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抑制剂 & 化合物

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Cat. No. Product Name Target Signaling Pathways
T2430 HPOB

Apoptosis; HDAC Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair
HPOB 是一种高选择性HDAC6抑制剂,IC50为 56 nM,其选择性是其他 HDAC 的 30 倍以上。它提高 DNA 损伤抗癌药物在转化细胞中的有效性。
T9891 PARP1-IN-8 

N-(3-chlorophenyl)-3-(1-oxo-4-phenylphthalazin-2(1H)-yl)propanamide

PARP Chromatin/Epigenetic; DNA Damage/DNA Repair
PARP1-IN-8 (N-(3-chlorophenyl)-3-(1-oxo-4-phenylphthalazin-2(1H)-yl)propanamide) 是PARP1的有效抑制剂(IC50 = 97 nM)。
T1083L Theophylline monohydrate

Quibron,茶碱一水合物

HDAC; PDE; Adenosine Receptor Chromatin/Epigenetic; DNA Damage/DNA Repair; GPCR/G Protein; Metabolism; Neuroscience
Theophylline monohydrate (Quibron) 似乎抑制磷酸二酯酶和前列腺素的产生,调节钙通量和细胞内钙分布,并拮抗腺苷。茶碱是黄嘌呤的天然生物碱衍生物,从植物山茶花和小粒咖啡中分离出来。在生理上,该药剂可放松支气管平滑肌,产生血管舒张(脑血管除外),刺激中枢神经系统,刺激心肌,利尿,增加胃酸分泌;它还可以抑制炎症并改善横膈膜的收缩性。
T12344L1 OTS186935 FA

OTS186935 FA(2093400-18-9 Free base)

Histone Methyltransferase Chromatin/Epigenetic
OTS186935 FA 是一种蛋白甲基转移酶 SUV39H2 抑制剂。OTS186935 FA在 MDA-MB-231 乳腺癌细胞和 A549 肺癌细胞中抑制肿瘤的生长。
T8979 AEM1

Nrf2 Immunology/Inflammation
AEM1 是 Nrf2抑制剂,能够降低 A549 细胞中 Nrf2 依赖基因的表达,并在体外和体内抑制 A549 细胞的生长。
T15451 GW-870086

Glucocorticoid Receptor Endocrinology/Hormones
GW-870086 是抗炎剂,是糖皮质激素受体激动剂,在 A549 细胞中,能够降低 NFκB 报告基因活性(pIC50: 10.1)。
T8967 SW155246

DNA Methyltransferase Chromatin/Epigenetic
SW155246 是选择性 DNA 甲基转移酶 (DNMT1) 抑制剂,能够抑制 hDNMT1 (IC50:1.2 μM) 以及 mDNMT3A (IC50:38 μM)。它能够促使 A549细胞中肿瘤抑制基因 RASSF1的重新表达,可用于研究癌症和其他疾病。
T62281 PARP-1-IN-2

PARP Chromatin/Epigenetic; DNA Damage/DNA Repair
PARP-1-IN-2 是一种有效且可透过血脑屏障的 PARP1 抑制剂(IC50: 149 nM)。PARP-1-IN-2 在细胞实验中对人肺腺癌上皮细胞系 A549 显示出显著的抗增殖活性。PARP-1-IN-2 可诱导 A549 细胞凋亡。
T7018 WZB117

transporter Metabolism
WZB117 是葡萄糖转运蛋白 1 抑制剂,可下调糖酵解,诱导细胞周期停滞,有抗癌细胞生长的作用。
T22396 PF-6274484

PF 6274484

EGFR Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
PF-6274484 是一种EGFR 抑制剂,对于 EGFR-L858R/T790M 和 WT-EGFR 的 Ki 值分别为 0.14 和 0.18 nM。它在 H1975 肿瘤细胞和 A549 肿瘤细胞中抑制EGFR-L858R/T790M 自身磷酸化和EGFR-WT,IC50分别为6.6和 5.8 nM。
T60654 KDM4C-IN-1

Histone Demethylase Chromatin/Epigenetic
KDM4C-IN-1 是一种具有选择性和高效性的KDM4C 抑制剂(IC50:8 nM),具有潜在的抗癌活性。KDM4C-IN-1 抑制 HepG2 和 A549 细胞的生长,可用于研究白血病。
T8816 NAE-IN-M22

NEDD8 inhibitor M22

Apoptosis; E1/E2/E3 Enzyme Apoptosis; Ubiquitination
NAE-IN-M22 (NEDD8 inhibitor M22) 是一种选择性可逆的 NEDD8 激活酶抑制剂。 它抑制多种癌细胞系并诱导 A549 细胞凋亡,还可以在体内抑制肿瘤生长。
T1887 Inauhzin

INZ

Sirtuin Chromatin/Epigenetic; DNA Damage/DNA Repair
Inauhzin (INZ) 是一种新型小分子,通过抑制 SIRT1 活性有效地重新激活 p53,促进人 Y 细胞的 p53 依赖性凋亡,在 A549 细胞中的IC50为3 uM。
T7082 HDAC8-IN-1

HDAC Chromatin/Epigenetic; DNA Damage/DNA Repair
HDAC8-IN-1 是一种 HDAC8 抑制剂,在癌细胞系中的 IC50 为 27.2 nM,有抗增殖作用。
T36316 mTOR inhibitor-8

mTOR-IN-8

mTOR; Autophagy Autophagy; PI3K/Akt/mTOR signaling
mTOR inhibitor-8 是一种有效的 mTOR 抑制剂和自噬诱导剂,具有抗病毒和抗肿瘤活性。mTOR inhibitor-8 抑制A549细胞的生长,可用于研究非小细胞肺癌。
T63343 ULK1-IN-2

Apoptosis; Autophagy Apoptosis; Autophagy
ULK1-IN-2 是一种有效的 ULK1 抑制剂,具有潜在的抗癌活性,可诱导细胞凋亡同时阻断自噬。ULK1-IN-2 对癌细胞具有较高的细胞毒作用,对 A549 细胞的 IC50 值为 1.94 μM。ULK1-IN-2 可用于研究非小细胞肺癌。
T36675 ERK Inhibitor

