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32

抑制剂 & 化合物

2

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Cat. No. Product Name Target Signaling Pathways
T7008 Vacquinol-1

Vacquinol 1

JNK MAPK
Vacquinol-1 能够激活 MAPK 通路,是MKK4特异性激活剂。它可以诱导肝细胞癌细胞凋亡,在多形性胶质母细胞瘤小鼠模型中特异性诱导人胶质母细胞瘤细胞死亡、减缓肿瘤进展并延长生存期。
T1785 Palbociclib

PD 0332991,帕博西尼,帕布昔利布

CDK Cell Cycle/Checkpoint
Palbociclib (PD 0332991) 是一种 CDK 抑制剂,抑制 CDK4 和 CDK6 (IC50=11/16 nM),具有口服活性。Palbociclib 具有抗肿瘤活性,有用于 ER 阳性和 HER2 阴性乳腺癌的研究潜力。
T0334 Rosiglitazone

BRL49653,罗格列酮

Ferroptosis; TRP/TRPV Channel; PPAR; Autophagy Apoptosis; Autophagy; DNA Damage/DNA Repair; Membrane transporter/Ion channel; Metabolism
Rosiglitazone (BRL49653) 是一种 PPARγ 激动剂、TRPC5 激活剂和 TRPM3 抑制剂,具有口服活性。Rosiglitazone 也是一种降糖剂,是噻唑烷二酮类胰岛素增敏剂。
T6481 Droxinostat

NS 41080,4-(4-氯-2-甲基苯氧基)-N-羟基丁酰胺

Apoptosis; HDAC Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair
Droxinostat (NS 41080) 是HDAC3、HDAC6和HDAC8抑制剂,IC50分别为16.9、2.47和1.46 μM。
T22443 Triglycidyl isocyanurate

Tris(2,3-epoxypropyl) Isocyanurate,Teroxirone,TGIC,1,3,5-三缩水甘油-S-三嗪三酮,TGI

Apoptosis Apoptosis
Triglycidyl isocyanurate (Teroxirone) 是一种三氮烯三环氧化合物,可通过 p53的激活抑制非小细胞肺癌细胞的生长。它诱导细胞凋亡,具有抗血管生成和抗肿瘤活性,用于癌症研究。
T9945 MNK8 

3-methyl-6-(naphthalen-1-yl)pyrimidine-2,4(1H,3H)-dione

STAT JAK/STAT signaling; Stem Cells
MNK8 (3-methyl-6-(naphthalen-1-yl)pyrimidine-2,4(1H,3H)-dione) 是一种有效的STAT3抑制剂,降低STAT3与DNA 结合的能力,对肝癌细胞也有良好的生长抑制作用。
T6646 Rosiglitazone hydrochloride

盐酸罗格列酮,BRL-49653 HCl,Rosiglitazone HCl

Ferroptosis; TRP/TRPV Channel; PPAR; Autophagy Apoptosis; Autophagy; DNA Damage/DNA Repair; Membrane transporter/Ion channel; Metabolism
Rosiglitazone hydrochloride (BRL-49653 HCl) 是一种降血糖药物,通过与脂肪细胞中的 PPAR 受体结合来刺激胰岛素分泌。它对 PPARγ1、PPARγ2 和 PPARγ 的EC50值分别为 30 nM、100 nM 和 60 nM。它也是TRPC5的激活剂和TRPM3的抑制剂。
T6239 Palbociclib monohydrochloride

PD 0332991 hydrochloride,Palbociclib hydrochloride,帕布昔利布盐酸盐,Palbociclib (PD-0332991) HCl

CDK Cell Cycle/Checkpoint
Palbociclib monohydrochloride (PD 0332991 hydrochloride) 是一种口服的细胞周期蛋白依赖性激酶 (CDK) 抑制剂,具有潜在的抗肿瘤活性。它抑制 CDK4和 CDK6,IC50分别为11 nM,16 nM。它有用于 ER 阳性和 HER2 阴性乳腺癌的研究潜力。
T6240 Palbociclib Isethionate

