4235 Roblitinib

FGF-401

FGFR Angiogenesis; Tyrosine Kinase/Adaptors
Roblitinib (FGF-401) 是一种口服有效的,高选择性的FGFR4抑制剂(IC50:1.9 nM),具有抗癌作用。
T6759 AP-III-a4

ENOblock

Glucokinase Metabolism
AP-III-a4 (ENOblock) 是第一个非底物类似物,可直接与烯醇酶结合,IC50=0.576 uM,可阻碍体内癌细胞转移。
T8645 PF-06446846

Others Others
PF-06446846 是口服有活性的 PCSK9抑制剂。它能够在密码子区域附近阻断 80S ribosome,选择性地直接抑制 PCSK9 的翻译。
T4264 Takinib

EDHS-206

Apoptosis; MAPK Apoptosis; MAPK
Takinib (EDHS-206) 是一种TAK1自磷酸化的抑制剂,也是恶性疟原虫蛋白激酶 9 抑制剂,在 ATP 结合口袋内非竞争性结合。它诱导 TNF-α 刺激的细胞凋亡,可研究类风湿关节炎和转移性乳腺癌。
T9518 Inarigivir ammonium

ORI-9020 ammonium,SB-9200 ammonium,Inarigivir铵

HBV Microbiology/Virology
Inarigivir ammonium (SB-9200 ammonium) 是一种二核苷酸抗病毒化合物,可显着降低表达乙型肝炎病毒的转基因小鼠的 HBV DNA。它是一种激活细胞内先天免疫的视黄酸诱导基因-I 激动剂。
T1900 LDN-212854

LDN212854,BMP Inhibitor III

ALK; TGF-beta/Smad Angiogenesis; Stem Cells; Tyrosine Kinase/Adaptors
LDN-212854 (BMP Inhibitor III) 是一种新型BMP 抑制剂,抑制 ALK2 的IC50=1.3 nM,比对ALK1,ALK3,ALK4和ALK5的抑制性高2,66,1641和7135倍。
T27835 Lin281632

Lin-28 1632,Lin-281632,Lin 281632,Lin28 1632,Lin 28 163

Lin281632 是 RNA 结合蛋白 Lin28 和溴结构域的抑制剂。 Lin281632 促进 mESC 分化。
T4686 Simeprevir

TMC435,西咪匹韦,TMC-435350,Olysio

HCV Protease; SARS-CoV Microbiology/Virology; Proteases/Proteasome
Simeprevir (TMC435) 是一种有效的 HCV NS3/4A 蛋白酶抑制剂,抑制 HCV 复制,EC50 为 7.8 nM。它也是 SARS-CoV-2 3CLpro 抑制剂。
T5863 Indinavir sulfate

L735524 sulfate,MK-639 sulfate,硫酸茚地那韦

SARS-CoV; HIV Protease Microbiology/Virology; Proteases/Proteasome
Indinavir sulfate (L735524 sulfate) 是一种 HIV 蛋白酶抑制剂。它抑制 HIV-1 蛋白酶,IC50 值为 0.41 nM,Ki 值为 0.24 nM。它也是SARS-CoV 3CLpro 抑制剂,IC50为 1.71 μM。
T9249 ITMN4077

Antiviral Immunology/Inflammation
ITMN4077 对感染人类 HuH7 细胞的丙型肝炎病毒具有抗病毒活性,评估为抑制 HCV 亚基因组复制子复制,EC50 为 2.131μM。
T83658 SQLE-IN-1

Antifungal Microbiology/Virology
SQLE-IN-1 是一种角鲨烯环氧化酶 (SQLE) 抑制剂,具有抗肿瘤活性,可抑制肝癌细胞系 Huh7 的增殖和迁移能力,抑制细胞胆固醇的生成,增加抑癌基因PTEN的表达,抑制PI3K和AKT的蛋白表达。
T27733 KKJ00626

KKJ-00626,KKJ 00626

KKJ00626, an inhibitor of HBV virus, inhibits HBV replication in transfected Huh7 cells.
T79332 Antiproliferative agent-32

Apoptosis Apoptosis
Antiproliferative agent-32(Compound 1c)通过抑制PI3K/Akt/mTOR信号通路实现磷酸化。该化合物有效抑制Huh7和SK-Hep-1细胞的增殖,并诱导细胞凋亡,同时引起线粒体损伤,显示其在肝细胞癌研究中的潜在应用价值。
T61946 IMP2-IN-1

IMP2-IN-1 (compound 4) 是有效的IMP2抑制剂,对 IMP2 RNA 的IC50为 81.3-127.5 μM。IMP2-IN-1 降低 SW480 细胞中 IMP2 水平。IMP2-IN-1 显著抑制分化和未分化 Huh7 细胞的活力。
T27750 KSJ0001

KSJ-0001,KSJ 0001

KSJ0001, a HBV virus inhibitor, inhibits HBV replication in transfected Huh7 cells.
T37039 Betulinic Aldehyde oxime

