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抑制剂 & 化合物

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Cat. No. Product Name Target Signaling Pathways
T2490 Osimertinib

AZD-9291,Mereletinib,奥希替尼

EGFR Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
Osimertinib (AZD-9291) 是一种 EGFR 三代抑制剂,抑制二代 EGFR 抑制剂产生的 T790M 耐药突变,具有不可逆性和口服活性。Osimertinib 具有抗肿瘤活性,用于治疗 EGFR 突变的非小细胞肺癌。
T3634 Osimertinib mesylate

甲磺酸奥希替尼,Mereletinib mesylate,奥希替尼甲磺酸盐,AZD-9291 mesylate

EGFR Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
Osimertinib mesylate (Mereletinib mesylate) 是一种不可逆的突变选择性 EGFR 抑制剂,对EGFRL858R 和EGFRL858R/T790M 的IC50值分别为 12 和 1 nM。
T70353 JG-231

HSP Cytoskeletal Signaling; Metabolism
JG-231 是 JG-98 类似物,具有抗癌活性。JG-231 对三阴性乳腺癌 (TNBC) 的 MDA-MB-231 异植肿瘤模型具有抑制作用。JG-231 可抑制 Hsp70-BAG3 的相互作用。JG-231 对三阴性乳腺癌 (TNBC) 的 MDA-MB-231 异植肿瘤模型具有抑制作用。
T6810 CPI-360

Synonym 2,CPI 360,CPI360

Apoptosis; Histone Methyltransferase Apoptosis; Chromatin/Epigenetic
CPI-360是一种小分子EZH2抑制剂(IC50:0.002 μM,EC50: 0.080μM),在EZH200依赖性肿瘤异种移植模型中显示出抗肿瘤活性。
T9588 JI130

Others Others
JI130 能够削弱 Hes1 抑制转录的能力。 JI130 治疗显著减少了小鼠胰腺肿瘤异种移植模型中的肿瘤体积。
T64357 FA16

FA 16,FA-16

Ferroptosis Apoptosis
FA16 是一种选择性、代谢稳定的铁死亡 (ferroptosis) 诱导剂 ,IC50 值为1.26 μM。FA16 是 2-(三氟甲基) 苯并咪唑的衍生物。FA16 对胱氨酸/谷氨酸反转运蛋白 (system Xc-) 介导了细胞内谷氨酸和细胞外胱氨酸的交换有抑制作用。FA16 在 HepG2 异种移植瘤模型中显著抑制肿瘤生长。
T5405 BI-1347

CDK Cell Cycle/Checkpoint
BI-1347 是一种有效的、选择性的 CDK8/cyclinC 抑制剂,IC50值为 1 nM,可抑制肿瘤生存。
T8973 HS-1793

Others Others
HS-1793 是 resveratrol 类似物,可以诱导细胞凋亡,在多种癌细胞中有抗肿瘤的能力。
T3633 Crenigacestat

LY3039478

Gamma-secretase Neuroscience; Proteases/Proteasome; Stem Cells
Crenigacestat (LY3039478) 是一种口服具有活性的Notch 和γ-secretase 的抑制剂,其在多种肿瘤细胞中的IC50为 ∼1nM。
T7214 TEPP-46

ML265

PKM Metabolism
TEPP-46 (ML265) 是选择性的丙酮酸激酶 M2 (pyruvate kinase M2; PKM2) 激活剂,AC50=92 nM,对 PKM1,PKL 和 PKR 作用较小或没有作用。
T60187 RP-6685

DNA/RNA Synthesis Cell Cycle/Checkpoint; DNA Damage/DNA Repair
RP-6685, a highly potent and selective inhibitor of DNA polymerase theta (Polθ), manifests remarkable oral activity. With an IC 50 value of 5.8 nM in the PicoGreen assay, RP-6685 effectively hinders the enzymatic activity of Polθ. In addition, it demonstrates significant antitumor efficacy as observed in a mouse tumor xenograft model [1].
T60148 MSC-4106

YAP Stem Cells
MSC-4106 是一种有效的、具有口服活性的 YAP/TAZ-TEAD 抑制剂。 MSC-4106 阻断 TEAD1 和 TEAD3 的自棕榈酰化,并且对 NCI-H226 异种移植瘤模型显示抑制作用。
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。
T27011 CHMFL-FLT3-122

