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抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T5345	V-9302	Others	Others
	V-9302 是一种跨膜谷氨酰胺通量的竞争性拮抗剂。它选择性的靶向氨基酸转运体 ASCT2 (SLC1A5)，不影响 ASCT1。它能够阻碍 HEK-293 细胞中由 ASCT2 介导的谷氨酰胺摄取 (IC50=9.6 μM)。
T9072	Tuxobertinib BDTX-189	EGFR; HER; BTK; RIP kinase	Angiogenesis; Apoptosis; JAK/STAT signaling; NF-κB; Tyrosine Kinase/Adaptors
	Tuxobertinib (BDTX-189) 是一种高效可口服的选择性 EGFR 和 HER2变构突变抑制剂，具有抗癌活性。它对 EGFR、HER2、BLK 和 RIPK2 的 KD 值分别为 0.2、0.76、13 和 1.2 nM。
T10717	Inobrodib CBP-IN-1	Epigenetic Reader Domain	Chromatin/Epigenetic
	Inobrodib (CBP-IN-1) 是一种口服活性的强选择性p300/CBP 抑制剂，与 p300 和 CBP 结合，Kd 值为 1.3 和 1.7 nM。它抑制前列腺癌细胞系的细胞增殖并降低雄激素受体和 C-MYC 调节的基因表达。
T11279	FGFR1/DDR2 inhibitor 1	Discoidin Domain Receptor (DDR); FGFR; Others	Angiogenesis; Others; Tyrosine Kinase/Adaptors
	FGFR1/DDR2 inhibitor 1 是一种具有口服活性的成纤维细胞生长因子受体 1 和盘状蛋白域受体 2 的抑制剂，能够抑制 FGFR1 (IC50:31.1 nM) 和 DDR2 (IC50:3.2 nM)，具有抗肿瘤作用。
T1290	Oxiconazole nitrate 硝酸奥昔康唑,Ro 13-8996	Others; Antibiotic; Antifection; Antifungal	Microbiology/Virology; Others
	Oxiconazole nitrate (Ro 13-8996) 是广谱抗真菌药物，抑制T. tonsurans 和T.rubrum 的生长，MIC90值分别为 0.25 和 0.5 μg/mL。
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。
T10313	AMXT-1501 tetrahydrochloride	Others	Others
	AMXT-1501 tetrahydrochloride is an inhibitor of polyamine transport. It blocks tumor growth in immunocompetent mice but not in athymic nude mice lacking T cells.
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。
T24188	J-104871 UNII-6137X5QNJF,J 104871
	J-104871 is an FTase inhibitor. J-104871 inhibits FTase in an FPP-competitive manner in whole cells as well as in the in vitro system. J-104871 suppressed tumor growth in nude mice transplanted with activated H-ras-transformed NIH3T3 cells.
T71494	ISC-4
	ISC-4 is an Akt inhibitor, which activates prostate apoptosis response protein-4 and reduces colon tumor growth in a nude mouse model.
T69479	CGC 11093
	CGC 11093 is a polyamine analog; inhibits growth of human prostate tumor xenografts in nude mice. It may prove useful in promoting regression of choroidal neovascularization.
T25367	EM-800 EM800,EM 800
	EM-800 is a high affinity ligand for estrogen receptor-α (ERα), the prodrug of EM-652. EM-800 independently inhibited the growth of E1-stimulated ZR-75-1 xenograft tumors in nude mice.
T27866	LXY6090 LXY 6090,LXY-6090
	LXY6090 is a HIF-1 inhibitor. LXY6090 inhibited the activity of HIF-1 and downregulated the protein level of HIF-1α in breast cancer cells. LXY6090 showed in vivo anticancer efficacy by decreasing the HIF-1α expression in nude mice bearing MX-1 tumor xeno
T73693	Peginterferon beta-1a
	Peginterferon beta-1a (Peginterferon β-1a) 是一个聚乙二醇化干扰素 beta-1a 分子。Peginterferon beta-1a 诱导癌细胞凋亡并且在裸鼠模型中显示出抗肿瘤活性。Peginterferon beta-1a 可用于癌症和多发性硬化 (RMS) 的研究。
T61532	Tubulin polymerization-IN-6
	Tubulin polymerization-IN-6 (compound 5f) is a potent inhibitor of tubulin polymerization, with an IC50 of 1.09 μM. It not only inhibits cell migration and tube formation but also has anti-angiogenic properties. Additionally, Tubulin polymerization-IN-6 has been found to effectively hinder tumor growth in HT29 xenograft Balb/c nude mice [1].
T72620	c-Myc inhibitor 9