Palbociclib (PD0332991) Isethionate,帕博西尼羟乙基磺酸盐,PD 0332991 isethionate,帕布昔利布羟乙基磺酸盐

CDK Cell Cycle/Checkpoint
Palbociclib Isethionate (PD 0332991 isethionate) 是一种高选择性的CDK4/6抑制剂,IC50为11 nM 和16 nM。它对一组 36 种额外的蛋白激酶没有抑制作用。
T77440 Codrituzumab

RG-7686,RO5137382,GC33

Codrituzumab (GC3)是一种人源化针对 glypican-3 肝癌蛋白的抗体,可与索拉非尼联合使用来研究不可治愈的晚期肝细胞癌 (HCC) 。
T4368 Miriplatin

米铂,SM-11355

DNA Alkylator/Crosslinker DNA Damage/DNA Repair
Miriplatin (SM-11355) 是一种烷化剂,是一种用于 TACE 的铂络合物,有望用于治疗肝细胞癌。
T64529 MDL-800

MDL 800,MDL800

Sirtuin Chromatin/Epigenetic; DNA Damage/DNA Repair
SIRT6, responsible for deacetylation of histone H3 Nε-acetyl-lysines 9 (H3K9ac) and 56 (H3K56ac), is a tumor suppressor which has frequently been found to have low expression in various cancers. MDL-800 is a selective SIRT6 activator. It increased the deacetylase activity of SIRT6 by up to 22-fold and led to a global decrease in H3K9ac and H3K56ac levels in human hepatocellular carcinoma (HCC) cells. Also, it inhibited the proliferation of HCC cells via SIRT6-driven cell-cycle arrest and was eff...
TP1472 Tyroserleutide

Others Others
Tyroserleutide 是一种可从猪脾脏的降解产物中分离得到的小分子三肽,在体内外均对肿瘤生长具有抑制作用。
T76858 Ascrinvacumab

PF-03446962

ALK; TGF-beta/Smad Angiogenesis; Stem Cells; Tyrosine Kinase/Adaptors
Ascrinvacumab (PF-03446962) 是一种针对 ALK-1 的高效人源化 IgG2 单克隆抗体。Ascrinvacumab 对人 ALK1 的 Kd 值为 7 nM。Ascrinvacumab 对 TGF-β 有抑制作用,可用于研究肝细胞癌 (HCC)。
T21297 Miriplatin hydrate

SM-11355 (hydrate),Miripla,Miriplatin,SM 11355,SM11355,SM-11355,Miriplatin hydrate

DNA Alkylation DNA Damage/DNA Repair
Miriplatin hydrate (SM-11355 (hydrate)) (MPT)是一种用于TACE 的新型铂类化合物,在肝细胞癌(HCC)的治疗中显示出良好的前景。米铂是一种亲脂性铂复合物,容易悬浮在碘油中,并在肿瘤组织中逐渐释放活性铂化合物。
T3226 Paritaprevir

ABT-450,Veruprevir,帕利瑞韦

HCV Protease Microbiology/Virology; Proteases/Proteasome
Paritaprevir (ABT-450) 是一种口服生物可利用的合成酰基磺酰胺抑制剂,可抑制丙型肝炎病毒 (HCV) 蛋白酶复合物,由非结构蛋白 3 和 4A (NS3/NS4A) 组成,对 HCV 基因型 1 具有潜在活性。 给药后,paritaprevir 可逆地结合 HCV NS3/NS4A 蛋白酶的活性中心和结合位点,并阻止 NS3/NS4A 蛋白酶介导的多蛋白成熟。这会破坏病毒蛋白的加工和病毒复制复合物的形成,从而抑制病毒在 HCV 基因型 1 感染的宿主细胞中的复制。 NS3 是一种丝氨酸蛋白酶,对于 HCV 多蛋白内多个位点的蛋白水解切割至关重要,并且在 HCV 核糖核酸 (RNA) 复制过程中起关键作用。 NS4A 是 NS3 的激活因子。 HCV 是属于黄病毒科的一种小的、有包膜的单链 RNA 病毒,感染与肝细胞癌 (HCC) 的发展有关。
T62151 CHNQD-01255