ERK inhibitor is a cell-permeable inhibitor that binds ERK2 near its docking domain (KD = 5 μM). This prevents its interaction with protein substrates without inhibiting catalytic activity. ERK inhibitor blocks ERK-specific phosphorylation of ribosomal S6 kinase-1 and ternary complex factor Elk-1 but does not affect ERK1/2 phosphorylation by MEK1/2. Presumably through its effects on ERK, ERK inhibitor completely prevents proliferation of HeLa cells (IC50 = 15-20 μM), A549 lung carcinoma cells (I...
T9105 NF-κB-IN-1

1,6-Heptadiene-3,5-dione, 1,7-bis(3,4-dimethoxyphenyl)-4-[(4-hydroxy-3-methoxyphenyl)methylene]-, (1E,6E)-

IκB/IKK; NF-κB NF-κB
NF-κB-IN-1 (1,6-Heptadiene-3,5-dione, 1,7-bis(3,4-dimethoxyphenyl)-4-[(4-hydroxy-3-methoxyphenyl)methylene]-, (1E,6E)-)是一种 4-亚芳基姜黄素类似物,是抑制有效的NF-κB 信号通路抑制剂。它可有效抑制肺癌细胞的活力并减弱 A549 细胞的克隆活性。它可直接抑制IKK 来阻断 NF-κB 的激活。
T78156 MC4033

Apoptosis Apoptosis
MC4033是一种选择性的,可逆的KAT8赖氨酸乙酰转移酶抑制剂,IC50为12.1μM,具有抗癌活性,并能诱导凋亡(apoptosisautophagy)。
T22317 DRB18

transporter Metabolism
DRB18 is a highly effective pan-class inhibitor of glucose transporter proteins (GLUT). It significantly modulates energy-related metabolism in A549 cells by inducing alterations in the abundance of metabolites associated with glucose-related pathways. DRB18 exerts its effects by promoting G1/S phase arrest, increasing oxidative stress, and prompting necrotic cell death, ultimately displaying notable anti-tumor activity [1].
T15411 GPNA hydrochloride

Apoptosis; Others Apoptosis; Others
GPNA hydrochloride 是一种 γ-谷氨酰转移酶的知名底物,可逆地诱导 A549 细胞凋亡。它是一种特定的谷氨酰胺转运蛋白ASCT2抑制剂,还抑制依赖 Na+的载体,如 SNAT 家族 (SNAT1/2/4/5) 和不依赖 Na+的亮氨酸转运蛋白 LAT1/2。
T36493 CMLD-2

Apoptosis; HuR Apoptosis; Chromatin/Epigenetic
CMLD-2是一种 HuR-ARE 相互作用的抑制剂(Ki:350 nM),能竞争性地结合 HuR 蛋白并破坏其与富含腺嘌呤元素(ARE)的 mRNA 目标的相互作用。CMLD-2诱导细胞凋亡并通过 MAD2下调表现出抗肿瘤作用。CMLD-2 (1-75 μM ; 24-72 h) 对甲状腺癌细胞的活力具有抑制作用.CMLD-2 (20-30 μM ; 24-48 h) 激活 Caspases 并诱导H1299和A549细胞凋亡.CMLD-2 (30 μM ; 24-48 h) 诱导H1299和A549细胞的G1细胞周期停止和线粒体扰动。 CMLD-2(30μM;24-48小时)减少H1299细胞中HuR 和HuR 调节的mRNAs 和蛋白质的表达.CMLD-2(35μM;72小时)降低SW1736、8505C、BCPAP 和K1细胞的定向迁移能力。CMLD-2诱导SW1736、8505C、BCPAP 和K1细胞中的MAD2 mRNA 水平强烈下降。
T9582 CLEFMA

NF-κB NF-κB
CLEFMA 是一种姜黄素,抑制肿瘤生长与 NF-κB 调节的抗炎和抗转移作用有关,具有抗肿瘤活性。
T20882 4-Nitrobenzoic acid

Kyselina p-nitrobenzoova,4Nitrobenzoic acid,Nitrodracylic acid,4 Nitrobenzoic acid

4-Nitrobenzoic acid (4Nitrobenzoic acid) 是一种药物中间体,常在叶酸、DABA、PABA 和染料的生产中出现。
T19661 8-Chloroadenosine

NSC 354258,8-Cl-Ado,NSC354258,NSC-354258,8-氯腺嘌呤核苷

AMPK Chromatin/Epigenetic; PI3K/Akt/mTOR signaling
8-Chloroadenosine (NSC-354258) 是一种 5' AMP 激活的蛋白激酶激动剂,可能用于治疗慢性淋巴细胞白血病。 它的活性与 mTOR 通路的抑制有关。它是一种核苷类似物。在体内代谢为 8-氯-ATP。在转录过程中掺入 RNA 并抑制 RNA 合成。在 MM.1S、RPMI-8226 和 U266 癌细胞系中表现出细胞毒性;在 A549 和 H1299 细胞中诱导 G2/M 细胞周期停滞和有丝分裂灾难。它已被证明可消耗 ATP 并抑制血液恶性肿瘤以及肺癌和乳腺癌细胞系中的肿瘤生长。
T35610 2,5-dimethyl Celecoxib

Apoptosis; Wnt/beta-catenin; Prostaglandin Receptor Apoptosis; Cytoskeletal Signaling; GPCR/G Protein; Immunology/Inflammation; Stem Cells
2,5-dimethyl Celecoxib 是塞来昔布衍生物和微粒体前列腺素 E 合酶 1 (mPGES-1) 的靶向抑制剂,mPGES-1 是炎症介质 PGE2 合成途径中的关键酶。
T11421 Glutaminase-IN-1

CB839 derivative

transporter Metabolism
Glutaminase-IN-1 (CB839 derivative),是一种新型 1,3,4-硒二氮基肾型谷氨酰胺酶(KGA) 的变构抑制剂,在侵袭性 H22 肝癌异种移植模型中显示出抗肿瘤活性。
T72057 H1k

CDK Cell Cycle/Checkpoint
H1k 是一种 eudistomin Y 荧光衍生物和溶酶体靶向抗增殖剂。它可以剂量依赖性地增加自噬信号,下调细胞周期蛋白依赖性激酶(cyclin-dependent kinase, CDK1)和细胞周期蛋白 B1的表达。
T72784 OTUB1/USP8-IN-1