	c-Myc inhibitor9 是一种c-Myc 抑制剂，logEC50值 ≥6。c-Myc inhibitor9 抑制异种移植裸鼠模型中肿瘤的生长。c-Myc inhibitor9 可用于癌症研究。
T82802	BX-2819	HSP	Cytoskeletal Signaling; Metabolism
	BX-2819为一种Hsp90抑制剂，具有41 nM 的IC50值，能有效抑制癌细胞增殖，并在裸鼠模型中显著抑制NCI-N87和HT-29肿瘤生长。
T68346	KRN383
	KRN383 also inhibited the proliferation of the ITD-positive cell lines with IC(50) values of < or =2.9 nM. A single oral administration of 80 mg/kg of KRN383 eradicated ITD-positive xenograft tumors in nude mice and prolonged the survival of SCID mice carrying ITD-positive AML cells. The effectiveness of a single oral dose of KRN383 suggests that it has the potential to be used in a wide variety of clinical regimens, including multicycle and combination therapies.
T61582	Anticancer agent 57
	Anticancer agent 57 (compound 14) demonstrates potent inhibition of MDA-MB-231, MDA-MB-468, and MCF-7 cell lines, with IC 50 values ranging from 6.43 to 8.00 μM. Additionally, this agent induces cell cycle arrest and promotes apoptosis. In vivo studies using nude mice xenografted with MADMB-231 cells have shown that Anticancer agent 57 effectively inhibits tumor growth. Consequently, Anticancer agent 57 can serve as a valuable tool for researching triple negative breast cancer (TNBC) [1].
T36191	CAY10681
	Inactivation of the tumor suppressor p53 commonly coincides with increased signaling through NF-κB in cancer. CAY10681 is a dual modulator of p53-MDM2 interaction and NF-κB signaling. It potently binds MDM2 (Ki = 250 nM), reducing MDM2-mediated turnover of p53. CAY10681 also inhibits phosphorylation of IκBα and dose-dependently reduces nuclear accumulation of p65. It blocks the proliferation of cancer cell lines (IC50s range from 33 to 37 μM). CAY10681 exhibits excellent oral bioavailability and...
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。
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...
TP1974	Obtustatin
	Highly potent integrin α1β1 inhibitor (IC50 = 0.8 nM for α1β1 binding to type IV collagen). Selective for α1β1 over α2β1, αIIbβ3, αvβ3, α4β1, α5β6, α9β1 and α4β7. Inhibits FGF2-stimulated angiogenesis in the chicken chorioallantoic model. Displays antitum
T74691	Aprinocarsen sodium
	Aprinocarsen (ISIS 3521) sodium，是针对蛋白激酶C-α（PKC-α）的特异性反义寡核苷酸抑制剂，为一种20-mer寡核苷酸，通过调节细胞分化和增殖来发挥作用。其能有效抑制人类肿瘤细胞系在裸鼠体内的生长，展示了作为人类癌症化疗化合物的潜力。
T63864	Antiproliferative agent-4
	Antiproliferative agent-4 对一些癌细胞表现出很好的抗增殖作用。Antiproliferative agent-4 能够抑制裸鼠肿瘤生长，且表现出低毒性。Antiproliferative agent-4 能够降低 EC109 细胞线粒体膜电位，提高细胞凋亡率和 ROS 水平。
T64027	ALK-IN-23
	ALK-IN-23 是 ALK 的有效抑制剂，能够作用于 ALKWT (IC50: 1.6 nM)、ALKL1196M (IC50: 0.71 nM) 和 ALKG1202R (IC50: 1.3 nM)。ALK-IN-23 能够诱导细胞凋亡 (apoptosis) 并将细胞阻滞在 G2 期。ALK-IN-23 在体外对癌细胞迁移和集落形成具有抑制作用。在 H2228 异种移植裸鼠模型中，ALK-IN-23 具有良好的抗肿瘤效果且毒性较低。
T29172	YD277 YD 277,YD-277
	YD277 is a small molecule derived from ML264, a KLF5 inhibitor that elicits cytotoxic effects in colon cancer cell lines. YD277 significantly induced G1 cell cycle arrest and apoptosis in MDA-MB-231 and MDA-MB-468 TNBC cells, independent of KLF5 inhibitio
T75363	Fluorescein Di-β-D-Glucuronide
	Fluorescein Di-β-D-Glucuronide 作为一款荧光探针，以其非侵入性的优势被广泛应用于裸鼠肠道细菌β-葡萄糖醛酸酶（βG）活性成像研究中。该探针通过成像技术有效揭示了肠道细菌β-葡萄糖醛酸酶在体内外的活性，进而为特定细菌β-葡萄糖醛酸酶抑制剂的药效学评估提供了重要工具。
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...