CHMFLFLT3122,CHMFL FLT3 122

FLT Angiogenesis; Tyrosine Kinase/Adaptors
CHMFL-FLT3-122 是一种强效口服 FLT3 激酶抑制剂,用于治疗 FLT3-ITD 阳性急性髓性白血病。CHMFL-FLT3-122能显著抑制 MV4-11细胞异种移植模型(50 mg/kg)的肿瘤生长,且在体内无明显毒性。
T39954 AU-15330

Epigenetic Reader Domain; PROTACs Chromatin/Epigenetic; PROTAC
AU-15330是SWI/SNF ATPase亚基SMARCA2和SMARCA4的蛋白水解靶向嵌合体(PROTAC)降解剂。AU-15330 能有效抑制肿瘤在前列腺癌异种移植模型中的生长,并与 AR 拮抗剂恩杂鲁胺具有协同作用。AU-15330在去势抵抗性前列腺癌(CRPC)模型中显示出部分治疗效果和AU-15330具有无毒性的特点。
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...
T14214 AMG 511

PI3K PI3K/Akt/mTOR signaling
AMG 511 是一种高效的、口服有效的 I 类 pan-PI3K 抑制剂,对 PI3Kα, β, δ 和 γ 作用的 Ki 值分别为 4 nM, 6 nM, 2 nM 和 1 nM。它它显著抑制了 PI3K 信号,减少 p-Akt (Ser473)。它在小鼠胶质母细胞瘤移植瘤模型中具有抗肿瘤作用。
T35666 PRGL493

Others Others
PRGL493为高效、选择性的长链酰基辅酶a合成酶4 (ACSL4) 抑制剂,能在乳腺和前列腺细胞以及动物模型中抑制细胞增殖和肿瘤生长,主要应用于癌症研究。
T69529 BI-0474

Ras GPCR/G Protein; MAPK
BI-0474 是一种高效的 KRASG12C 抑制剂,对 GDP-KRAS:SOS1 蛋白-蛋白相互作用具有抑制作用,IC50 值为 7.0 nM。BI-0474 对携带 G12C 突变的 NCI-H358 细胞具有显著的抗增殖活性,在非小细胞肺癌异种移植模型中显示出显著的抗肿瘤活性。BI-0474 可用于研究癌症。
T60202 MMRi62

7-[(2,3-dichlorophenyl)-(pyridin-2-ylamino)methyl]quinolin-8-ol

Ferroptosis Apoptosis
MMRi62 (7-[(2,3-dichlorophenyl)-(pyridin-2-ylamino)methyl]quinolin-8-ol) 是一种铁死亡 (ferroptosis) 诱导剂,靶向 MDM2-MDM4 (抑癌基因 p53 负调控因子)。MMRi62 对胰腺导管腺癌 (PDAC) 细胞显示出 p53 独立的促凋亡 (apoptosis) 活性,并诱导其自噬 (autophagy)。MMRi62 诱导铁死亡,伴随着活性氧增加和铁蛋白重链 (FTH1) 溶酶体降解。MMRi62 还可导致突变型 p53 的蛋白酶体降解,并对具有 KRAS 和 TP53 高频突变特征的原位异种移植 PDAC 小鼠模型具有体内药效。
T12009 Telomerase-IN-1

Telomerase DNA Damage/DNA Repair
Telomease-IN-1是一种端粒酶抑制剂(IC50:0.19μM)。Telomease-IN-1通过ER 过度反应(EOR)的内质网应激(ERS)激活hTERT 的表达,然后诱导ERS,导致细胞凋亡。Telomease-IN-1通过表达下游信号分子包括CHOP(CAAT /增强子结合蛋白同源蛋白))和线粒体凋亡途径,导致细胞增殖受到抑制。Telomease-IN-1对端粒酶具有较高的抑制活性,对SMMC-7721细胞具有较高的抗增殖能力,对人正常肝细胞无明显毒性作用。Telomease-IN-1 在异种移植肿瘤模型表现出抗肿瘤活性。
T36674 DMU-212

Apoptosis; ERK Apoptosis; MAPK
DMU-212 是具有口服活性的白藜芦醇的甲基化衍生物,表现出抗分裂、抗增殖、抗氧化和促进细胞凋亡的活性。它通过诱导凋亡和激活ERK1/2蛋白阻止有丝分裂。
T28458 PS432

PS-432,PS 432

PS432 is an allosteric inhibitor of atypical PKCs. PS432 targets the PIF-pocket resulting in significantly reduce tumor growth without side effects in mouse xenograft model.
T29941 AM-6826