DUB Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Ubiquitination
OTUB1/USP8-IN-1 是一种高效的 OTUB1/USP8 抑制剂,具有潜在的抗癌活性,对 OTUB1 和 USP8 的 IC50 值分别为 0.17 和 0.28 nM。OTUB1/USP8-IN-1 可用于研究非小细胞肺癌。
T10960L Darbufelone mesylate

CI-1004 mesylate

Prostaglandin Receptor; LTR GPCR/G Protein; Immunology/Inflammation
Darbufelone mesylate (CI-1004 mesylate) 对细胞中 PGF2α 和 LTB4 产生有抑制作用。Darbufelone mesylate 对 PGHS-2 有抑制作用,IC50 值为 0.19 μM,对 PGHS-1 的IC50 值为 20 μM。
T31411 DHA-37

DHA 37

DHA-37 is an inducer of autophagic cell death through upregulation of HMGB1 in A549 cells.
T11929 M2N12

Phosphatase Metabolism
M2N12 是一种高度选择性的细胞分裂周期蛋白磷酸酶 25C 抑制剂,IC50值为 0.09 μM。它还抑制 Cdc25A 和 Cdc25B 的活性,IC50值分别为 0.53 μM 和 1.39 μM。它具有抗肿瘤活性,可研究癌症。
T78941 Anticancer agent 130

Apoptosis Apoptosis
Anticanceragent 130 (化合物 8d) 能有效诱导A549细胞的凋亡,表现出显著的抗癌活性。
T82715 Cisplatin-resistant cells-IN-1

Cisplatin-resistant cells-IN-1(化合物8)对顽固的铂类药物抗性细胞具有较高的细胞毒性。在低纳摩尔浓度范围内(IC50:0.14–1.79 μM in A549/A549-R, K562/K562-R, and MCF-7/MCF-7TamR cells),该化合物能有效降低代谢活性。
T81569 PAK4-IN-3

PAK Cytoskeletal Signaling
PAK4-IN-3 (compound 27e) 作为PAK4抑制剂,展现了10 nM的IC50。此化合物针对A549细胞表现出0.61 μM的IC50抗增殖效果,并能以浓度依赖的方式诱导A549细胞发生凋亡 (apoptosis),同时使细胞周期停滞在G0/G1期。
T74400 TC113

TC113是一种与c(RGDyK)偶联的Gemcitabine。它通过整合素αvβ3可被A549细胞内化。此外,TC113对WM266.4和A549细胞表现出显著的抗增殖效果。
T63590 c-Met-IN-10

c-Met-IN-10 是高效的 c-Met 激酶抑制剂 (IC50: 16 nM)。c-Met-IN-10 能够抑制癌细胞 A549、H460 和 HT-29 的活性,通过抑制 HT-29 细胞集落形成,进而诱导 HT-29 和 A549 细胞凋亡 apoptosis,抑制 A549 细胞移动。c-Met-IN-10 能够用于抗癌研究。
T72544 4-Formylcolchicine

4-Formylcolchicine 为一有效抗癌化合物,展示对 A549、HT-29、HCT116 细胞具有细胞毒性活性,其 IC50 值分别为 1.007 µM、0.128 µM、0.054 µM。
T64179 Anticancer agent 65

Anticancer agent 65 在肿瘤细胞系中显示出良好的效果,尤其是 A549 细胞 (IC50: 1.07 μM)。Anticancer agent 65 能够将 A549 细胞的细胞周期阻滞在 S 期,诱导细胞凋亡,增加 p53、p21 的表达水平,并促使 ROS 生成和 MMP 崩溃。
T61405 LSD1-IN-14

LSD1-IN-14, a powerful and specific inhibitor of LSD1 (with an IC50 value of 0.89 μM), effectively suppresses the growth of A549 and THP-1 cells and promotes the apoptosis of tumor cells [1].
T68209 Kopsoffinol

Kopsoffinol is a bisindole alkaloid that has been shown to have in vitro growth inhibitory activity against human PC-3, HCT-116, MCF-7, and A549 cells and moderate effects in reversing multidrug-resistance in vincristine-resistant human KB cells.
T64085 KRAS G12C inhibitor 43

KRAS G12C inhibitor 43 是 KRAS G12C 的有效抑制剂,能够抑制 H358 细胞 (IC50: 0.001-1 μM μM)、 A549 细胞 (IC50>1 μM)、 HCC 细胞 (IC50>1 μM) 的迁移和增殖。
T72476 Anticancer agent 59

Anticancer agent 59 对多种癌细胞具有抑制活性,特别是在 A549 细胞中 (IC50= 0.2 μM),Anticancer agent 59 诱导肿瘤细胞凋亡,也诱导 Ca2+和ROS 水平升高,能显著降低线粒体膜电位。Anticancer agent 59 在 A549 异种移植小鼠模型中能显著抑制肿瘤生长。
T83914 Glutaminase C Inhibitor 11

Glutaminase C inhibitor 11是一种glutaminase C (GAC)的抑制剂。它能够抑制GAC酶的活性(EC50 = 10.64 nM),降低A549非小细胞肺癌(NSCLC)细胞的活力(IC50 = 4.025 nM)。在A549细胞中,Glutaminase C inhibitor 11(0.1和1 µM)能减少细胞集落形成并降低细胞内谷氨酸水平。在体内,Glutaminase C inhibitor 11(100 mg/kg)能够减缓A549小鼠异位瘤模型中的肿瘤生长。
T79724 IGF2BP1-IN-1

IGF2BP1-IN-1(Compound A11)是一款高效的IGF2BP1抑制剂,对IGF2BP1蛋白有很强的结合能力,KD值仅为2.88 nM。该化合物能显著抑制A549和HCT116癌细胞株的增殖,IC50值分别为9 nM和34 nM,且能诱导癌细胞发生凋亡。此外,IGF2BP1-IN-1在A549异种移植小鼠模型中有效抑制了肿瘤生长。
T60546 Anti-MRSA agent 6

Anti-MRSA agent 6 (compound 3q6) 是一种有效的抗耐甲氧西林金黄色酿脓葡萄球菌(anti-MRSA)剂,对 MCF-7、A549 细胞具有低细胞毒性。
T64034 Antitumor agent-45