T78788	EGFR-IN-82	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	EGFR-IN-82（化合物8a）是一种口服活性的EGFR抑制剂，显示出对EGFRL858R/T790M/C797S的IC50为0.09 nM，以及对EGFRDel19/T790M/C797S的IC50为0.06 nM的高选择性，而对EGFRWT的抑制作用不明显。此化合物具备显著的抗增殖能力，并能有效抑制肿瘤增长，常用于非小细胞肺癌（NSCLC）的研究。
T73121	FGFR4-IN-8	FGFR	Angiogenesis; Tyrosine Kinase/Adaptors
	FGFR4-IN-8 (Compound 7v) 是 ATP 竞争性、高选择性的 FGFR4 野生型及其突变体共价抑制剂，对 FGFR4、FGFR4V550L、FGFR4V550M 及 FGFR4C552S 的 IC50 值分别为 0.5、0.25、1.6、931 nM。该化合物能有效抑制 Hep3B 肝细胞癌细胞增殖，显示出显著的抑制效果，具有潜在的临床应用价值。
T74783	HDAC-IN-53	HDAC	Chromatin/Epigenetic; DNA Damage/DNA Repair
	HDAC-IN-53是一种口服活性的选择性HDAC1-3抑制剂，其IC50分别为47 nM、125 nM和450 nM。该化合物不针对II类HDAC(HDAC4、5、6、7、9；IC50>10 μM)展现抑制作用。HDAC-IN-53能够诱导caspase依赖的细胞凋亡并在裸鼠中显著抑制人肿瘤异种移植物生长，同时抑制携带MC38结肠癌的免疫活性小鼠的肿瘤发展。
T71279	BPR1K653
	BPR1K653 is a potent Aurora kinase inhibitor with potential anticancder activity. BPR1K653 specifically inhibited the activity of Aurora-A and Aurora-B kinase at low nano-molar concentrations in vitro. BPR1K653 was potent in targeting a variety of cancer cell lines regardless of the tissue origin, p53 status, or expression of MDR1. At the cellular level, BPR1K653 induced endo-replication and subsequent apoptosis in both MDR1-negative and MDR1-positive cancer cells. Importantly, it showed potent ...
T68249	IRC-083927 HCl
	IRC-083927 HCl is novel and potent microtubule inhibitor with potential anticancer activity. IRC-083927 inhibits the tubulin polymerization by a binding to the colchicine site. IRC-083927 inhibits in vitro cell growth of human cancer cell lines in the low nanomolar range. More interesting, it remains highly active against cell lines resistant to microtubule-interacting agents (taxanes, Vinca alkaloids, or epothilones). Chronic oral treatment with IRC-083927 (5 mg/kg) inhibits the growth of two h...
T36084	PKI-179
	PKI-179 is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 shows anti-tumor activity in vivo[1][2]. PKI-179 inhibits the cell proliferation, with IC50s of 22 nM and 29 nM for MDA361 and PC3 cells, respectively[1].PKI-179 shows inhibitory activity against a panel of 361 other ...
T65994	(6S)-N-Benzyl-6-(4-hydroxybenzyl)-8-(naphthalen-1-ylmethyl)-4,7-dioxohexahydro-2H-pyrazino[1,2-a]pyrimidine-1(6H)-carboxamide
	Wnt signaling is required for direct multiple biological processes and also plays key roles in the pathogenesis of various diseases. Cyclic AMP response element-binding protein (CREB) is a transcription factor that is a member of the leucine zipper family of DNA binding proteins. This protein binds as a homodimer to the cAMP-responsive element, an octameric palindrome. The protein is phosphorylated by several protein kinases, and induces transcription of genes in response to hormonal stimulation...
T37585	Ensartinib
	Ensartinib (X-396) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively. The ability of Ensartinib (X-396) to inhibit the growth of different cancer cell lines harboring ALK fusions or point mutations is tested. Ensartinib is potent in H3122 lung cancer cells harboring EML4-ALK E13;A20 (IC50: 15nM). Ensartinib is also potent in H2228 lung cancer cells harboring EML4-ALK E6a/b; A20 (IC50: 45 nM). Furthermore, X-376 is potent in SUDHL-1 lymphoma cells harboring N...