AM 6826

AM-6826 is a Pan-Pim inhibitor. In a mouse xenograft tumor model, AM-6826 can inhibit the growth of KMS-12-BM melanoma by 93%.
T69839 RK-582

RK-582 is an orally efficacious spiroindolinone-based tankyrase inhibitor for the treatment of colon cancer. It exhibits a markedly improved robust tumor growth inhibition in a COLO-320DM mouse xenograft model when orally administered.
T37098 Chk1-IN-5

Chk1-IN-5

Chk1-IN-5 is a highly effective inhibitor of checkpoint kinase 1 (Chk1), which hinders the phosphorylation of Chk1 and effectively suppresses tumor growth in a colon cancer xenograft model[1].
T70754 NMS-P953

NMS-P953 is a JAK2 inhibitor, displaying significant tumor growth inhibition in SET-​2 xenograft tumor model. NMS-P953 has a mechanism of action confirmed in vivo by typical modulation of known biomarkers, and with a favorable pharmacokinetic and safety profile.
T35480 dBRD9-A

dBRD9-A

Potent BRD9 degrader. Selectively binds BRD9 and elicits near complete degradation of BRD9 at nanomolar concentrations. Inhibits growth of synovial sarcoma cells in vitro and tumor progression in a synovial sarcoma xenograft mouse model.
T70677 PLS-123

PLS-123 is a novel covalent irreversible Btk inhibitor with potential anti-proliferative activity. PLS-123 exhibited more potent anti-proliferative effects than ibrutinib in multiple cellular and in vivo preclinical models of B-cell lineage malignancy, including 14 kinds of cell lines, patients’ primary tumor cells and mouse xenograft model.
T39853 ARD-61

ARD-61 is a potent and specific PROTAC androgen receptor (AR) degrader, exhibiting high effectiveness. It effectively induces the degradation of AR and progesterone receptors (PR) in AR+ cancer cell lines, leading to apoptosis. Additionally, ARD-61 demonstrates significant tumor growth inhibition in the MDA-MB-453 xenograft model in mice.
T61806 Antitumor agent-44

Antitumor agent-44 (Compound 5n) elicits potent antitumor effects by inducing disruption of mitochondrial homeostasis, cell cycle arrest, and apoptosis in human adenocarcinoma cells. Moreover, Antitumor agent-44 demonstrates significant anti-tumor activity in a lung cancer cell xenograft mice model [1].
T34582 SC-III3

SC-III3 is a novel scopoletin derivative, induces autophagy of human hepatoma HepG2 cells through AMPK/mTOR signaling pathway by acting on mitochondria. SC-III3 reduces the viability of HepG2 cells and tumor growth of HepG2 xenograft mouse model. It induc
TP2001 MM 54

Potent apelin receptor antagonist (Ki = 82 nM; IC50 = 93 nM). Antagonizes the inhibitory affect of [Pyr1]-Apelin-13 on forskolin-induced cAMP accumulation in CHO-K1-APJ cells. Recuces tumor expansion and lengthens survival time in a mouse xenograft model
T37222 GLS1 Inhibitor

GLS1 inhibitor is an inhibitor of glutaminase 1 (GLS1; IC50= 0.021 μM).1It inhibits the growth of NCI H1703 non-small cell lung cancer (NSCLC) cellsin vitro(GI50= 0.011 μM). GLS1 inhibitor (100 mg/kg) reduces tumor growth, increases tumor levels of glutamine, and decreases tumor levels of glutamate and aspartate in an NCI H1703 mouse xenograft model. 1.Finlay, M.R.V., Anderton, M., Bailey, A., et al.Discovery of a thiadiazole-pyridazine-based allosteric glutaminase 1 inhibitor series that demons...
T79347 Anticancer agent 146

Necroptosis Apoptosis
Anticanceragent 146(compound 1.19)是一种诱导坏死(Necroptosis)的化合物,它在小鼠MDA-MB-231异种移植模型中显示出抗肿瘤活性。
T79096 IPG7236

CCR Immunology/Inflammation; Microbiology/Virology
IPG7236为选择性CCR8拮抗剂,于人乳腺癌小鼠异种移植模型中展现显著肿瘤抑制效果,适用于癌症研究。
T78177 CCT374705