Antitumor agent-45 对 c-Met 表达具有抑制作用,能够将 A549 细胞的细胞阻滞在 G0/G1 和 G2/M 期,并诱导其凋亡。
T63895 EGFR-IN-62

EGFR-IN-62 是 EGFR 激酶的有效抑制剂,对 L858R/T790 M、WT 和 L858R/T790 M/C797S 的 IC50 值分别为10 nM、29 nM 和2 42 nM。EGFR-IN-62 可将 A549 和/或 H1975细胞周期阻滞在 G1/G0 期,并诱导凋亡和运动抑制,有效的抑制 A549 细胞 (IC50: 2.53 μM) 和 H1975 细胞 (IC50: 1.56 μM) 的增殖。
T27115 CZh226

CZh-226,CZh 226

CZh226 is a potent and selective PAK4 inhibitor (PAK4 Ki = 9 nM; PAK1 Ki = 3112 nM). CZh226 potently inhibits the migration and invasion of A549 tumor cells by regulating the PAK4-directed downstream signaling pathways in vitro.
T74605 Antitumor agent-64

Antitumor agent-64 (Compound 8d),一种薯蓣皂苷元衍生物,对A549细胞系展示出显著的细胞毒性。通过线粒体相关途径促进A549细胞的凋亡(apoptosis)。

化合物

HPOB
Cat.No: T2430
Synonym:
Target: Apoptosis, HDAC
PARP1-IN-8 
Cat.No: T9891
Synonym: N-(3-chlorophenyl)-3-(1-oxo-4-phenylphthalazin-2(1H)-yl)propanamide
Target: PARP
Theophylline monohydrate
Cat.No: T1083L
Synonym: Quibron,茶碱一水合物
Target: HDAC, PDE, Adenosine Receptor
OTS186935 FA
Cat.No: T12344L1
Synonym: OTS186935 FA(2093400-18-9 Free base)
Target: Histone Methyltransferase
AEM1
Cat.No: T8979
Synonym:
Target: Nrf2
GW-870086
Cat.No: T15451
Synonym:
Target: Glucocorticoid Receptor
SW155246
Cat.No: T8967
Synonym:
Target: DNA Methyltransferase
PARP-1-IN-2
Cat.No: T62281
Synonym:
Target: PARP
WZB117
Cat.No: T7018
Synonym:
Target: transporter
PF-6274484
Cat.No: T22396
Synonym: PF 6274484
Target: EGFR
KDM4C-IN-1
Cat.No: T60654
Synonym:
Target: Histone Demethylase
NAE-IN-M22
Cat.No: T8816
Synonym: NEDD8 inhibitor M22
Target: Apoptosis, E1/E2/E3 Enzyme
Inauhzin
Cat.No: T1887
Synonym: INZ
Target: Sirtuin
HDAC8-IN-1
Cat.No: T7082
Synonym:
Target: HDAC
mTOR inhibitor-8
Cat.No: T36316
Synonym: mTOR-IN-8
Target: mTOR, Autophagy
ULK1-IN-2
Cat.No: T63343
Synonym:
Target: Apoptosis, Autophagy
ERK Inhibitor
Cat.No: T36675
Synonym:
Target:
NF-κB-IN-1
Cat.No: T9105
Synonym: 1,6-Heptadiene-3,5-dione, 1,7-bis(3,4-dimethoxyphenyl)-4-[(4-hydroxy-3-methoxyphenyl)methylene]-, (1E,6E)-
Target: IκB/IKK, NF-κB
MC4033
Cat.No: T78156
Synonym:
Target: Apoptosis
DRB18
Cat.No: T22317
Synonym:
Target: transporter
GPNA hydrochloride
Cat.No: T15411
Synonym:
Target: Apoptosis, Others
CMLD-2
Cat.No: T36493
Synonym:
Target: Apoptosis, HuR
CLEFMA
Cat.No: T9582
Synonym:
Target: NF-κB
4-Nitrobenzoic acid
Cat.No: T20882
Synonym: Kyselina p-nitrobenzoova,4Nitrobenzoic acid,Nitrodracylic acid,4 Nitrobenzoic acid
Target:
8-Chloroadenosine
Cat.No: T19661
Synonym: NSC 354258,8-Cl-Ado,NSC354258,NSC-354258,8-氯腺嘌呤核苷
Target: AMPK
2,5-dimethyl Celecoxib
Cat.No: T35610
Synonym:
Target: Apoptosis, Wnt/beta-catenin, Prostaglandin Receptor
Glutaminase-IN-1
Cat.No: T11421
Synonym: CB839 derivative
Target: transporter
H1k
Cat.No: T72057
Synonym:
Target: CDK
OTUB1/USP8-IN-1
Cat.No: T72784
Synonym:
Target: DUB
Darbufelone mesylate
Cat.No: T10960L
Synonym: CI-1004 mesylate
Target: Prostaglandin Receptor, LTR
DHA-37
Cat.No: T31411
Synonym: DHA 37
Target:
M2N12
Cat.No: T11929
Synonym:
Target: Phosphatase
Anticancer agent 130
Cat.No: T78941
Synonym:
Target: Apoptosis
Cisplatin-resistant cells-IN-1
Cat.No: T82715
Synonym:
Target:
PAK4-IN-3
Cat.No: T81569
Synonym:
Target: PAK
TC113
Cat.No: T74400
Synonym:
Target:
c-Met-IN-10
Cat.No: T63590
Synonym:
Target:
4-Formylcolchicine
Cat.No: T72544
Synonym:
Target:
Anticancer agent 65
Cat.No: T64179
Synonym:
Target:
LSD1-IN-14
Cat.No: T61405
Synonym:
Target:
Kopsoffinol
Cat.No: T68209
Synonym:
Target:
KRAS G12C inhibitor 43
Cat.No: T64085
Synonym:
Target:
Anticancer agent 59
Cat.No: T72476
Synonym:
Target:
Glutaminase C Inhibitor 11
Cat.No: T83914
Synonym:
Target:
IGF2BP1-IN-1
Cat.No: T79724
Synonym:
Target:
Anti-MRSA agent 6
Cat.No: T60546
Synonym:
Target:
Antitumor agent-45
Cat.No: T64034
Synonym:
Target:
EGFR-IN-62
Cat.No: T63895
Synonym:
Target:
CZh226
Cat.No: T27115
Synonym: CZh-226,CZh 226
Target:
Antitumor agent-64
Cat.No: T74605
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T1083 Theophylline

