105
25
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T16163 |
MV1
|
Apoptosis | Apoptosis |
MV1 是一种 IAP 拮抗剂。 当与 HaloTag 配体结合时,它会导致 HaloTag 融合蛋白的蛋白质敲低。 | |||
T6100 |
Torin 2
|
Apoptosis; ATM/ATR; DNA-PK; mTOR; Autophagy | Apoptosis; Autophagy; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
Torin 2 是一种特异性 mTOR 抑制剂,IC50值为0.25 nM,并改善了药代动力学特性。它抑制 ATM/ATR/DNA-PK 的 EC50 分别为 28 nM/35 nM/118 nM。 | |||
T6143 |
PI-103
PI103,PI 103 |
Apoptosis; DNA-PK; PI3K; mTOR; Autophagy | Apoptosis; Autophagy; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
PI-103 是一种 PI3K 和 mTOR 抑制剂,抑制 p110α、p110β、p110δ、p110γ、mTORC1和 mTORC2,IC50分别为 8 nM、88 nM、48 nM、150 nM、20 nM 和 83 nM。它可诱导自噬,还抑制 DNA-PK,IC50为 2 nM。 | |||
T1784 |
Everolimus
依维莫司,RAD001,SDZ-RAD |
Apoptosis; Others; mTOR; Autophagy | Apoptosis; Autophagy; Others; PI3K/Akt/mTOR signaling |
Everolimus (SDZ-RAD) 是 Rapamycin 的衍生物,也是一种口服活性的mTOR1选择性抑制剂。它与FKBP-12结合可产生免疫抑制复合物,还抑制肿瘤细胞增殖并诱导细胞凋亡和自噬,有免疫抑制和抗癌活性。 | |||
T16156 |
MT 63-78
|
Apoptosis; AMPK; mTOR | Apoptosis; Chromatin/Epigenetic; PI3K/Akt/mTOR signaling |
MT 63-78 是一种有效的直接AMPK 激活剂,EC50为 25 μM。它诱导细胞有丝分裂阻滞和细胞凋亡,通过抑制脂肪生成和mTORC1途径来阻止前列腺癌的生长,具有抗肿瘤作用。 | |||
T9831 |
MKC-1
Ro-31-7453 |
Apoptosis; Akt; Microtubule Associated; mTOR | Apoptosis; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
MKC-1 (Ro-31-7453) 是一种口服生物可利用的小分子双吲哚基马来酰亚胺细胞周期抑制剂,具有潜在的抗肿瘤活性。 | |||
T2066 |
Quizartinib
AC220,奎扎替尼 |
Apoptosis; FLT; Autophagy; Ligands for Target Protein for PROTAC | Angiogenesis; Apoptosis; Autophagy; PROTAC; Tyrosine Kinase/Adaptors |
Quizartinib (AC220) 是一种具有口服活性的高选择性Ⅱ 型 FLT3酪氨酸激酶抑制剂,可诱导细胞凋亡。它抑制 Wt FLT3 和 突变型 FLT3-ITD 自磷酸化,IC50分别为 4.1 nM 和 1.1 nM。它可通过优化的 linker 与 VHL 配体连接,从而形成 PROTAC Flt3 降解剂。 | |||
T29097 |
VAS 3947
VA-S3947,VA S3947,VAS3947 |
Apoptosis; NADPH-oxidase | Apoptosis; Immunology/Inflammation |
VAS 3947 是一种特异的 NADPH 氧化酶 (NOX) 抑制剂。VAS 3947具有强大的抗血小板作用, 通过 UPR 激活,主要由于蛋白质聚集和错误折叠,独立于抗 NOX 活性诱导细胞凋亡。 | |||
T77584 |
Tubulin inhibitor 35
Tubulin IN 35 |
Apoptosis; Microtubule Associated; Topoisomerase | Apoptosis; Cytoskeletal Signaling; DNA Damage/DNA Repair |
Tubulin inhibitor 35 (Tubulin IN 35) 是一种有效的拓扑异构酶 I 和微管蛋白聚合 的双重抑制剂,具有抗肿瘤活性,对 MGC-803 和 RKO 细胞株的迁移和侵袭有抑制作用,中断细胞周期,诱导凋亡 (apoptosis)。 | |||
T6007 |
Birinapant
TL32711,比瑞那帕 |
Apoptosis; IAP; HIV Protease | Apoptosis; Microbiology/Virology; Proteases/Proteasome |
Birinapant (TL32711) 是一种二价 Smac 模拟物,是 XIAP 和 cIAP1的强效拮抗剂,Kd 值分别为 45 nM 和小于 1 nM。它靶向与 TRAF2 相关的 cIAP,并消除 TNF 诱导的 NF-κB 活化。 | |||
T6248 |
XL888
|
HSP | Cytoskeletal Signaling; Metabolism |
XL888 是一种 ATP 竞争性的 Hsp90 抑制剂,IC50值为 24 nM。 | |||
T1844 |
KPT330,(E)-
(E)-RN,KPT-330,KPT330,KPT 330 |
Others; CRM1 | Membrane transporter/Ion channel; Others |
(E)-RN (KPT 330) 是一种 CRM1 选择性核输出抑制剂。它抑制细胞核中的蛋白质运输并诱导间皮瘤细胞中的细胞周期停滞和凋亡。 | |||
T63260 |
Snail/HDAC-IN-1
|
Apoptosis; Antifungal | Apoptosis; Microbiology/Virology |