化合物

Cat.No: T5345

Target: Others

Cat.No: T9072

Synonym: BDTX-189

Target: EGFR, HER, BTK, RIP kinase

Cat.No: T10717

Synonym: CBP-IN-1

Target: Epigenetic Reader Domain

FGFR1/DDR2 inhibitor 1

Cat.No: T11279

Target: Discoidin Domain Receptor (DDR), FGFR, Others

Oxiconazole nitrate

Cat.No: T1290

Synonym: 硝酸奥昔康唑,Ro 13-8996

Target: Others, Antibiotic, Antifection, Antifungal

Cat.No: T12134

Synonym: NSC354961

Target: Apoptosis, c-Myc

AMXT-1501 tetrahydrochloride

Cat.No: T10313

Target: Others

Cat.No: T8973

Target: Others

Cat.No: T24188

Synonym: UNII-6137X5QNJF,J 104871

Cat.No: T71494

Cat.No: T69479

Cat.No: T25367

Synonym: EM800,EM 800

Cat.No: T27866

Synonym: LXY 6090,LXY-6090

Peginterferon beta-1a

Cat.No: T73693

Tubulin polymerization-IN-6

Cat.No: T61532

c-Myc inhibitor 9

Cat.No: T72620

Cat.No: T82802

Target: HSP

Cat.No: T68346

Anticancer agent 57

Cat.No: T61582

Cat.No: T36191

P-gp inhibitor 15

Cat.No: T79261

Cat.No: T68875

Cat.No: TP1974

Aprinocarsen sodium

Cat.No: T74691

Antiproliferative agent-4

Cat.No: T63864

Cat.No: T64027

Cat.No: T29172

Synonym: YD 277,YD-277

Fluorescein Di-β-D-Glucuronide

Cat.No: T75363

Cat.No: T37844

Cat.No: T78788

Target: EGFR

Cat.No: T73121

Target: FGFR

Cat.No: T74783

Target: HDAC

Cat.No: T71279

Cat.No: T68249

Cat.No: T36084

(6S)-N-Benzyl-6-(4-hydroxybenzyl)-8-(naphthalen-1-ylmethyl)-4,7-dioxohexahydro-2H-pyrazino[1,2-a]pyrimidine-1(6H)-carboxamide

Cat.No: T65994

Cat.No: T37585

Cat. No.	Product Name	Target	Signaling Pathways
T3S0737	Flavokawain A 2'-羟基-4,4',6'-三甲氧基查耳酮,Flavokavain A	Apoptosis; p38 MAPK	Apoptosis; MAPK
	Flavokawain A (Flavokavain A) 是 kava 提取物中的查耳酮，是一种抗癌试剂，具有抗肿瘤活性。它通过 Bax 蛋白依赖和线粒体依赖的凋亡途径诱导细胞凋亡，有潜力用于膀胱癌的相关研究。

天然产物

Cat.No: T3S0737

Synonym: 2'-羟基-4,4',6'-三甲氧基查耳酮,Flavokavain A

Target: Apoptosis, p38 MAPK

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