Theo-24,1,3-Dimethylxanthine,茶碱

Endogenous Metabolite; HDAC; PDE; Adenosine Receptor; Autophagy Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair; GPCR/G Protein; Metabolism; Neuroscience
Theophylline (1,3-Dimethylxanthine) 是茶中的甲基黄嘌呤衍生物,具有利尿、平滑肌松弛、支气管扩张、心脏和中枢神经系统兴奋作用。
T2870 Matrine

Vegard,苦参碱,Matridin-15-one,Matrinium,α-Matrine,(+)-Matrine

Mitophagy; Ferroptosis; Opioid Receptor; Autophagy Apoptosis; Autophagy; Endocrinology/Hormones; GPCR/G Protein; Neuroscience
Matrine (Vegard) 是一种从槐属植物中分离出来的生物碱,可作为一种κ阿片受体激动剂,有抗肿瘤活性。
T3008 Lawsone methyl ether

2-Methoxy-1,4-naphthoquinone,2-Methoxy-p-naphthoquinone,2-Methoxynaphthoquinone,2-甲氧基-1,4-萘并醌

Apoptosis; Antibacterial; Antifungal Apoptosis; Microbiology/Virology
Lawsone methyl ether (2-Methoxy-1,4-naphthoquinone) 是从凤仙花和Swertia calycina 中分离出的,有抗真菌和抗菌活性。
T2S1593 Gypenoside XLVI

Others Others
Gypenoside XLVI 是一种来源于绞股蓝的主要达玛烷型三萜皂苷。它具有四环三萜结构,能够有效抑制非小细胞肺癌 A549 细胞的活性。
T4S1540 Myrislignan

Apoptosis; NF-κB Apoptosis; NF-κB
Myrislignan 是一种木酚素,从Myristica fragransHoutt 分离得到,具有抗炎作用。它通过抑制NF-kB 信号通路的激活,减轻LPS 诱导的小鼠巨噬细胞炎症反应。
T5758 sphondin

6-甲氧基当归素,牛防风素,牛防风素

COX; Prostaglandin Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
Sphondin 具有抗惊厥、抗炎和抗增殖活性,对 IL-1beta 诱导的 A549 细胞中 COX-2 蛋白水平和 PGE(2) 释放的增加具有抑制作用。
T3771 Methyl protodioscin

山药,Smilax saponin B,NSC-698790

Apoptosis Apoptosis
Methyl protodioscin (Smilax saponin B) 是一种甾二糖苷,能诱导细胞周期阻滞,具有抗肿瘤活性。
T3870 Cyasterone

杯苋甾酮,Cyasteron

Apoptosis; EGFR Angiogenesis; Apoptosis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
Cyasterone (Cyasteron) 是主要分离自金疮小草的一种天然 EGFR 抑制剂。它通过诱导细胞凋亡和细胞周期阻滞表现出抗增殖作用,可用于抗人类肿瘤的相关研究。
T3404 Cucurbitacin B

Cuc B,葫芦素B,DATISCACIN,葫芦素 B,Amarine

Apoptosis; PTEN; Integrin; Endogenous Metabolite; HIF; STAT; Autophagy Angiogenesis; Apoptosis; Autophagy; Chromatin/Epigenetic; Cytoskeletal Signaling; JAK/STAT signaling; Metabolism; PI3K/Akt/mTOR signaling; Stem Cells
Cucurbitacin B (Cuc B) 是一具有抗癌活性的天然产物。
T2S0618 β-Elemonic Acid

3-oxo Tirucallic Acid,β-岚香酮酸,Beta-Elemonic acid,3-Oxotirucallenoic Acid,β-榄香酮酸,Elemadienonic Acid

Apoptosis; Reactive Oxygen Species; COX Apoptosis; Immunology/Inflammation; Metabolism; Neuroscience; NF-κB
β-Elemonic Acid (3-Oxotirucallenoic Acid) 是从乳香树中分离得到的一种三萜,具有抗癌和抗炎作用。它抑制脯氨酰内肽酶,诱导细胞凋亡,活性氧和COX-2表达。
T7027 EURYCOMANONE

东革阿里提取物,Pasakbumin A

Others Others
Eurycomanone (Pasakbumin A) 能够抑制雌激素生成过程中磷酸二酯酶和芳香酶的活性,促进精子生成。它对 HepG2 细胞具有细胞毒性,能够上调 p53 和 Bax 以及下调 Bcl-2 ,诱导细胞凋亡。它具有抗癌活性,在浓度范围内以剂量依赖性方式抑制 A549 肺癌细胞增殖 从 5 到 20 微克/毫升。
TN1721 Gypenoside L

ERK; p38 MAPK; Calcium Channel; NF-κB; ROS Immunology/Inflammation; MAPK; Membrane transporter/Ion channel; Metabolism; NF-κB
Gypenoside L 是存在于绞股蓝中的一种皂苷,可增加 SA-β-半乳糖苷酶活性,促进衰老相关分泌细胞因子的产生。它还可以激活p38和ERK MAPK 通路和NF-κB 通路以诱导衰老,具有抗肿瘤和抗炎活性。
T6S0077 Byakangelicol

COX Immunology/Inflammation; Neuroscience
Byakangelicol 是一种分离自白芷的白三醇,能够抑制环加氧酶-2的表达及活性,从而减少白细胞介素-1β诱导的 A549 细胞中前列腺素 E2 的释放。它可用于研究气道炎症。
TN1516 Cnidicin

蛇床素,4,9-双[(3-甲基-2-丁烯-1-基)氧基]-7H-呋喃并[3,2-G][1]苯并吡喃-7-酮

NOS; NO Synthase Immunology/Inflammation
Cnidicin 是一种香豆素,对肥大细胞脱颗粒及 RAW 264.7 细胞产生一氧化氮具有抑制作用。
TN1003 DL-Alanine