Snail/HDAC-IN-1是一种Snail/HDAC 抑制剂剂,具有抗菌抗癌活性, 可降低Snail蛋白的表达,诱导细胞凋亡,可用于研究实体肿瘤。 | |||
T24051 |
Exisulind
Sulindac sulfone,CP248 |
Apoptosis; PKA | Apoptosis; Tyrosine Kinase/Adaptors |
Exisulind (CP248) 通过激活蛋白激酶 G (PKG) 诱导细胞凋亡。 Exisulind 在实体瘤和血液癌细胞系中表现出抗肿瘤活性,并且是结肠癌、前列腺癌、膀胱癌、乳腺癌和肺癌啮齿动物模型中肿瘤生长的抑制剂。 | |||
T8901 |
YUM70
|
Apoptosis; GPR; HSP | Apoptosis; Cytoskeletal Signaling; Endocrinology/Hormones; GPCR/G Protein; Metabolism |
YUM70 是一种选择性葡萄糖调节蛋白 78 抑制剂,抑制全长蛋白的 GRP78 ATPase 活性的IC50值为 1.5 μM。它在胰腺癌中诱导内质网应激介导的细胞凋亡。 | |||
T24212 |
XX-650-23
XX65023,XX 650 23 |
Apoptosis; Epigenetic Reader Domain | Apoptosis; Chromatin/Epigenetic |
XX-650-23 是一种小分子 CREB 抑制剂,阻断 CREB 与其所需的共激活因子 CBP(CREB 结合蛋白)之间的关键相互作用,诱导AML细胞凋亡和细胞周期停滞,可用于研究急性髓系白血病 (AML)。 | |||
T60217 |
TAS1553
|
Others | Others |
TAS1553是一种高效的可口服蛋白质-蛋白质相互作用(PPI)抑制剂,其IC50值为0.0396 μM。TAS1553 有效地阻碍DNA复制并减少细胞内dATP池。此外,TAS1553诱导凋亡,[1]使其在癌症研究中极具价值。 | |||
T12134 |
MYCMI-6
NSC354961 |
Apoptosis; c-Myc | Apoptosis; Cell Cycle/Checkpoint |
MYCMI-6 (NSC-354961) 是一种内源性MYC:MAX 蛋白相互作用抑制剂,选择性结合 MYC bHLHZip 域,Kd 值为 1.6 μM。它阻断 MYC 驱动的转录,以 MYC 依赖性的方式抑制肿瘤细胞的生长 ,诱导细胞凋亡。 | |||
TQ0081 |
JPH203
KYT-0353 |
Others | Others |
JPH203 (KYT-0353) 是一种 L 型氨基酸转运蛋白 1 (LAT-1) 的抑制剂,具有有效性和特异性。JPH203 可以抑制细胞对亮氨酸的摄取,抑制细胞增殖、诱导细胞凋亡,具有抗炎和抗肿瘤活性。 | |||
T9138 |
Indirubin-3′-oxime
Indirubin-3'-monoxime |
GSK-3; CDK; JNK | Cell Cycle/Checkpoint; MAPK; PI3K/Akt/mTOR signaling; Stem Cells |
Indirubin-3′-oxime 是一种有效的细胞周期蛋白依赖性蛋白激酶抑制剂,是 indirubin 的合成衍生物。它可通过激活软骨细胞中的 Wnt/β-catenin 信号来促进身高增长,可能在阿尔茨海默病的神经元凋亡中发挥作用。 | |||
T6763 |
Xevinapant
ARRY-334543,SM-406,AT406,Debio-1143 |
IAP | Apoptosis |
Xevinapant (Debio-1143) 是一种有效的 Smac 模拟物和 IAP 的拮抗剂,能够抑制 XIAP,cIAP1 和 cIAP2 蛋白,Ki 值分别为 66.4,1.9 和 5.1 nM。 | |||
T3211 |
Midostaurin
米哚妥林,N-Benzoylstaurosporine,PKC412,CGP41231,CGP 41251,苯甲酰基十字孢碱 |
Others; PKC | Chromatin/Epigenetic; Cytoskeletal Signaling; Others |
Midostaurin (PKC412) 是一种多靶点蛋白激酶抑制剂,有抗肿瘤活性,对 PKCα/β/γ、Syk、Flk-1、Akt、PKA、c-Kit、c-Fgr、c-Src、FLT3、PDFRβ和VEGFR1/2的IC50值范围为 22 到500 nM 之间。 | |||
T35528L |
TD52 dihydrochloride
TD52 dihydrochloride(1798328-24-1 Free base),TD52 2HCl |
Others | Others |
TD52 dihydrochloride (TD52 2HCl), a derivative of Erlotinib, is a potent and orally active inhibitor of protein phosphatase 2A (CIP2A). It exhibits strong anti-cancer properties by regulating the CIP2A/PP2A/p-Akt signaling pathway, resulting in the induction of apoptosis in triple-negative breast cancer (TNBC) cells. Mechanistically, TD52 dihydrochloride disrupts the binding of Elk1 to the CIP2A promoter, effectively reducing CIP2A levels. Notably, TD52 dihydrochloride demonstrates powerful anti... | |||
T16522 |
Phenoxodiol
脱氢雌马酚,Dehydroequol,Idronoxil,Haginin E |
Apoptosis; IAP; Caspase; Topoisomerase; p53 | Apoptosis; DNA Damage/DNA Repair; Proteases/Proteasome |
