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26

抑制剂 & 化合物

7

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T16961	Supinoxin RX-5902	Apoptosis; DNA/RNA Synthesis	Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	Supinoxin (RX-5902) 是磷酸化 p68 RNA 解旋酶的强效口服活性抑制剂，是一种抗肿瘤试剂。它与 Y593 磷酸化的 p68 相互作用并减弱 β-catenin 的核穿梭性。它诱导细胞凋亡并抑制 TNBC 癌细胞系的生长，IC50的范围为 10 nM 至 20 nM。
T7512	BMS-191011 BMS-A	Potassium Channel	Membrane transporter/Ion channel
	BMS-191011 (BMS-A) 是一种大电导 Ca2+激活的钾通道 (Ca2+-activated potassium (maxi-K) channel) 激活剂，在中风模型中有研究价值。
T41345	AFMK Formyl-N-acetyl-5-methoxykynurenamine,Acetyl-N-formyl-5-methoxykynurenamine	Apoptosis; Free radical scavengers; Antioxidant; Endogenous Metabolite	Apoptosis; Metabolism; oxidation-reduction
	AFMK (Formyl-N-acetyl-5-methoxykynurenamine) 是褪黑激素的活性代谢物，具有抗氧化和自由基清除活性。 AFMK 是一种凋亡调节剂，可提高吉西他滨在 PANC-1 细胞中的抗肿瘤作用。
T3960	T56-LIMKi T5601640	LIM Kinase	Cell Cycle/Checkpoint
	T56-LIMKi (T5601640) 是一种选择性LIMK2抑制剂，抑制Panc-1细胞生长的IC50值为35.2 μM。
T24574	OXA-06 Dihydrochloride
	OXA-06 Dihydrochloride is a PANC-1 cell migration and MYPT1 phosphorylation inhibitor.
T4449	LB100 LB-100,LB 100	Phosphatase	Metabolism
	LB100 (LB-100) 是一种水溶性蛋白磷酸酶 2A(PP2A) 抑制剂。
T83015	Antiproliferative agent-42
	Antiproliferative agent-42（compound 7m）为一种二氢双吡咯化合物，在Panc-1细胞系上显示出明显的抗增殖活性，其IC50值为12.54 μM。
T37844	Kigamicin C
	Kigamicins are natural antitumor antibiotics that selectively kill pancreatic cancer PANC-1 cells only under nutrient-starved conditions. They also show antimicrobial activity against Gram-positive bacteria, including methicillin-resistant S. aureus. Kigamicin C inhibits PANC-1 cell survival in nutrient-deprived media at a 100-fold lower concentration than that required for cells maintained in nutrient-rich media. A related compound, kigamicin D, is active in vivo, suppressing the tumor growth o...
T83877	2-(cyclohexylmethyl)-Plumbagin
	2-(cyclohexylmethyl)-Plumbagin是naphthoquinone plumbagin的衍生物。在模拟胰腺癌肿瘤微环境的营养匮乏条件下，与营养丰富条件下的PANC-1细胞相比，对PANC-1人类胰腺癌细胞表现出选择性的细胞毒性，50%优选细胞毒性值(PC50s)分别为0.11和47.2 µM。1 µM浓度下，还可诱导PANC-1细胞发生凋亡。此外，2-(cyclohexylmethyl)-Plumbagin在营养匮乏条件下，而非营养丰富条件下，选择性降低PANC-1细胞中Akt和哺乳动物雷帕霉素靶蛋白(mTOR)的磷酸化。在以每周五次、每次50和250 µg/动物剂量给药的MiaPaCa-2胰腺癌小鼠异种移植模型中，能减少肿瘤体积和重量。
T72569	Cathepsin L/S-IN-1
	CathepsinL/S-IN-1 是 Cathepsin L 和 Cathepsin S 的双重抑制剂，IC50分别为 4.10 μM 和 1.79 μM。CathepsinL/S-IN-1 对胰腺癌 BxPC-3 和 PANC-1 细胞具有显著的抗转移和侵袭作用。
T60672	GSD-11
	GSD-11 抑制 Akt/mTOR 信号通路。GSD-11 是一种有效的选择性抗紧缩剂，抑制 PANC-1 细胞的迁移和集落形成，具有用于胰腺癌研究的潜力。
T79249	Antitumor agent-101	Histone Methyltransferase	Chromatin/Epigenetic
	Antitumor agent-101是一种针对赖氨酸甲基转移酶G9a/GLP的选择性共价抑制剂，其对G9a的IC50为8.5 nM，对GLP为5.5 nM。在PANC-1异种移植模型中，Antitumor agent-101展现了其抗肿瘤活性。