DL-2-Aminopropionic acid

Endogenous Metabolite Metabolism
DL-Alanine (DL-2-Aminopropionic acid) 是一种氨基酸,是L-和D-丙氨酸的外消旋化合物。DL-Alanine 与硝酸银水溶液一起用于纳米颗粒生成时常作为还原剂和封端剂。DL-Alanine 是一种甜味剂,可把它位与甘氨酸和糖精钠归为一类。DL-Alanine 在组织和肝脏之间的葡萄糖-丙氨酸循环中起重要作用。DL-Alanine 可用于研究 Cu、Zn、Cd 等过渡金属螯合。
T2973 Astragaloside IV

AST-IV,黄芪甲苷IV,AS-IV,黄芪皂苷 IV

MMP; ERK; Estrogen/progestogen Receptor; JNK Endocrinology/Hormones; MAPK; Proteases/Proteasome
Astragaloside IV (AS-IV) 是从黄芪中分离得到的一种皂苷,抑制ERK1/2和JNK 激活,在乳腺癌细胞 MDA-MB-231 中,下调(MMP)-2和(MMP)-9的信号通路。
TN5538 6-Methoxykaempferol

Others Others
6-Methoxykaempferol 是一种存在于 brazilian propolis 中的黄酮。6-Methoxykaempferol 对癌细胞具有抗增殖活性,对离体大鼠脑突触体的神经保护作用,可降低的谷胱甘肽水平。6-Methoxykaempferol 表现出一定的脂肪酶活性,可用于恶病质的治疗。
TN5274 Yunnancoronarin A

Others Others
Yunnancoronarin A shows cytotoxicity against the lung adenocarcinoma cells A549 and leukemia cells K562, with the IC(50) value of 2.20 microM.
T82429 Euphoheliosnoid A

Euphoheliosnoid A (Compound 24) 为二萜类化合物,以 2.5 μM 浓度显著提升 NK 细胞针对 H1299-luci 及 A549-luci 细胞的杀伤效率。
TN2669 1beta-Hydroxytorilin

Others Others
1beta-Hydroxytorilin exhibits cytotoxicity against human A549, SK-OV-3, SK-MEL-2, and HCT15 tumor cells.
T82427 Euphoscopin C

Euphoscopin C, 一种自Euphorbia helioscopia分离得到的二萜类化合物,可显著增强NK细胞对H1299-luci细胞和A549-luci细胞的杀伤活性。
T21523 β-Tocotrienol

Beta-Tocotrienol

Caspase Apoptosis; Proteases/Proteasome
Beta-Tocotrienol to serve as a new anticancer agent for treating human lung and brain cancers. It inhibits the growth of both A549 (GI50=1.38±0.334μM) and U87MG (GI50=2.53±0.604μM) cells at rather low concentrations.
TN2114 Pseudoginsenoside Rh2

拟人参皂苷RH2,拟人参皂苷 Rh2

ERK; Raf; p53 Apoptosis; MAPK
Pseudoginsenoside Rh2 has cytotoxicity, it induces mitochondrial apoptosis in A549 cells and is responsible for excessive activation of the Ras/Raf/ERK/p53 pathway. (20Z) -Pseudoginsenoside Rh2 and (20E)-Pseudoginsenoside Rh2 have antioxidative activity.
TN5373 Ustusolate A

1. Ustusolate A shows weak cytotoxicity against HL-60 and A549 cells with IC50 values of 20.6 and 30.0 microM, respectively.
TN1872 Linderone

Others Others
Linderone A shows anticancer activity against A549 non-small cell lung cancer cells and PC-3 prostate adenocarcinoma cell line.
TN5210 Ustusolate C

Others Others
Ustusolate C and ustusolate E exhibit moderate cytotoxicity against A549 and HL-60 cells with IC50 values of 10.5 and 9.0 microM, respectively.
TN4172 Guajadial B

Topoisomerase DNA Damage/DNA Repair
Guajadial B acts as a Top1 catalytic inhibitor and delays Top1 poison-mediated DNA damage. Guajadial B shows cytotoxicities against five human cancer cell lines, it is the most effective having an IC50 value of 150 nM toward A549 cells.
T82808 Bufoserotonin C

Bufoserotonin C为蟾酥中新发现的吲哚生物碱,展现出对抗肿瘤的活性。其在A549细胞系中的IC50为34.3 μM。
TN3617 Cedrelopsin

Others Others
Cedrelopsin shows significant inhibition against A549 cells with IC50 values of 3.6-5.9 ug/mL.
TN4356 Jolkinolide A

Akt; STAT; mTOR Cytoskeletal Signaling; JAK/STAT signaling; PI3K/Akt/mTOR signaling; Stem Cells
Jolkinolide A has anti-tumor activity. It inhibited VEGF expression in A549 cells through the inhibition of the Akt-STAT3-mTOR signaling pathway, and directly inhibited the proliferation and migration of HUVECs.
T13629 Cyclo(Ala-Gly)

Others Others
Cyclo (Ala-Gly) is a mangrove endophytic fungus, a metabolite of Penicillium thomi, which is cytotoxic to A549, HepG2 and HT29 cells. The IC50 value is in the range of 9.5-18.1 μM.
TN5879 Edgeworin

Edgeworin is a DNA polymerase beta (pol beta) inhibitor, it inhibits both the lyase and polymerase activities of DNA polymerase beta; it can potentiate the inhibitory action of the anticancer drug bleomycin in cultured A549 cells via an inhibition of DNA
TN2666 1alpha-Hydroxytorilin

Others Others
1alpha-Hydroxytorilin exhibits cytotoxicity against human A549, SK-OV-3, SK-MEL-2, and HCT15 tumor cells.
T83481 1,1′-Disinomenine

1,1'-Disinomenine,一种从Sinomenium acutum茎部分离得到的生物碱,对A549和Hela细胞表现出较弱的抑制效果。
TN2191 Scutebarbatine A

BCL; Caspase Apoptosis; Proteases/Proteasome
Scutebarbatine A shows significant antitumor effects on A549 cells in vivo and in vitro via mitochondria-mediated apoptosis by up-regulating expressions of caspase-3 and 9, and down-regulating Bcl-2. Scutebarbatine A and barbatine A show a significant ability to protect cells against H2O2 with ED50 values of 5.0 and 16.8 μM, respectively.
TN5211 Ustusolate E