Phenoxodiol (Idronoxil) 是合成genestein 的类似物,激活线粒体caspase 系统,抑制XIAP,使癌细胞对fas 介导的凋亡敏感。它在细胞周期的G1/S 期诱导细胞周期阻滞,通过独立于p53的方式上调p21WAF1。它通过稳定可分裂复合物抑制DNA 拓扑异构酶II,从而阻止DNA 复制。 | |||
T16974 |
TAK-243
MLN7243 |
Apoptosis; E1/E2/E3 Enzyme; NF-κB | Apoptosis; NF-κB; Ubiquitination |
TAK-243 (MLN7243) 是一种泛素激活酶 UAE 的抑制剂 (IC50=1 nM),具有选择性。TAK-243 可阻断泛素结合,破坏单泛素信号传导以及整体蛋白质泛素化。TAK-243 具有抗肿瘤活性,可以促进细胞凋亡。 | |||
T77729 |
MY-1076
|
Apoptosis; YAP | Apoptosis; Stem Cells |
MY-1076 是一种高效的 YAP 抑制剂,具有抗胃癌活性。MY-1076 剂量依赖性诱导G2/M期阻滞,诱导 YAP 降解和细胞凋亡,抑制微管蛋白聚合。MY-1076 抑制 MGC-803、SGC-7901、HCT-116 和 KYSE450 细胞增殖。 | |||
T10406 |
Tuvusertib
M1774,ATR inhibitor 1 |
Apoptosis; ATM/ATR; Others; Chk | Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Others; PI3K/Akt/mTOR signaling |
Tuvusertib (M1774) 是一种可口服的共济失调毛细血管扩张和 Rad3相关(ATR)激酶抑制剂(Ki< 1 µΜ),具有选择性和潜在的抗肿瘤活性。Tuvusertib 选择性抑制 ATR 活性,阻断丝氨酸/苏氨酸蛋白激酶检查点激酶1 (CHK1)的下游磷酸化,从而抑制 DNA 损伤检查点激活,破坏 DNA 损伤修复,诱导肿瘤细胞凋亡。 | |||
T2170 |
SKF-96365 hydrochloride
1-[2-(4-甲氧基)-2-[3-(4-甲氧基苯基)丙氧基]乙基]咪唑,SKF96365 |
Apoptosis; Potassium Channel; Calcium Channel; TRP/TRPV Channel; Autophagy | Apoptosis; Autophagy; Membrane transporter/Ion channel; Metabolism |
SKF-96365 hydrochloride (SKF96365) 是store-operated Ca2+entry 抑制剂,也是TRP channel 阻滞剂。它显著抑制豚鼠离体心脏 hERG、hKCNQ1/hKCNE1、hKir2.1 和 hKv4.3 电流,延长QTc 间期。它通过诱导结直肠癌细胞的细胞周期阻滞和凋亡起抗肿瘤作用。 | |||
T11793 |
KY-05009
|
Wnt/beta-catenin | Cytoskeletal Signaling; Stem Cells |
KY-05009 是 ATP 竞争性的、有效的 TNIK 抑制剂,Ki 为 100 nM。KY-05009抑制人肺腺癌细胞中 TGF-β1 诱导的上皮-间质转化。KY-05009 还抑制TNIK 的蛋白表达和Wnt 靶基因的转录活性,并诱导癌细胞凋亡,显示抗癌活性。 | |||
T27417L |
Glutathione arsenoxide hydrochloride
GSAO HCl,Glutathione arsenoxide hydrochloride(1271726-51-2 Free base) |
Apoptosis; AChR | Apoptosis; Neuroscience |
Glutathione arsenoxide hydrochloride (Glutathione arsenoxide hydrochloride(1271726-51-2 Free base)) 是一种潜在的抗癌活性分子和肿瘤代谢抑制剂。Glutathione arsenoxide hydrochloride 靶向线粒体内膜腺嘌呤核苷酸转移酶 (ANT),对细胞增殖有抑制作用,促进细胞凋亡。Glutathione arsenoxide hydrochloride 可用于识别如蛋白质二硫异构酶一样的细胞表面蛋白质。 | |||
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。 | |||
T27078 |
CPUY201112
CPUY 201112,CPUY-201112 |
||
CPUY201112, a novel inhibitor of heat shock protein Hsp90, induces p53-mediated apoptosis in MCF-7 cells. | |||
T68468 |
FJ9
|
||
FJ9 is a FZD7 inhibitor which disrupts protein-protein interaction between Frz7 and the PDZ domain of DVL, and induces apoptosis in melanoma cell line and non-small cell lung cancer cell line. | |||
T26973 |
Cefatrizine
Cephatriazine,BL-S-640,BLS640,S 640P,BL S 640 |
||
Cefatrizine is an inhibitor of eukaryotic elongation factor-2 kinase, a unique calcium/calmodulin-dependent protein kinase, is well known to regulate apoptosis, autophagy and ER stress in many types of human cancers. | |||
T61719 |
DC-CPin711
|
||
DC-CPin711, a potent and selective inhibitor of the bromodomain of CREB-binding protein (CBP) with an IC50 of 0.0626 μM, effectively halts the cell cycle at the G1 phase and promotes apoptosis [1]. | |||