CCT374705为口服活性BCL6抑制剂,体外显示出显著的抗增殖效果,并在淋巴瘤异种移植小鼠模型中有效地抑制了肿瘤生长。
T62559 TGFβRI-IN-4

TGFβRI-IN-4 是一种高效的、口服具有活力的 TGFβ 受体 I 型激酶 (TGFβRI) 抑制剂,能够作用于 ALK5 (IC50: 44 nM) 和 NIH3T3 (IC50: 42.5 nM)。TGFβRI-IN-4 在异种移植瘤模型中,能够抑制肿瘤生长和肿瘤重量。
T63320 Axl-IN-6

Axl-IN-6 是口服具有活性的 AXL 抑制剂。Axl-IN-6 在 MV-4-11 皮下异种移植瘤模型中,表现出良好的耐受性,并且能够显著的抑制肿瘤生长。
T63671 Anticancer agent 60

Anticancer agent 60 对人 HepG2 细胞具有抗增殖效果,其 IC50 值为 4.13 μM。在人 HepG2 异种移植小鼠模型中,Anticancer agent 60 表现出抗肿瘤活性。
T36108 YW3-56 (hydrochloride) (technical grade)

YW3-56 (hydrochloride) (technical grade)

YW3-56 is an inhibitor of protein arginine deiminase 2 (PAD2) and PAD4 (IC50s = 0.5-1 and 1-5 μM, respectively).1It inhibits the growth of U2OS osteosarcoma cells (IC50= ~2.5 μM) in a p53-dependent mannerviainduction of SESN2 and subsequent inhibition of mTORC1. YW3-56 (10 mg/kg) reduces tumor growth in an S-180 murine sarcoma tumor model. It also inhibits tumor growth in the 1883 MDA-MB-231 breast cancer bone metastasis mouse xenograft model.2 1.Wang, Y., Li, P., Wang, S., et al.Anticancer pept...
T78676 ERα degrader 6

Estrogen Receptor/ERR Endocrinology/Hormones
ERα degrader6(Compound 31q)是一种ERα降解剂,其KI值为75 nM。该化合物还能以IC50 37.7 nM的浓度抑制ARO。ERα degrader6在MCF-7肿瘤异种移植模型中抑制肿瘤生长,可用于乳腺癌研究。
T71783 Oxythiamine chloride HCl

Oxythiamine chloride HCl is a thiamine antimetabolite that has anticancer activities. It is converted by thiamine pyrophosphokinase to oxythiamine pyrophosphate, a transketolase inhibitor. Oxythiamine decreases transketolase activity in breast cancer. It inhibits the nonoxidative synthesis of ribose and decreases RNA and DNA synthesis in pancreatic cancer. In vivo, oxythiamine induces cell cycle arrest at the G1 phase and apoptosis in an adenocarcinoma model. Oxythiamine, in combination with sor...
T70344 BJ-2302

BJ-2302 is a SRC inhibitor. BJ-2302 effectively suppressed MDA-MB-231 cell invasion (Matrigel invasion assay) and metastasis (chorioallantoic membrane assay xenografted with MDA-MB-231-luc2-tdTomato cancer cells). Additionally, BJ-2302 (1 mg/kg) strongly suppressed TNBC cell proliferation in vitro and tumor growth in a xenograft mouse tumor model. The anti-metastatic and anti-tumor effects of BJ-2302 were superior to those of Z-FL-COCHO (1 mg/kg) or batimastat (30 mg/kg), a pan-MMP inhibitor.
T68400 STA-9584

STA-9584 is a potent vascular disrupting agent, which exhibits potent antitumor activity by selectively targeting microvasculature at both the center and periphery of tumors. In vitro, 2-methoxy-5-(5-(3,4,5-trimethoxyphenyl)isoxazol-4-yl)aniline (STA-9122) (active metabolite of STA-9584 ) displayed increased potency relative to other tubulin-binding agents and was highly cytotoxic to tumor cells. STA-9584 induced significant tumor regressions in prostate and breast xenograft models in vivo and, ...
T68788 Ellipticine quinone

Ellipticine quinone, also known as NSC-383230, is a Drp1 inhibitor. rpitor1 and Drpitor1a inhibited the GTPase activity of Drp1 without inhibiting the GTPase of dynamin 1. Ellipticine quinone showed greater potency than the current std. Drp1 GTPase inhibitor, mdivi-​1, (IC50 for mitochondrial fragmentation are (0.06, and 10 μM, resp.)​. Ellipticine quinone suppressed lung cancer tumor growth in a mouse xenograft model. Ellipticine quinone also inhibited mitochondrial ROS prodn., prevented mi...
T79261 P-gp inhibitor 15