Others Others
Ustusolate E exhibits moderate cytotoxicity against A549 and HL-60 cells with the IC50 value of 9.0 microM.
T82298 Glucozaluzanin C

Glucozaluzanin C,一种木脂素类化合物,由菊科鸢尾根的MeOH提取物中分离得到,显示出对多种细胞系具有显著的生物活性。具体而言,其在A549、SK-OV-3、SK-MEL-2、XF498和HCT15细胞上的ED50值依次为2.45 μg/mL、1.37 μg/mL、0.40 μg/mL、1.41 μg/mL、1.43 μg/mL。
T81132 Soladulcoside A

Soladulcoside A,一种甾体糖苷及抗肿瘤剂,源自龙葵全株。该化合物可抑制A549细胞,并展示对治疗非小细胞肺癌(NSCLC)等癌症的潜在应用。
T37543 Anhydroepiophiobolin A

Anhydroepiophiobolin A is a sesterterpenoid fungal metabolite that has been found in B. oryzae. It is cytotoxic to HepG2 and K562 cells (IC50s = 47.1 and 35.6 μM, respectively) as well as A549, SKOV3, SK-MEL-2, XF498, and HCT15 cells (IC50s = 1.6-1.9 μg/ml). Anhydroepiophiobolin A is phytotoxic to S. viridis and D. erucoides in a leaf puncture assay.
TN3429 Aphagranin A

Others Others
Aphagranin A exhibits strong antiproliferative activity against the growth of six lines of human cancer cells (MCF-7, A549, HepG2, Bel-7402, SGC-7901, and BGC-823.
T83104 Anthragallol 1,2-dimethyl ether

Anthragallol 1,2-dimethyl ether 可从O. umbellata提取。该化合物对A549细胞和MDA-MB-231细胞展现细胞毒性,IC50值分别为5.9 μg/ml和8.8 μg/ml。
T75646 Moroidin

Moroidin是一种双环八肽,隶属于荨麻疹科环肽科,有效抑制纯化的微管蛋白聚合,表现为微管蛋白聚合抑制剂。此外,Moroidin对包括A549人肺癌细胞在内的多种癌细胞显示出细胞毒性作用,能诱导细胞凋亡。
TN2554 1-Monopalmitin

Glyceryl palmitate

Apoptosis Apoptosis
1-Monopalmitin (Glyceryl palmitate) 是一种从Mougeotia nummuloides 和 Spirulina major 提取出来的小分子化合物,具有潜在的抗肿瘤活性,抑制A549和SPC-A1细胞增殖,诱导G2/M阻滞和半胱天冬酶依赖性细胞凋亡。
T8199 (±)-α-Bisabolol

Bisabolol

Apoptosis; Antioxidant Apoptosis; oxidation-reduction
(±)-α-Bisabolol (Bisabolol) 是一种从洋甘菊、念珠菌树等植物精油中提取的倍半萜烯醇,是一种天然防腐剂,具有舒缓、抗刺激、抗炎、抗氧化和抗癌活性。(±)-α-Bisabolol 通过诱导细胞周期停滞、线粒体死亡和抑制 PI3K/Akt 信号通路来发挥作用,对 A549 NSC-LC 细胞产生抗癌作用 (IC50 = 15 μM)。(±)-α-Bisabolol 能强效诱导胶质瘤细胞凋亡。
T83597 (+)-Menthyl acetate

(+)-Menthyl acetate是一种从Cunila angustifolia Benth精油中分离得到的化学化合物。它对MCF-7细胞株具有较高的选择性,其半抑制浓度(IC50)为34.0 μg/mL,而对SK-Mel-28细胞株的选择性较低,IC50为279.9 μg/mL,并且对A549细胞没有致死作用。
TN3771 Dasycarpol

Others Others
Dasycarpol(9beta-Hydroxyfraxinellone) shows significant neuroprotective activity against glutamate-induced neurotoxicity in primary cultures of rat cortical cells at a concentration of 0.1 microM. Dasycarpol also shows moderate inhibitory activity on lung
TN4959 Schizandriside

Prostaglandin Receptor GPCR/G Protein; Immunology/Inflammation
Schizandriside may have anti-inflammatory effects, it has inhibitory activities against nitric oxide and prostaglandin E(2) production in IFN-γ- and lipopolysaccharide-stimulated RAW 264.7 cells. It shows significant cytotoxicity against A549, SK-OV-3, SK
T83323 4-Chloro-3-methoxy-5-methylphenyl 6-O-(6-deoxy-β-L-mannopyranosyl)-β-D-glucopyranoside

化合物3(4-Chloro-3-methoxy-5-methylphenyl 6-O-(6-deoxy-β-L-mannopyranosyl)-β-D-glucopyranoside)是一种从Lilium regale提取的抗癌天然产物,具有显著抑制肺癌A549细胞增殖的活性,显示出其研究癌症治疗潜力。
TN3525 Boehmenan

ERK; Phosphatase; EGFR; PARP; MEK; Wnt/beta-catenin; Akt; Caspase; STAT; p53 Angiogenesis; Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair; JAK/STAT signaling; MAPK; Metabolism; PI3K/Akt/mTOR signaling; Proteases/Proteasome; Stem Cells; Tyrosine Kinase/Adaptors
(±)-Boehmenan shows potent protein-tyrosine phosphatase 1B (PTP1B) inhibitory activity in vitro with the IC(50) values of 43.5 uM, it inhibits PTP1B activity in a competitive manner. Boehmenan exhibits the potent cytotoxic effects against many cancer cell
T35750 Trypacidin

Trypacidin is a fungal metabolite originally isolated fromA. fumigatus.1It is active againstB. subtilisandM. bovis(MICs = 12.5 and 1.25 μg/ml, respectively), as well asT. cruziandT. gondii(MICs = 5-10 and 10-20 μg/ml, respectively).1,2It reduces viability and induces lysis of A549 human lung cancer cells (IC50s = 7.4 μM for both).3Trypacidin increases survival in a mouse model ofT. gondiiinfection when administered in six doses of 12.5 mg/kg each.1 1.Balan, J., Ebringer, L., Nemec, P., et al.Ant...
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天然产物