T40250 |
SHP2 protein degrader-1
SHP2 protein degrader-1 |
||
SHP2 protein degrader-1 is a highly efficient allosteric inhibitor targeting SHP2. It effectively induces degradation of SHP2 protein, resulting in cell apoptosis. This compound shows promising potential for studying diseases associated with SHP2. | |||
T14554 |
BI-0252
|
Others | Others |
BI-0252 is an inhibitor of MDM2-p53 (IC50:4 nM). BI-0252 can induce tumor regressions in all animals of a mouse SJSA-1 xenograft. And it concomitant induction of the tumor protein p53 (TP53) target genes and markers of apoptosis. | |||
T68262 | AEG40826 | ||
AEG40826 (HGS1029) is the hydrochloride salt of a small-molecule inhibitor of IAP (Inhibitor of Apoptosis Protein) family proteins with potential antineoplastic activity. IAP inhibitor HGS1029 selectively inhibits the biological activity of IAP proteins, which may restore apoptotic signaling pathways; this agent may work synergistically with cytotoxic drugs to overcome tumor cell resistance to apoptosis. IAPs are overexpressed by many cancer cell types, suppressing apoptosis by binding and inhib... | |||
T11739 |
K145
|
Others | Others |
K145 is inactive against SphK1 and other protein kinases. K145 induces cell apoptosis and has potently antitumor activity. K145 is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM. | |||
T40395 |
ζ-Stat trisodium
NSC37044 trisodium,ζ-Stat trisodium |
||
ζ-Stat trisodium (NSC37044 trisodium) is a potent and selective inhibitor of protein kinase C-ζ (PKC-ζ), exhibiting an IC50 of 5 μM. It effectively suppresses the proliferation of melanoma cell lines and promotes apoptosis. Moreover, ζ-Stat trisodium demonstrates notable antitumor activity in vitro. | |||
T36317 |
SM-1295
|
||
SM-1295 serves as an antagonist to the inhibitor of apoptosis protein (IAP), demonstrating dissociation constant (Kd) values of 3077 nM for XIAP-BIR3, 3.2 nM for c-IAP1-BIR3, and 9.5 nM for c-IAP2-BIR3, respectively[1][2]. | |||
T17545 | Biotin-BS | Others | Others |
Biotin-BS is a chemical compound composed of two distinct ligands: methyl-bestatin (MeBS) for cIAP1 and biotin. These ligands are interconnected through linkers. MeBS serves as a ligand specifically for the cellular inhibitor of apoptosis protein 1 (cIAP1) ubiquitin ligase[1]. | |||
T36201 |
AZD5582 dihydrochloride
AZD 5582 dihydrochloride |
||
Dimeric Smac mimetic; potent inhibitor of X-linked (XIAP) and cellular (cIAP) inhibitor of apoptosis protein (IC50 values are 15, 15 and 21 nM for XIAP, cIAP1 and cIAP2 respectively). Binds to the BIR3 domain of XIAP to prevent interaction with caspase-9. Causes degradation of cIAP1 and cIAP2 and induces apoptosis in MDA-MB-231 breast cancer cells. Causes tumor regression in MDA-MB-231 xenograft-bearing mice. Hennessy et al (2013) Discovery of a novel class of dimeric Smac mimetics as potent IAP... | |||