CHNQD-01255 是一种口服具有活力的 Arf-GEFs 抑制剂,能够有效地抵抗肝细胞癌 (HCC)。
T38977 Autophagy-IN-C1

Autophagy-IN-C1

Autophagy-IN-C1是一种含有尿素的金鸡纳生物碱衍生物。Autophagy-IN-C1 不仅诱导肝细胞癌(HCC)细胞凋亡,而且阻断自噬。
T60277 2-Acetamidofluorene

2-Acetamidofluorene 是一种强致癌物。2-Acetamidofluorene 可用于诱导肝细胞癌 (HCC) 和多原发肿瘤。
T74768 Antitumor agent-92

Apoptosis Apoptosis
Antitumor agent-92为一种淫羊藿素衍生物,能够引起细胞周期在G0/G1期的停滞,并诱导细胞凋亡。该化合物展现出在肝细胞癌(HCC)研究中的应用潜力。
T62704 HBV-IN-23

HBV-IN-23 (Compound 5k) 是一种 HBV DNA 复制抑制剂 (IC50: 0.58 μM)。HBV-IN-23 能够抑制药物敏感和耐药株。HBV-IN-23 可以诱导 HepG2 细胞凋亡,表现出抗肝癌细胞 (HCC) 效果。
T62676 DS89002333

DS89002333 是一种强效的、口服具有活力的 PRKACA 抑制剂 (IC50: 0.3 nM)。DS89002333 在表达 DNAJB1-PRKACA 融合基因的 FL-HCC 患者源性异种移植模型中具有良好的抗肿瘤作用。DS89002333 能够用于研究纤维化肝细胞癌 (FL-HCC)。
T68875 Xylocydine

Xylocydine is a novel Cdk inhibitor, which is an effective inducer of apoptosis in hepatocellular carcinoma cells in vitro and in vivo. Xylocydine also strongly inhibits the activity of Cdk7 and Cdk9, in vitro as well as in cell cultures, that is temporally associated with apoptotic cell death in xylocydine-induced HCC cells. Xylocydine can effectively suppress the growth of HCC xenografts in Balb/C-nude mice by preferentially inducing apoptosis in the xenografts, whereas the drug did not cause...
T78819 VEGFR-2-IN-33

VEGFR Angiogenesis; Tyrosine Kinase/Adaptors
VEGFR-2-IN-33(Compound 4d)为一种有效的VEGFR抑制剂,其IC50值为61.04 nM。该化合物在抑制HepG2细胞增殖方面表现出更高的效力,IC50仅为4.31 nM,因此常用于肝细胞癌(HCC)研究领域。
T79407 HL23

Others Others
HL23是一种HDAC抑制剂,对抗HCC具有活性。通过增强TXNIP启动子乙酰化,此化合物上调TXNIP表达,进而介导钾通道活性并触发TXNIP依赖性钾剥夺,抑制HCC的进展和转移。HL23与Sorafenib联合应用时显示出协同作用,并且其效力超过Sorafenib与Vorinostat的联用。
T68942 Caricotamide

Caricotamide is a synthetic co-substrate that activates the human endogenous enzyme NRH:quinone oxidoreductase 2 (NQO2) with potential chemoadjuvant activity. When caricotamide is administered simultaneously with the prodrug tretazicar, NQO2 converts tretazicar to the bifunctional alkylating agent dinitrobenzamide, which is capable of forming a high degree of DNA interstrand cross-links, resulting in the inhibition of DNA replication and the induction of apoptosis. NQO2 has been found to be over...
T61961 Pyruvate Carboxylase-IN-2

Pyruvate Carboxylase-IN-2 是毛兰素的天然类似物。Pyruvate Carboxylase-IN-2 (compound 29) 是有效的丙酮酸羧化酶(pyruvate carboxylase) 抑制剂。在基于细胞裂解物和基于细胞的 PC 活性中,Pyruvate Carboxylase-IN-2的 IC50s 分别为 0.065 和 0.097 μM。Pyruvate Carboxylase-IN-2介导人肝细胞癌 (HCC) 的抗癌作用。
T60341 Pyruvate Carboxylase-IN-1