Theophylline
Cat.No: T1083
Synonym: Theo-24,1,3-Dimethylxanthine,茶碱
Target: Endogenous Metabolite, HDAC, PDE, Adenosine Receptor, Autophagy
Matrine
Cat.No: T2870
Synonym: Vegard,苦参碱,Matridin-15-one,Matrinium,α-Matrine,(+)-Matrine
Target: Mitophagy, Ferroptosis, Opioid Receptor, Autophagy
Lawsone methyl ether
Cat.No: T3008
Synonym: 2-Methoxy-1,4-naphthoquinone,2-Methoxy-p-naphthoquinone,2-Methoxynaphthoquinone,2-甲氧基-1,4-萘并醌
Target: Apoptosis, Antibacterial, Antifungal
Gypenoside XLVI
Cat.No: T2S1593
Synonym:
Target: Others
Myrislignan
Cat.No: T4S1540
Synonym:
Target: Apoptosis, NF-κB
sphondin
Cat.No: T5758
Synonym: 6-甲氧基当归素,牛防风素,牛防风素
Target: COX, Prostaglandin Receptor
Methyl protodioscin
Cat.No: T3771
Synonym: 山药,Smilax saponin B,NSC-698790
Target: Apoptosis
Cyasterone
Cat.No: T3870
Synonym: 杯苋甾酮,Cyasteron
Target: Apoptosis, EGFR
Cucurbitacin B
Cat.No: T3404
Synonym: Cuc B,葫芦素B,DATISCACIN,葫芦素 B,Amarine
Target: Apoptosis, PTEN, Integrin, Endogenous Metabolite, HIF, STAT, Autophagy
β-Elemonic Acid
Cat.No: T2S0618
Synonym: 3-oxo Tirucallic Acid,β-岚香酮酸,Beta-Elemonic acid,3-Oxotirucallenoic Acid,β-榄香酮酸,Elemadienonic Acid
Target: Apoptosis, Reactive Oxygen Species, COX
EURYCOMANONE
Cat.No: T7027
Synonym: 东革阿里提取物,Pasakbumin A
Target: Others
Gypenoside L
Cat.No: TN1721
Synonym:
Target: ERK, p38 MAPK, Calcium Channel, NF-κB, ROS
Byakangelicol
Cat.No: T6S0077
Synonym:
Target: COX
Cnidicin
Cat.No: TN1516
Synonym: 蛇床素,4,9-双[(3-甲基-2-丁烯-1-基)氧基]-7H-呋喃并[3,2-G][1]苯并吡喃-7-酮
Target: NOS, NO Synthase
DL-Alanine
Cat.No: TN1003
Synonym: DL-2-Aminopropionic acid
Target: Endogenous Metabolite
Astragaloside IV
Cat.No: T2973
Synonym: AST-IV,黄芪甲苷IV,AS-IV,黄芪皂苷 IV
Target: MMP, ERK, Estrogen/progestogen Receptor, JNK
6-Methoxykaempferol
Cat.No: TN5538
Synonym:
Target: Others
Yunnancoronarin A
Cat.No: TN5274
Synonym:
Target: Others
Euphoheliosnoid A
Cat.No: T82429
Synonym:
Target:
1beta-Hydroxytorilin
Cat.No: TN2669
Synonym:
Target: Others
Euphoscopin C
Cat.No: T82427
Synonym:
Target:
β-Tocotrienol
Cat.No: T21523
Synonym: Beta-Tocotrienol
Target: Caspase
Pseudoginsenoside Rh2
Cat.No: TN2114
Synonym: 拟人参皂苷RH2,拟人参皂苷 Rh2
Target: ERK, Raf, p53
Ustusolate A
Cat.No: TN5373
Synonym:
Target:
Linderone
Cat.No: TN1872
Synonym:
Target: Others
Ustusolate C
Cat.No: TN5210
Synonym:
Target: Others
Guajadial B
Cat.No: TN4172
Synonym:
Target: Topoisomerase
Bufoserotonin C
Cat.No: T82808
Synonym:
Target:
Cedrelopsin
Cat.No: TN3617
Synonym:
Target: Others
Jolkinolide A
Cat.No: TN4356
Synonym:
Target: Akt, STAT, mTOR
Cyclo(Ala-Gly)
Cat.No: T13629
Synonym:
Target: Others
Edgeworin
Cat.No: TN5879
Synonym:
Target:
1alpha-Hydroxytorilin
Cat.No: TN2666
Synonym:
Target: Others
1,1′-Disinomenine
Cat.No: T83481
Synonym:
Target:
Scutebarbatine A
Cat.No: TN2191
Synonym:
Target: BCL, Caspase
Ustusolate E
Cat.No: TN5211
Synonym:
Target: Others
Glucozaluzanin C
Cat.No: T82298
Synonym:
Target:
Soladulcoside A
Cat.No: T81132
Synonym:
Target:
Anhydroepiophiobolin A
Cat.No: T37543
Synonym:
Target:
Aphagranin A
Cat.No: TN3429
Synonym:
Target: Others
Anthragallol 1,2-dimethyl ether
Cat.No: T83104
Synonym:
Target:
Moroidin
Cat.No: T75646
Synonym:
Target:
1-Monopalmitin
Cat.No: TN2554
Synonym: Glyceryl palmitate
Target: Apoptosis
(±)-α-Bisabolol
Cat.No: T8199
Synonym: Bisabolol
Target: Apoptosis, Antioxidant
(+)-Menthyl acetate
Cat.No: T83597
Synonym:
Target:
Dasycarpol
Cat.No: TN3771
Synonym:
Target: Others
Schizandriside
Cat.No: TN4959
Synonym:
Target: Prostaglandin Receptor
4-Chloro-3-methoxy-5-methylphenyl 6-O-(6-deoxy-β-L-mannopyranosyl)-β-D-glucopyranoside
Cat.No: T83323
Synonym:
Target:
Boehmenan
Cat.No: TN3525
Synonym:
Target: ERK, Phosphatase, EGFR, PARP, MEK, Wnt/beta-catenin, Akt, Caspase, STAT, p53
Trypacidin
Cat.No: T35750
Synonym:
Target:
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