TP2292 |
survivin (baculoviral IAP repeat-containing protein 5) (21-28)
|
Others | Others |
Survivin (baculoviral inhibitor of apoptosis IAP repeat-containing protein-5) is a member of the IAP gene family, which has been implicated in both inhibitions of apoptosis and mitosis regulation1. Survivin is one of the most uniformly up-regulated genes | |||
T28038 |
Milademetan HCl (1398568-47-2 free base)
Milademetan HCl,DS3032,DS 3032,DS-3032,DS3032b,DS-3032b,DS 3032b |
||
Milademetan is a potent and selective MDM2 inhibitor. MDM2 inhibitor DS-3032b binds to and prevents the binding of MDM2 protein to the transcriptional activation domain of the tumor suppressor protein p53 upon oral administration. By preventing this MDM2-p53 interaction, the proteosome-mediated enzymatic degradation of p53 is inhibited and the transcriptional activity of p53 is restored. This results in the restoration of p53 signaling and leads to the p53-mediated induction of tumor cell apopto... | |||
T63969 |
SM-433
|
||
SM-433 是 Smac 模拟物,是凋亡抑制蛋白(IAPs)的抑制剂。SM-433 对 XIAP BIR3 蛋白具有较强的亲和力 (IC50<1 μM)。 | |||
T35542 |
LLP-3
|
||
Survivin (also known as baculoviral IAP repeat-containing protein 5 (BIRC5)) is a member of the inhibitor of apoptosis (IAP) family that interacts with and inhibits the apoptotic function of several proteins. LLP-3 is a cell-permeable ligand of Survivin that blocks its interaction with Ran, resulting in the induction of apoptosis (IAP) in glioma stem cells (IC50 = 31 μM). It abolishes the growth of glioblastoma multiforme cell in spheres and in tumor slice cultures. | |||
T75738 |
Microcystin-RR
|
||
Microcystin-RR (Cyanoviridin RR),一种有效的口服活性蛋白磷酸酶抑制剂,能诱导细胞凋亡和小鼠肝脏内质网应激。 | |||
T38753 |
CR-1-31-B
|
||
CR-1-31-B, a synthetic rocaglate, acts as a highly potent inhibitor of eIF4A. By disrupting the interaction between eIF4A and RNA, it effectively obstructs the initiation phase of protein synthesis. Specifically, CR-1-31-B interferes with the association between Plasmodium falciparum eIF4A (PfeIF4A) and RNA. Additionally, CR-1-31-B induces apoptosis in neuroblastoma and gallbladder cancer cells [4]. | |||
T71556 |
MK-1496
|
||
MK1496 is a n orally bioavailable Polo-like kinase 1 (Plk1) inhibitor with potential antineoplastic activity. Polo-like kinase 1 inhibitor MK1496 selectively inhibits Plk1, inducing selective G2/M arrest followed by apoptosis in a variety of tumor cells while causing reversible cell arrest at the G1 and G2 stage without apoptosis in normal cells. Plk1, named after the polo gene of Drosophila melanogaster, is a serine/threonine protein kinase involved in regulating mitotic spindle function in a n... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TN1651 |
Furanodiene
|