T82673	CPF-7 Caerulein precursor fragment
	CPF-7（Caerulein precursor fragment）是一种促进胰岛素释放的肽，可以通过增加PANC-1导管细胞中Snai1表达来引导上皮-间质转换（EMT），并且CPF-7还能通过提高Ngn3表达以诱导外分泌细胞可塑性。此外，CPF-7适用于2型糖尿病的相关研究。
T36404	PRLX-93936
	PRLX-93936 is an analog of erastin that has antitumor activity. It inhibits the hypoxia-inducible factor 1 (HIF-1) signaling pathway under hypoxic conditions (IC50 = 0.09 μM in a cell-based reporter assay). PRLX-93936 (1 μM) also inhibits hypoxia-induced increases in HIF-1α expression in ME-180 cervical cancer cells. It inhibits the growth of HT-1080 fibrosarcoma, OVCAR-5 ovarian cancer, BJELR tumorigenic primary fibroblast, and PANC-1 pancreatic cancer cells with IC50 values of less than 100 nM...
T79664	RUNX-IN-1	Apoptosis	Apoptosis
	RUNX-IN-1 Compound Conjugate 1) 具有与RUNX结合序列共价结合的特性，能有效抑制RUNX蛋白与其靶位点的相互作用。该化合物能激活p53依赖的细胞凋亡(apoptosis)过程，并能够抑制细胞增殖。此外，RUNX-IN-1在PANC-1异种移植小鼠模型中显示出对肿瘤生长的抑制作用。
T62503	EGFR/BRAFV600E-IN-1
	EGFR/BRAFV600E-IN-1 (Compound 23) 是一种有效的 EGFR (IC50: 0.08 μM) 和 BRAFV600E (IC50: 0.15 μM) 双重抑制剂。EGFR/BRAFV600E-IN-1 在 G1 前和 G2/M 期均诱导细胞凋亡 (apoptosis) 及细胞周期停滞。EGFR/BRAFV600E-IN-1 对 A-549 (IC50: 1.2 μM)、MCF-7 (IC50: 0.79 μM)、Panc-1 (IC50: 1.3 μM)、HT-29 (IC50: 1.23 μM) 表现出抗增殖作用。
T79665	RUNX-IN-2	Apoptosis	Apoptosis
	RUNX-IN-2 (Compound Conjugate 3) 具有高度特异性，能与RUNX结合序列共价结合并阻断RUNX蛋白与其靶位点的互动。该化合物能诱导p53依赖性细胞凋亡(apoptosis)，抑制细胞增殖，并在PANC-1异种移植小鼠模型中抑制肿瘤生长，显示出高效的烷基化活性。
T83889	C-02
	C-02是一种由巨噬细胞抑制剂Lonidamine和Cereblon配体Thalidomide组成的蛋白酶体靶向嵌合体（PROTAC）。在20 µM浓度下使用时，可诱导786-O和PANC-1细胞中的Hexokinase 2降解。C-02对786-O、4T1、PANC-1、HGC-27和MCF-7癌细胞具有细胞毒性（IC50分别为34.07、5.08、31.53、6.11和21.65 µM）。同时，20 µM浓度下减少4T1细胞的细胞外酸化率（ECAR）和氧气消耗率（OCR），表明其抑制糖酵解和引起线粒体损伤。在体内，C-02（50 mg/kg）能减少4T1小鼠乳腺癌模型的肿瘤体积，并诱导肿瘤内细胞因子积累和细胞焦亡。
T36398	Paclitaxel octadecanedioate
	Paclitaxel octadecanedioate is a prodrug form of paclitaxel that is comprised of paclitaxel conjugated to 1,18-octadecanedioic acid.1 Unlike paclitaxel, it does not promote tubulin polymerization in vitro when used at a concentration of 10 μM. A 5:1 mixture of paclitaxel octadecanedioate:human serum albumin (HSA) is cytotoxic to HT-1080, PANC-1, and HT-29 cells (IC50s = 12, 2.48, and 8.62 nM, respectively). This mixture reduces tumor growth and increases survival in an HT-1080 mouse xenograft mo...
T68861	MS-0022
	MS-0022 is a SMO antagonist. MS-0022 showed effective Hh signaling pathway inhibition at the level of SMO in the low nM range, and Hh pathway inhibition downstream of Suppressor of fused (SUFU) in the low µM range. MS-0022 reduced growth in the tumor cell lines PANC-1, SUIT-2, PC-3 and FEMX in vitro. MS-0022 is a treatment led to a transient delay of tumor growth that correlated with a reduction of stromal Gli1 levels in SUIT-2 xenografts in vivo.