Pyruvate Carboxylase-IN-1 (compound 37) 是一种有效的丙酮酸羧化酶(PC) 抑制剂,对于基于细胞裂解物和基于细胞的 PC 活性,IC50s 分别为 0.204 和 0.104 μM。Pyruvate Carboxylase-IN-1 是毛兰素的天然类似物。Pyruvate Carboxylase-IN-1 抑制 PC 的酶活性,介导人肝细胞癌 (HCC) 的抗癌作用。
T69395 Nicotinamide-d4

Nicotinamide-d4 is intended for use as an internal standard for the quantification of nicotinamide by GC- or LC-MS. Nicotinamide is an amide form of niacin, which is also known as vitamin B3, that can be biosynthesized in vivo or obtained through the diet. It is a precursor in the synthesis of the metabolic cofactor NAD+ and an inhibitor of sirtuin 1 (SIRT1; IC50 = <50 µM). Nicotinamide (10 µM) increases the activity of serine palmitoyltransferase (SPT) and the biosynthesis of ceramide, glucosyl...
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。
T35573 Adenosine 5’-methylenediphosphate (hydrate)

Adenosine 5’-methylenediphosphate is an inhibitor of ecto-5’-nucleotidase, also known as CD73, with a Kivalue of 37 nM.1It inhibits cAMP accumulation induced by adenosine 5’-monophosphate , adenosine 5’-diphosphate , or adenosine 5’-triphosphate but not adenosine in VA-13 human fibroblasts when used at a concentration of 100 μM. Adenosine 5’-methylenediphosphate reduces proliferation of U138MG glioma cells, as well as inhibits the invasion and migration of MHCC97H hepatocellular carcinoma (HCC) ...
T75134 MC-GGFG-AM-(10Me-11F-Camptothecin)

MC-GGFG-AM-(10Me-11F-Camptothecin) 是ZW251合成的Linker-Payload偶联物。ZW251是靶向人GPC3的抗体-活性分子偶联物(ADC),包括人源化IgG1抗体、喜树碱(camptothecin)类的扑异构酶1抑制剂ZD06519及连接子(马来酰亚胺锚定和甘酰甘酰苯丙酰甘氨酸(GGFG)-氨基甲基(AM)可切割连接体)。该药物对人和食蟹猴GPC3具高亲和力,在表达GPC3的HCC细胞系中快速内化并可对GPC3阴性癌细胞进行旁观者介导杀伤。