Apoptosis; PARP; Reactive Oxygen Species; Caspase; CDK; P-gp | Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; DNA Damage/DNA Repair; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience; NF-κB; Proteases/Proteasome |
Furanodiene 是从姜黄中提取的一种萜类天然产物,可抑制外排转运蛋白Pgp 功能并降低 Pgp 蛋白水平。它通过抗血管生成和诱导ROS 产生,DNA 链断裂和细胞凋亡发挥抗癌作用。 | |||
TN1305 |
Ethoxysanguinarine
乙氧基血根碱,6-Ethoxydihydrosanguinarine |
Apoptosis; AChR | Apoptosis; Neuroscience |
Ethoxysanguinarine (6-Ethoxydihydrosanguinarine) 是存在于龙葵中的一种苯并菲啶生物碱天然产物,通过抑制蛋白磷酸酶 2A,可抑制结直肠癌细胞活力,诱导细胞凋亡。 | |||
T5S0506 |
Rotundic acid
Rutundic acid,铁冬青酸 |
Apoptosis; Others; p38 MAPK; Akt; mTOR | Apoptosis; Cytoskeletal Signaling; MAPK; Others; PI3K/Akt/mTOR signaling |
Rotundic acid (Rutundic acid) 是一种从圆形肠球菌中获得的三萜类天然产物,具有抗炎和保护心脏的能力。它可通过 AKT/mTOR 和 MAPK 途径在肝细胞癌中诱导 DNA 损伤和细胞凋亡。 | |||
T3895 |
Polyphyllin I
重楼皂苷I,重楼皂甙 |
Apoptosis; Akt; JNK; PDK; mTOR; Autophagy | Apoptosis; Autophagy; Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling |
Polyphyllin I 是从七叶一枝花中提取的生物活性成分,具有很强的抗肿瘤活性。它是 JNK 信号通路的激活剂,也是 PDK1/Akt/mTOR 信号传导的抑制剂。它诱导自噬,G2/M 期阻滞和细胞凋亡。 | |||
TN4761 |
Phellamurin
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P-gp | Membrane transporter/Ion channel; Neuroscience |
Phellamurin 是一种来自黄檗叶的黄酮糖苷,可诱导细胞凋亡,具有抗肿瘤活性。它抑制肠道 P-糖蛋白,还抑制凤蝶的产卵。 | |||
T2851 |
Daphnetin
7,8-Dihydroxycoumarin,Daphnetol,瑞香素 |
EGFR; PKA; PKC; Parasite; Autophagy | Angiogenesis; Autophagy; Chromatin/Epigenetic; Cytoskeletal Signaling; JAK/STAT signaling; Microbiology/Virology; Tyrosine Kinase/Adaptors |
Daphnetin (7,8-Dihydroxycoumarin) 是从 Genus Daphne 中分离得到的香豆素衍生物,有抗氧化、抗炎、抗疟疾和解热作用,可用于凝血功能障碍、类风湿性关节炎等疾病的相关研究。 | |||
T2974 |
Cyclovirobuxine D
黄杨碱,CVB-D,Bebuxine,Cyclovirobuxin D,环维黄杨星D |
Apoptosis; Others; Akt; mTOR; Autophagy | Apoptosis; Autophagy; Cytoskeletal Signaling; Others; PI3K/Akt/mTOR signaling |
Cyclovirobuxine D (Bebuxine) 是中药黄杨的主要活性成分,可诱导自噬并减弱Akt 和mTOR 的磷酸化。它通过抑制细胞周期进程和诱导线粒体介导的细胞凋亡抑制癌细胞的增殖,有用于心肌梗死引起的心力衰竭的研究潜力。 | |||
T4034 |
Solamargine
Solamargin,δ-Solanigrine,澳洲茄边碱 |
Apoptosis; p38 MAPK; P-gp; STAT | Apoptosis; JAK/STAT signaling; MAPK; Membrane transporter/Ion channel; Neuroscience; Stem Cells |
Solamargine (δ-Solanigrine) 是一种来源于茄属植物的类固醇 Solasodine 的衍生物,诱导非选择性细胞毒性和 P-gp 抑制作用。它通过下调 MMP-2 和 MMP-9 的表达和活性来显著抑制 HepG2 细胞的迁移和侵袭,在多种癌症中均表现出抗癌活性。 | |||
T2P2806 |
Hederacolchiside A1
黑海常春藤苷A1,革叶常春藤皂苷 A1,Raddeanoside R13 |
Apoptosis; ERK; MEK; Akt; PI3K; Parasite; mTOR | Apoptosis; Cytoskeletal Signaling; MAPK; Microbiology/Virology; PI3K/Akt/mTOR signaling |
Hederacolchiside A1 (Raddeanoside R13) 是从白头翁中分离的一种有抗利什曼原虫和抗肿瘤增殖活性的天然产物。 | |||
T4085 |
Paris saponin VII
重楼皂苷 VII,Chonglou Saponin VII,Polyphyllin-VII,Dioscinin,Paris saponin-VII |
Apoptosis; BCL; Others; PARP; p38 MAPK; Akt; Caspase; P-gp; Autophagy | Apoptosis; Autophagy; Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair; MAPK; Membrane transporter/Ion channel; Neuroscience; Others; PI3K/Akt/mTOR signaling; Proteases/Proteasome |