T70352	PH11
	PH11 is a novel Focal Adhesion Kinase (FAK) inhibitor. PH11 restores TRAIL apoptotic pathway in PANC-1 cells through down-regulation of c-FLIP via inhibition of FAK and the phosphatidylinositol-3 kinase (PI3K)/AKT pathways. Tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) emerges as one of the most-promising experimental cancer therapeutic drugs and is currently being tested in clinical trials. However, both intrinsic and acquired resistance of human cancer cells to TRAIL...
T37983	GM 1489
	GM 1489 is a broad-spectrum inhibitor of matrix metalloproteinases (MMPs) with Ki values of 0.002, 0.1, 0.5, 0.2, and 20 μM for MMP-1, MMP-8, MMP-2, MMP-9, and MMP-3, respectively. It reduces 5-aza-2'-deoxycytidine-induced increases in MMP-1, MMP-2, MMP-3, MMP-7, MMP-9, and MMP-14 expression as well as cell invasion in AsPC-1, BxPC-3, Hs766T, MiaPaCa2, and PANC-1 cancer cells. Topical administration of GM 1489 (100 μg) inhibits increases in ear thickness and epidermal hyperplasia induced by phor...
T36514	QD-394
	QD-394 is an inducer of reactive oxygen species (ROS) production.1It induces lipid peroxidation, increases in intracellular accumulation of reactive oxygen species (ROS), and decreases in the reduced glutathione (GSH) to oxidized GSH (GSSG) ratio in MIA PaCa-2 pancreatic cancer cells when used at concentrations ranging from 0.5 to 10 μM. QD-394 is cytotoxic to MIA PaCa-2, PANC-1, and BxPC-3 cancer cells (IC50s = 0.64, 0.34, and 0.9 μM, respectively). QD-394 acts synergistically with napabucasin ...
T37248	Pantothenate Kinase Inhibitor
	Pantothenate Kinase Inhibitor (PANKi) is a reversible inhibitor of pantothenate kinase (PanK; IC50s = 70, 92, and 25 nM for PanK1β, PanK2, and PanK3, respectively), the rate-limiting enzyme in the synthesis of coenzyme A .1It binds to the ATP-PanK3 complex with an apparent binding constant of 300 nM and exhibits mixed-type inhibition with respect to ATP and pantothenate. PANKi inhibits CoA biosynthesis in C3A cells (IC50= 0.9 μM) with no effect on cell viability when used at concentrations up to...
T6069	Gemcitabine hydrochloride Gemcitabine HCl,吉西他滨盐酸盐,Gemzar,LY188011,盐酸吉西他滨,LY 188011 hydrochloride	Apoptosis; Nucleoside Antimetabolite/Analog; DNA/RNA Synthesis; Autophagy	Apoptosis; Autophagy; Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	Gemcitabine hydrochloride (LY 188011 hydrochloride) 是一种人工合成的胞嘧啶核苷衍生物，一种 DNA 合成抑制剂。Gemcitabine 具有抗肿瘤活性和抗代谢活性。Gemcitabine 可以引起细胞自噬和凋亡。
T10106	3-arylisoquinolinamine derivative	Others	Others
	3-arylisoquinolinamine derivative is a compound with antitumor activity.