P-gp inhibitor 15 (compound 7a) 是一种Pgp-非底物抑制剂,能够抑制Pgp-ATP酶的活性并干扰罗丹明123的Pgp介导外流。此外,P-gp inhibitor 15能增强紫杉醇的抗肿瘤效果,有效抑制裸鼠KBV异种移植肿瘤模型的肿瘤生长。
T79112 CDK4/6-IN-17

CDK Cell Cycle/Checkpoint
CDK4/6-IN-17(compound 12)为具有口服活性的CDK4/6抑制剂,在BE(2)细胞的IC50为10-100 nM。CDK4/6-IN-17在COLO205异种移植模型中有效抑制肿瘤生长。
T71947 SGK1 inhibitor

SGK1 inhibitor is an inhibitor of serum- and glucocorticoid-regulated kinase 1 (SGK1) and SGK2. It is selective for SGK1 and SGK2 over SGK3 in the presence of a high concentration of ATP. SGK1 inhibitor prevents phosphorylation of GSK3β in U2OS cells and decreases cell viability in BYL719-insensitive HCC1954 cells when used in combination with the PI3Kα inhibitor BYL719. SGK1 inhibitor reduces tumor growth in an HCC1954 mouse xenograft model when administered in combination with BYL719.
T63654 OTS186935 hydrochloride

OTS186935 hydrochloride 是蛋白甲基转移酶 SUV39H2 的有效抑制剂 (IC50: 6.49 nM)。OTS186935 hydrochloride 在小鼠异种移植模型中,能够明显抑制肿瘤生长,且没有明显毒性。OTS193320 hydrochloride 能够调节癌细胞中 γ-H2AX 的产生。

化合物

Osimertinib
Cat.No: T2490
Synonym: AZD-9291,Mereletinib,奥希替尼
Target: EGFR
Osimertinib mesylate
Cat.No: T3634
Synonym: 甲磺酸奥希替尼,Mereletinib mesylate,奥希替尼甲磺酸盐,AZD-9291 mesylate
Target: EGFR
JG-231
Cat.No: T70353
Synonym:
Target: HSP
CPI-360
Cat.No: T6810
Synonym: Synonym 2,CPI 360,CPI360
Target: Apoptosis, Histone Methyltransferase
JI130
Cat.No: T9588
Synonym:
Target: Others
FA16
Cat.No: T64357
Synonym: FA 16,FA-16
Target: Ferroptosis
BI-1347
Cat.No: T5405
Synonym:
Target: CDK
HS-1793
Cat.No: T8973
Synonym:
Target: Others
Crenigacestat
Cat.No: T3633
Synonym: LY3039478
Target: Gamma-secretase
TEPP-46
Cat.No: T7214
Synonym: ML265
Target: PKM
RP-6685
Cat.No: T60187
Synonym:
Target: DNA/RNA Synthesis
MSC-4106
Cat.No: T60148
Synonym:
Target: YAP
MYCMI-6
Cat.No: T12134
Synonym: NSC354961
Target: Apoptosis, c-Myc
CHMFL-FLT3-122
Cat.No: T27011
Synonym: CHMFLFLT3122,CHMFL FLT3 122
Target: FLT
AU-15330
Cat.No: T39954
Synonym:
Target: Epigenetic Reader Domain, PROTACs
MDL-800
Cat.No: T64529
Synonym: MDL 800,MDL800
Target: Sirtuin
AMG 511
Cat.No: T14214
Synonym:
Target: PI3K
PRGL493
Cat.No: T35666
Synonym:
Target: Others
BI-0474
Cat.No: T69529
Synonym:
Target: Ras
MMRi62
Cat.No: T60202
Synonym: 7-[(2,3-dichlorophenyl)-(pyridin-2-ylamino)methyl]quinolin-8-ol
Target: Ferroptosis
Telomerase-IN-1
Cat.No: T12009
Synonym:
Target: Telomerase
DMU-212
Cat.No: T36674
Synonym:
Target: Apoptosis, ERK
PS432
Cat.No: T28458
Synonym: PS-432,PS 432
Target:
AM-6826
Cat.No: T29941
Synonym: AM 6826
Target:
RK-582
Cat.No: T69839
Synonym:
Target:
Chk1-IN-5
Cat.No: T37098
Synonym: Chk1-IN-5
Target:
NMS-P953
Cat.No: T70754
Synonym:
Target:
dBRD9-A
Cat.No: T35480
Synonym: dBRD9-A
Target:
PLS-123
Cat.No: T70677
Synonym:
Target:
ARD-61
Cat.No: T39853
Synonym:
Target:
Antitumor agent-44
Cat.No: T61806
Synonym:
Target:
SC-III3
Cat.No: T34582
Synonym:
Target:
MM 54
Cat.No: TP2001
Synonym:
Target:
GLS1 Inhibitor
Cat.No: T37222
Synonym:
Target:
Anticancer agent 146
Cat.No: T79347
Synonym:
Target: Necroptosis
IPG7236
Cat.No: T79096
Synonym:
Target: CCR
CCT374705
Cat.No: T78177
Synonym:
Target:
TGFβRI-IN-4
Cat.No: T62559
Synonym:
Target:
Axl-IN-6
Cat.No: T63320
Synonym:
Target:
Anticancer agent 60
Cat.No: T63671
Synonym:
Target:
YW3-56 (hydrochloride) (technical grade)
Cat.No: T36108
Synonym: YW3-56 (hydrochloride) (technical grade)
Target:
ERα degrader 6
Cat.No: T78676
Synonym:
Target: Estrogen Receptor/ERR
Oxythiamine chloride HCl
Cat.No: T71783
Synonym:
Target:
BJ-2302
Cat.No: T70344
Synonym:
Target:
STA-9584
Cat.No: T68400
Synonym:
Target:
Ellipticine quinone
Cat.No: T68788
Synonym:
Target:
P-gp inhibitor 15
Cat.No: T79261
Synonym:
Target:
CDK4/6-IN-17
Cat.No: T79112
Synonym:
Target: CDK
SGK1 inhibitor
Cat.No: T71947
Synonym:
Target:
OTS186935 hydrochloride
Cat.No: T63654
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T79971 Asparanin A