Paris saponin VII (Dioscini) 是从延龄草的根和根茎中分离的一种甾体皂苷。它减弱线粒体膜电位,增加凋亡相关蛋白的表达,并降低Bcl-2、caspase-9、caspase-3、PARP-1和p-Akt 的蛋白表达水平。它在 K562/ADR 细胞中诱导强烈的自噬,可研究白血病。 | |||
T2799 |
(20S)-Protopanaxadiol
20-Epiprotopanaxadiol,20(S)-APPD,20 (S)-原人参二醇,原人参二醇 |
Apoptosis; Reactive Oxygen Species; P-gp | Apoptosis; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience; NF-κB |
(20S)-Protopanaxadiol (20-Epiprotopanaxadiol) 是人参皂甙的代谢产物,是一种凋亡诱导剂,抑制Akt 活性并诱导多种肿瘤细胞凋亡。 | |||
TN2190 |
Scoulerine
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Apoptosis; Beta-Secretase; BACE; Parasite | Apoptosis; Microbiology/Virology; Neuroscience |
Scoulerine 是抗有丝分裂化合物。它抑制细胞增殖,阻止细胞周期,并诱导癌细胞凋亡。它也是BACE1(淀粉样前体蛋白裂解酶 1) 的抑制剂。 | |||
T3884 |
Neoandrographolide
Neoandrographiside,新穿心莲内酯 |
NOS; COX | Immunology/Inflammation; Neuroscience |
Neoandrographolide (Neoandrographiside) 是一种二萜类化合物,从穿心莲中分离得到。 | |||
T30969 |
Clitocine
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Apoptosis; BCL | Apoptosis |
Clitocine 是一种来从蘑菇中提取的一种腺苷类似物,是一种有效的转录通读剂,是一种无义突变的抑制剂,具有抗癌活性,可诱导携带 p53 无义突变等位基因的细胞产生 p53 蛋白。Clitocine 通过促进 Mcl-1 降解来增强 TRAIL 介导的人结肠癌细胞凋亡。 | |||
T1020 |
Doxorubicin hydrochloride
Adriamycin,Doxorubicin (Adriamycin) HCl,Hydroxydaunorubicin hydrochloride,盐酸多柔比星,盐酸阿霉素,NSC 123127 |
Apoptosis; Mitophagy; HBV; HIV Protease; Topoisomerase; Antibacterial; Antibiotic; AMPK; Autophagy | Apoptosis; Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair; Microbiology/Virology; PI3K/Akt/mTOR signaling; Proteases/Proteasome |
Doxorubicin hydrochloride (Adriamycin) 属于蒽环类抗生素,是人类 DNA 拓扑异构酶 I/II 抑制剂 (IC50=0.8/2.67 μM)。Doxorubicin hydrochloride 具有细胞毒性和抗肿瘤活性。Doxorubicin hydrochloride 可降低 AMPK 及其下游靶蛋白乙酰辅酶 A 羧化酶的磷酸化,还可诱导凋亡和自噬。 | |||
T4S0498 |
Glaucocalyxin A
蓝萼甲素,Wangzaozin B,Leukamenin F |
Apoptosis; Akt; Caspase; PI3K | Apoptosis; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Proteases/Proteasome |
Glaucocalyxin A (Leukamenin F) 是来自日本黑纹病菌的一种对映型月桂基二萜,具有抗肿瘤作用。它通过调节PI3K/Akt 信号通路抑制 GLI1 的核易位,诱导骨肉瘤凋亡。 | |||
T1719 |
Bufalin
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ATPase | Membrane transporter/Ion channel |
Bufalin 是蟾酥中的一种成分,是Na+/K+-ATPase 抑制剂,具有抗肿瘤活性,可与其基 α1、α2 和 α3 结合,Kd 值分别为 42.5、45 和 40 nM。 | |||
TN5171 |
Tricetin
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Apoptosis; Others; Nrf2 | Apoptosis; Immunology/Inflammation; Others |
Tricetin 是一种从石榴中分离出的类黄酮。Tricetin 是 Keap1-Nrf2 蛋白相互作用(PPI)的强效竞争性抑制剂,通过激活 Nrf2/HO-1 信号通路和阻止线粒体依赖性细胞凋亡通路,保护帕金森病患免受 6-OHDA 诱导的神经毒性的影响。Tricetin 通过 Akt/GSK-1β途径抑制鼻咽癌的迁移和指示性蛋白酶早老素-1(PS-1)表达。Tricetin 抑制由Egr-1介导的氧化LDL 诱导的内皮炎症,保护大鼠软骨细胞免受IL-1β诱导的炎症和细胞凋亡。 | |||
T16011 |
Manumycin A
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Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