Betulinic aldehyde oxime is a pentacyclic triterpenoid and derivative of the cholesterol biosynthesis inhibitor betulin .1It is active againstE. aerogenes,E. coli,E. faecalis,P. aeruginosa,S. aureus, andC. albicans, as well asL. donovaniamastigotes, when used at a concentration of 50 μM.1,2Betulinic aldehyde oxime (50 μM) is cytotoxic to Huh7 hepatocellular carcinoma cells.2
T79271 FGFR4-IN-14

FGFR Angiogenesis; Tyrosine Kinase/Adaptors
FGFR4-IN-14(Compound 27i)是一种高效的FGFR4抑制剂,IC50值仅为2.4 nM。该化合物能够抑制包含V550L和N535K突变的细胞增殖,且在huh7、BaF3/ETV6-FGFR4-V550L和BaF3/ETV6-FGFR4-N535K细胞系中的IC50分别达到21 nM、2.5 nM和171 nM。在Huh7异种移植模型中,FGFR4-IN-14展现出了明显的抗肿瘤效果,适用于肝细胞癌(HCC)的相关研究。
T36668 Geranylgeranoic Acid

Geranylgeranoic acid (GGA) is an isoprenoid that has been found inS. chinensisand has anticancer activity.1It induces apoptosis in Huh7 and PLC/PRF/5 human hepatoma cells and MLE-10 transformed mouse hepatocytes, but not primary mouse hepatocytes, when used at concentrations ranging from 1 to 20 μM. GGA (10 μM) induces apoptosis in Huh7 cellsvialoss of the mitochondrial membrane potential and activation of interleukin-1β-converting enzyme (ICE) and cysteine protease precursor 32 (CPP32).2It also...
T61045 Topoisomerase I/II inhibitor 2

Topoisomerase I/II inhibitor 2 (compound 1a) 可显著抑制小鼠模型中的异种移植肿瘤的生长,可用于肝癌治疗。Topoisomerase I/II inhibitor 2 是一种DNA 拓扑异构酶 I/II 的双重抑制剂。Topoisomerase I/II inhibitor 2 是有效的拓扑异构酶抑制剂,对LM9 细胞和Huh7 细胞的 IC50值分别为 6.83 μM 和9.82 μM 。
T38238 2'-Deoxy-2'-fluorocytidine

Nucleoside Antimetabolite/Analog; Influenza Virus Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology
2'-Deoxy-2'-fluorocytidine 是一种核苷类似物,可有效抑制刚果出血热病毒的复制。2'-Deoxy-2'-fluorocytidine 与 T705 的协同作用会增强对CCHFV 复制的抵抗效力。
T83714 LAP TFA

Lupus Autoantigen Peptide,La Peptide

Lupus autoantigen peptide (LAP) 是源自La的一种抗病毒肽,La是系统性红斑狼疮 (SLE) 患者中发现的一种自身抗原,对应于La的11-28氨基酸。它抑制了丙型肝炎病毒 (HCV) 5’-UTR与内部核糖体进入位点 (IRES) 跨作用因子 (ITAFs),包括多嘧啶片段结合蛋白 (PTB) 和多聚(rC)-结合蛋白2 (PCBP2) 之间的相互作用。LAP (60 µM) 在使用Huh7细胞的报告者测定中抑制了HCV IRES介导的翻译,这一效应可以通过重组的PTB和PCBP2来逆转。
T82189 HMGB1-IN-2

HMGB1-IN-2 (compound 15) 是一种针对高度保守的核蛋白 HMGB1 的抑制剂,其在 RAW264.7 细胞中展现出 NO 抑制活性,IC50 为 20.2 μM。 HMGB1-IN-2 (30 μM) 能够减少 IL-1β、TNF-α、caspase-1 p20 的表达,并抑制 NF-κB p65 的磷酸化作用,显示出抗凋亡特性。在脓毒症急性肾损伤模型的小鼠中,HMGB1-IN-2(15 mg/kg;腹腔注射)可有效减轻肾脏伤害。此外,HMGB1-IN-2 对 Huh7 细胞和 A549 细胞的 IC50 分别为 77.0 μM 和 82.0 μM。
T35547 YW1128

YW1128 is an inhibitor of Wnt/β-catenin signaling with an IC50 value of 4.1 nM in a reporter assay.1 It decreases protein levels of β-catenin in the presence of the GSK3β inhibitor lithium chloride and increases protein levels of Axin1 in HEK293 cells. YW1128 decreases lipid accumulation and the expression of gluconeogenic and lipogenic genes in Huh7 cells. It decreases the hepatic expression of Wnt target genes, improves glucose tolerance, and prevents body weight increases and hepatic lipid ac...
T15675 Tirbanibulin Mesylate

KX2-391 Mesylate,KX01 Mesylate

Microtubule Associated; Src Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors
Tirbanibulin Mesylate (KX01 Mesylate) 是一种 Src 抑制剂,靶向 Src 的肽底物位点。在肿瘤细胞中,GI50值为 9-60 nM。
T36848 Combretastatin A-1