Apoptosis Apoptosis
Asparanin A 是一种具有抗癌活性的凋亡 (apoptosis) 诱导剂。它能够通过线粒体和 PI3K/AKT 信号通路使细胞周期在 G0/G1 期停滞,并有效抑制癌细胞生长。此外,Asparanin A 在小鼠Ishikawa子宫内膜癌异种移植模型中显示出显著的体内抑制肿瘤生长效力。
T36179 Aspulvinone O

Aspulvinone O is a fungal metabolite that has been found in P. variotti and has antioxidant and anticancer activities.1,2 It scavenges 2,2-diphenyl-1-picrylhydrazyl radicals in a cell-free assay (IC50 = 11.6 μM).1 Aspulvinone O inhibits aspartate transaminase 1 (GOT1; Kd = 3.32 μM) and is cytotoxic to PANC-1, AsPC-1, and SW1990 pancreatic cancer cells (IC50s = 20.54-26.8 μM).2 It reduces the oxygen consumption rate (OCR) and induces apoptosis in SW1990 cells. Aspulvinone O (2.5 and 5 mg/kg) redu...
TN3084 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone

Estrogen Receptor/ERR; Others Endocrinology/Hormones; Others
5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone 具有抗癌活性,体外对 ER 阳性乳腺癌MCF-7细胞表现出较强的抗增殖作用,对MCF-7细胞的IC50值为4.41 uM。5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone 能显著下调雌激素受体-α (ER-α)的表达浓度,并能抑制人乳腺癌细胞系BCAP-37异种移植模型体内的肿瘤生长。
T36954 Nemorosone

Nemorosone is a polycyclic polyprenylated acylphloroglucinol (PPAP) originally isolated from C. rosea that has antiproliferative properties.1 Nemorosone inhibits growth of NB69, Kelly, SK-N-AS, and LAN-1 neuroblastoma cells (IC50s = 3.1-6.3 μM), including several drug-resistant clones, but not MRC-5 human embryonic fibroblasts (IC50 = >40 μM).2 It increases DNA fragmentation in LAN-1 cells in a dose-dependent manner, and decreases N-Myc protein levels and phosphorylation of ERK1/2 by MEK1/2. Nem...

天然产物

Asparanin A
Cat.No: T79971
Synonym:
Target: Apoptosis
Aspulvinone O
Cat.No: T36179
Synonym:
Target:
5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone
Cat.No: TN3084
Synonym:
Target: Estrogen Receptor/ERR, Others
Nemorosone
Cat.No: T36954
Synonym:
Target:
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