Manumycin A is an antibiotic. Manumycin A induces apoptosis and exerts antitumor activity. Manumycin A inhibits exosome biogenesis and secretion via targeted inhibition of Ras/Raf/ERK1/2 signaling. Manumycin A acts as a selective, competitive inhibitor of | |||
T16381 |
Okadaic acid
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Others | Others |
Okadaic acid is a non-comepetitive, selective and reversible serine/threonine-specific protein phosphatases 1 (PP1), PP2A, and PP3 inhibitor (IC50s: 10-15 nM, 0.5 nM, and 4 nM, respectively). Okadaic acid is extracted from black sponges of the genus Halic | |||
T73876 |
Sanggenon G
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Sanggenon G 是一种具有细胞渗透性的有效的 X 连锁凋亡抑制蛋白 (XIAP) 抑制剂。Sanggenon G 特异性结合XIAP 的 BIR3 结构域,结合亲和力为 34.26 μM。Sanggenon G 增强caspase 激活。 | |||
T37055 |
Cytostatin
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Cytostatin is a natural antitumor inhibitor of cell adhesion to extracellular matrix, blocking adhesion of B16 melanoma cells to laminin and collagen type IV in vitro (IC50s = 1.3 and 1.4 μg/ml, respectively) and B16 cells metastatic activity in mice. It induces apoptosis of FS3 mouse fibrosarcoma cells (IC50 = 3.1 μg/ml). Cytostatin potently and selectively inhibits protein phosphatase 2A (PP2A; IC50 = 29 nM against the catalytic subunit), while having no effect against PP1, PP2B, or PP5. | |||
TN1440 |
Beta-Hydroxyisovalerylshikonin
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EGFR; Tyrosine Kinases; Prostaglandin Receptor; Src; AMPK; Fatty Acid Synthase | Angiogenesis; Chromatin/Epigenetic; GPCR/G Protein; Immunology/Inflammation; JAK/STAT signaling; Metabolism; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
Beta-hydroxyisovalerylshikonin 是分离自Lithospermium radix 的天然产物,具有抑制PTK 的作用, 对 EGFR 和 v-Src 受体作用的IC50分别为 0.7 μM 和 1 μM。它对多种肿瘤细胞系均有抑制作用,可以高效诱导 NCI-H522 和 DMS114 细胞的死亡。 | |||
TN4300 |
Isojacareubin
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MAPK; PKC; Antifection | Chromatin/Epigenetic; Cytoskeletal Signaling; MAPK; Microbiology/Virology |
Isojacareubin displays potent activity against H. pylori HP40 clinical isolate with MIC 23.9 uM, which is approximately two times greater than that of the standard drug amoxicillin. Isojacareubin is a potent inhibitor of protein kinase C (PKC), suppresses | |||
T35577 |
Phosphatidylserines (bovine)
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Phosphatidylserine is a naturally occurring phospholipid that comprises 2-10% of total phospholipids in mammals and is enriched in the central nervous system, particularly the retina. It is anionic and found mainly on the inner leaflet of the cell membrane. It is biosynthesized from phosphatidylcholine or phosphatidylethanolamine by phosphatidyl synthase 1 (PSS1) or PSS2, respectively, in the endoplasmic reticulum and can be reversibly converted back by the same enzymes. It can also be irreversi... |