化合物

Vacquinol-1
Cat.No: T7008
Synonym: Vacquinol 1
Target: JNK
Palbociclib
Cat.No: T1785
Synonym: PD 0332991,帕博西尼,帕布昔利布
Target: CDK
Rosiglitazone
Cat.No: T0334
Synonym: BRL49653,罗格列酮
Target: Ferroptosis, TRP/TRPV Channel, PPAR, Autophagy
Droxinostat
Cat.No: T6481
Synonym: NS 41080,4-(4-氯-2-甲基苯氧基)-N-羟基丁酰胺
Target: Apoptosis, HDAC
Triglycidyl isocyanurate
Cat.No: T22443
Synonym: Tris(2,3-epoxypropyl) Isocyanurate,Teroxirone,TGIC,1,3,5-三缩水甘油-S-三嗪三酮,TGI
Target: Apoptosis
MNK8 
Cat.No: T9945
Synonym: 3-methyl-6-(naphthalen-1-yl)pyrimidine-2,4(1H,3H)-dione
Target: STAT
Rosiglitazone hydrochloride
Cat.No: T6646
Synonym: 盐酸罗格列酮,BRL-49653 HCl,Rosiglitazone HCl
Target: Ferroptosis, TRP/TRPV Channel, PPAR, Autophagy
Palbociclib monohydrochloride
Cat.No: T6239
Synonym: PD 0332991 hydrochloride,Palbociclib hydrochloride,帕布昔利布盐酸盐,Palbociclib (PD-0332991) HCl
Target: CDK
Palbociclib Isethionate
Cat.No: T6240
Synonym: Palbociclib (PD0332991) Isethionate,帕博西尼羟乙基磺酸盐,PD 0332991 isethionate,帕布昔利布羟乙基磺酸盐
Target: CDK
Codrituzumab
Cat.No: T77440
Synonym: RG-7686,RO5137382,GC33
Target:
Miriplatin
Cat.No: T4368
Synonym: 米铂,SM-11355
Target: DNA Alkylator/Crosslinker
MDL-800
Cat.No: T64529
Synonym: MDL 800,MDL800
Target: Sirtuin
Tyroserleutide
Cat.No: TP1472
Synonym:
Target: Others
Ascrinvacumab
Cat.No: T76858
Synonym: PF-03446962
Target: ALK, TGF-beta/Smad
Miriplatin hydrate
Cat.No: T21297
Synonym: SM-11355 (hydrate),Miripla,Miriplatin,SM 11355,SM11355,SM-11355,Miriplatin hydrate
Target: DNA Alkylation
Paritaprevir
Cat.No: T3226
Synonym: ABT-450,Veruprevir,帕利瑞韦
Target: HCV Protease
CHNQD-01255
Cat.No: T62151
Synonym:
Target:
Autophagy-IN-C1
Cat.No: T38977
Synonym: Autophagy-IN-C1
Target:
2-Acetamidofluorene
Cat.No: T60277
Synonym:
Target:
Antitumor agent-92
Cat.No: T74768
Synonym:
Target: Apoptosis
HBV-IN-23
Cat.No: T62704
Synonym:
Target:
DS89002333
Cat.No: T62676
Synonym:
Target:
Xylocydine
Cat.No: T68875
Synonym:
Target:
VEGFR-2-IN-33
Cat.No: T78819
Synonym:
Target: VEGFR
HL23
Cat.No: T79407
Synonym:
Target: Others
Caricotamide
Cat.No: T68942
Synonym:
Target:
Pyruvate Carboxylase-IN-2
Cat.No: T61961
Synonym:
Target:
Pyruvate Carboxylase-IN-1
Cat.No: T60341
Synonym:
Target:
Nicotinamide-d4
Cat.No: T69395
Synonym:
Target:
FGFR4-IN-14
Cat.No: T79271
Synonym:
Target: FGFR
Adenosine 5’-methylenediphosphate (hydrate)
Cat.No: T35573
Synonym:
Target:
MC-GGFG-AM-(10Me-11F-Camptothecin)
Cat.No: T75134
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T6670 Silymarin

Silybin B,水飞蓟素

SARS-CoV Microbiology/Virology
Silymarin (Silybin B) 是一种多酚类黄酮,是从水飞蓟或水飞蓟的种子中提取的一种 SARS-CoV-2 主蛋白酶抑制剂。它可降低肿瘤细胞的增殖,血管生成以及胰岛素抵抗,用于预防和治疗肝脏疾病,有潜力研究 COVID-19 。
T2S0837 Astragalus Polysacharin

2-(Chloromethyl)-4-(4-nitrophenyl)thiazole,黄芪多糖,89250-26-0

TAM Receptor Tyrosine Kinase/Adaptors
2-(Chloromethyl)-4-(4-nitrophenyl)thiazole 是一种从黄芪 (Astragalus propinquus) 中提取得到的天然产物。2-(Chloromethyl)-4-(4-nitrophenyl)thiazole 具有抗癌活性,通过抑制肿瘤相关巨噬细胞 (TAM) 的 M2 极化在肝细胞癌 (HCC) 中显示除抗肿瘤活性。

天然产物

Silymarin
Cat.No: T6670
Synonym: Silybin B,水飞蓟素
Target: SARS-CoV
Astragalus Polysacharin
Cat.No: T2S0837
Synonym: 2-(Chloromethyl)-4-(4-nitrophenyl)thiazole,黄芪多糖,89250-26-0
Target: TAM Receptor
TargetMol Loading
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