化合物

Cat.No: T16961

Synonym: RX-5902

Target: Apoptosis, DNA/RNA Synthesis

Cat.No: T7512

Synonym: BMS-A

Target: Potassium Channel

Cat.No: T41345

Synonym: Formyl-N-acetyl-5-methoxykynurenamine,Acetyl-N-formyl-5-methoxykynurenamine

Target: Apoptosis, Free radical scavengers, Antioxidant, Endogenous Metabolite

Cat.No: T3960

Synonym: T5601640

Target: LIM Kinase

OXA-06 Dihydrochloride

Cat.No: T24574

Cat.No: T4449

Synonym: LB-100,LB 100

Target: Phosphatase

Antiproliferative agent-42

Cat.No: T83015

Cat.No: T37844

2-(cyclohexylmethyl)-Plumbagin

Cat.No: T83877

Cathepsin L/S-IN-1

Cat.No: T72569

Cat.No: T60672

Antitumor agent-101

Cat.No: T79249

Target: Histone Methyltransferase

Cat.No: T82673

Synonym: Caerulein precursor fragment

Cat.No: T36404

Cat.No: T79664

Target: Apoptosis

EGFR/BRAFV600E-IN-1

Cat.No: T62503

Cat.No: T79665

Target: Apoptosis

Cat.No: T83889

Paclitaxel octadecanedioate

Cat.No: T36398

Cat.No: T68861

Cat.No: T70352

Cat.No: T37983

Cat.No: T36514

Pantothenate Kinase Inhibitor

Cat.No: T37248

Gemcitabine hydrochloride

Cat.No: T6069

Synonym: Gemcitabine HCl,吉西他滨盐酸盐,Gemzar,LY188011,盐酸吉西他滨,LY 188011 hydrochloride

Target: Apoptosis, Nucleoside Antimetabolite/Analog, DNA/RNA Synthesis, Autophagy

3-arylisoquinolinamine derivative

Cat.No: T10106

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
T5668	Triacetylresveratrol 乙酰化白藜芦醇,三乙酰基白藜芦醇,Acetyl-trans-resveratrol	BCL; NF-κB; STAT	Apoptosis; JAK/STAT signaling; NF-κB; Stem Cells
	Triacetylresveratrol (Acetyl-trans-resveratrol) 是 Resveratrol 的乙酰化类似物，可降低 STAT3和 NF-κB 磷酸化，具有抗癌作用。
TWS2045	Bruceine D 鸦胆子素D,鸦胆子苦素D	Apoptosis; Antiviral; Gamma-secretase; Parasite	Apoptosis; Immunology/Inflammation; Microbiology/Virology; Neuroscience; Proteases/Proteasome; Stem Cells
	Bruceine D 是Notch 抑制剂，有抗癌活性，诱导几种人癌细胞调亡。它是一种有效的植物性昆虫拒食剂，有显著的系统特性和抑制害虫生长的作用。它具有较强的驱虫活性，抑制D. intermedius 的 EC50值为 0.57 mg/L。
T72742	(-)-Pinocembrin (-)-乔松素
	(-)-Pinocembrin 对 H37Ra 结核分枝杆菌展示了抗菌活性，无论是休眠还是活跃期，其 IC50 值分别为1.11 mg/mL 和 1.21 mg/mL。作为一种抗增殖剂，(-)-Pinocembrin 对于 THP-1、A549、Panc-1、HeLa 和 MCF7 细胞系，IC50 值范围为 1.88 至 11.00 mg/mL。
T36797	1-Alaninechlamydocin
	1-Alaninechalmydocin is a fungal metabolite originally isolated from a Great Lakes-derived Tolypocladium sp. and an inhibitor of histone deacetylases (HDACs). It reduces total HDAC activity in HeLa cell lysates in a concentration-dependent manner. 1-Alaninechlamydocin reduces proliferation of MIA PaCa-2, PANC-1, and hTERT-HPNE cells (GI50s = 5.3, 14, and 2.0 nM, respectively).
TN3401	Altenuene	Antifection	Microbiology/Virology
	Altenuene 是一种霉菌毒素，经常出现在被链格孢属真菌侵染的食物和饲料中。 Altenuene 表现出对金黄色葡萄球菌的中等活性。 Altenuene 还表现出对肺癌细胞系 A549、乳腺癌细胞系 MDA-MB-231 和胰腺癌细胞系 PANC-1 的细胞毒活性。
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...
TN4261	Isoaltenuene	Antifection	Microbiology/Virology
	Isoaltenuene shows antibiotic activity against Gram-positive bacteria; it also shows a minor phytotoxic activity on tomato leaves at level of 20 ug/spot . Isoaltenuene exhibits cytotoxic activity against lung cancer cell line A549, breast cancer cell line

天然产物

Triacetylresveratrol

Cat.No: T5668

Synonym: 乙酰化白藜芦醇,三乙酰基白藜芦醇,Acetyl-trans-resveratrol

Target: BCL, NF-κB, STAT

Cat.No: TWS2045

Synonym: 鸦胆子素D,鸦胆子苦素D

Target: Apoptosis, Antiviral, Gamma-secretase, Parasite

(-)-Pinocembrin

Cat.No: T72742

Synonym: (-)-乔松素

1-Alaninechlamydocin

Cat.No: T36797

Cat.No: TN3401

Target: Antifection

Cat.No: T36179

Cat.No: TN4261

Target: Antifection

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