Combretastatin A1

Akt; Microtubule Associated Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
Combretastatin A-1 是一种有效的微管抑制剂,具有抗肿瘤和抗血管活性,通过微管蛋白解聚介导的 AKT 失活抑制 Wnt/β-catenin 通路发挥作用,可用于研究肝癌。
T38269 Purfalcamine

Purfalcamine is an orally active, selective Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) inhibitor with an IC50 of 17 nM and an EC50 of 230 nM. Purfalcamine has antimalarial activity and causes malaria parasites developmental arrest at the schizont stage[1][2]. Purfalcamine has low activity against Toxoplasma gondii calcium-dependent protein kinase 3 (TgCDPK3)[1]. Purfalcamine (225, 450 nM) has no effect on the parasitemia in the first 32 hours. After about 40 hours, paras...

化合物

Roblitinib
Cat.No: T4235
Synonym: FGF-401
Target: FGFR
AP-III-a4
Cat.No: T6759
Synonym: ENOblock
Target: Glucokinase
PF-06446846
Cat.No: T8645
Synonym:
Target: Others
Takinib
Cat.No: T4264
Synonym: EDHS-206
Target: Apoptosis, MAPK
Inarigivir ammonium
Cat.No: T9518
Synonym: ORI-9020 ammonium,SB-9200 ammonium,Inarigivir铵
Target: HBV
LDN-212854
Cat.No: T1900
Synonym: LDN212854,BMP Inhibitor III
Target: ALK, TGF-beta/Smad
Lin281632
Cat.No: T27835
Synonym: Lin-28 1632,Lin-281632,Lin 281632,Lin28 1632,Lin 28 163
Target:
Simeprevir
Cat.No: T4686
Synonym: TMC435,西咪匹韦,TMC-435350,Olysio
Target: HCV Protease, SARS-CoV
Indinavir sulfate
Cat.No: T5863
Synonym: L735524 sulfate,MK-639 sulfate,硫酸茚地那韦
Target: SARS-CoV, HIV Protease
ITMN4077
Cat.No: T9249
Synonym:
Target: Antiviral
SQLE-IN-1
Cat.No: T83658
Synonym:
Target: Antifungal
KKJ00626
Cat.No: T27733
Synonym: KKJ-00626,KKJ 00626
Target:
Antiproliferative agent-32
Cat.No: T79332
Synonym:
Target: Apoptosis
IMP2-IN-1
Cat.No: T61946
Synonym:
Target:
KSJ0001
Cat.No: T27750
Synonym: KSJ-0001,KSJ 0001
Target:
Betulinic Aldehyde oxime
Cat.No: T37039
Synonym:
Target:
FGFR4-IN-14
Cat.No: T79271
Synonym:
Target: FGFR
Geranylgeranoic Acid
Cat.No: T36668
Synonym:
Target:
Topoisomerase I/II inhibitor 2
Cat.No: T61045
Synonym:
Target:
2'-Deoxy-2'-fluorocytidine
Cat.No: T38238
Synonym:
Target: Nucleoside Antimetabolite/Analog, Influenza Virus
LAP TFA
Cat.No: T83714
Synonym: Lupus Autoantigen Peptide,La Peptide
Target:
HMGB1-IN-2
Cat.No: T82189
Synonym:
Target:
YW1128
Cat.No: T35547
Synonym:
Target:
Tirbanibulin Mesylate
Cat.No: T15675
Synonym: KX2-391 Mesylate,KX01 Mesylate
Target: Microtubule Associated, Src
Combretastatin A-1
Cat.No: T36848
Synonym: Combretastatin A1
Target: Akt, Microtubule Associated
Purfalcamine
Cat.No: T38269
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T0687 Simvastatin

辛伐他汀,MK-0733,MK 733

Apoptosis; Mitophagy; Ferroptosis; HMG-CoA Reductase; Autophagy Apoptosis; Autophagy; Metabolism
Simvastatin (MK 733) 是一种 HMG-CoA 还原酶抑制剂 (Ki=0.2 nM),具有口服活性。Simvastatin 具有降血脂活性,可以抑制肝脏产生胆固醇,还可以用于预防心血管疾病。
T37452 Stephacidin B

Stephacidin B is a fungal metabolite that has been found inA. ochraceus.1Dimeric stephacidin B is rapidly converted to a monomer, avrainvillamide ,in vitro.2Stephacidin B is cytotoxic to a variety of cancer cells, including testosterone-independent PC3 and -sensitive LNCaP prostate cancer cells (IC50s = 0.37 and 0.06 μM, respectively) and estradiol-independent SK-BR-3 and -sensitive MCF-7 breast cancer cells (IC50s = 0.32 and 0.27 μM, respectively).1It induces apoptosis in HepG2 and Huh7 hepatoc...

天然产物

Simvastatin
Cat.No: T0687
Synonym: 辛伐他汀,MK-0733,MK 733
Target: Apoptosis, Mitophagy, Ferroptosis, HMG-CoA Reductase, Autophagy
Stephacidin B
Cat.No: T37452
Synonym:
Target:
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