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63

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T4400	DIM-C-pPhOH CDIM8	Apoptosis; Others	Apoptosis; Others
	DIM-C-pPhOH (CDIM8) 是一种核受体 4A1(NR4A1) 拮抗剂，可降低细胞增殖，对 ACHN 细胞和 786-O 细胞的IC50值分别为 13.6 μM 和 13.0 μM。它抑制癌细胞的生长和 mTOR 信号传导，诱导细胞凋亡和细胞应激。
T23861	CAY10526 CAY-10526,BTH,CAY 10526	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	CAY10526 (BTH) 是 mPGES-1 的选择性抑制剂，可抑制 NF-κB 信号通路。
T7698	BS194 (2S,3S)-3-[[3-(异丙基)-7-[(苯基甲基)氨基]吡唑并[1,5-A]嘧啶-5-基]氨基]-1,2,4-丁三醇	CDK	Cell Cycle/Checkpoint
	BS194 是一种有效的细胞周期蛋白依赖性蛋白激酶 (CDK) 抑制剂。
T15030	CycLuc1	Others	Others
	CycLuc1 是一种荧光素酶底物，具有血脑屏障渗透性。
T2069L	TH287 hydrochloride	DNA/RNA Synthesis; MTH1	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	TH287 hydrochloride 是一种选择性MTH1抑制剂，IC50值为 0.8 nM。它可用于治疗癌症的研究。
T3469	PCI-27483 PCI27483	Others	Others
	PCI-27483 是一种FVIIa/tissue factor 抑制剂，具有抗肿瘤的作用。
T33467	MOMIPP	PI3K	PI3K/Akt/mTOR signaling
	MOMIPP 是一种 PIKfyve 抑制剂，是一种巨胞饮作用的诱导剂，可穿过血脑屏障 (BBB)。
T80725	ZK53	Others	Others
	ZK53 是一种具有选择性和高效性的线粒体酪蛋白水解蛋白酶 P (HsClpP) 激活剂。ZK53 诱导细胞凋亡，抑制 HsClpP水解α-酪蛋白。ZK53 在异种移植和本土小鼠模型中抑制肿瘤生长。
T71534L	CIA-1 (Free base) CIA-1(Free base）	Gamma-secretase	Neuroscience; Proteases/Proteasome; Stem Cells
	CIA-1 (Free base) 是一种核受体 COUP-TFII 抑制剂，在前列腺癌细胞系中IC50 值在 1.2 μM 到 7.6 μM 之间。CIA-1 (Free base) 在前列腺癌异种移植小鼠模型中抑制肿瘤生长。
T6695	Tasquinimod 他喹莫德,ABR-215050	HDAC	Chromatin/Epigenetic; DNA Damage/DNA Repair
	Tasquinimod (ABR-215050) 是一种口服抗血管生成剂，有潜在的抗肿瘤活性。它也是 S100A9抑制剂，与 HDAC4Zn2+结合结构域结合的 Kd 值在10到30 nM 之间。
T63049	CHD1Li 6.11	Others	Others
	CHD1Li 6.11 是一种致癌 CHD1L 的有效抑制剂，能够作用于 cat-CHD1L 重组蛋白 (IC50: 3.3 μM)。CHD1Li 6.11 是一种口服具有活力的抗肿瘤剂，明显减少由分离的准间充质细胞 (M 表型) 产生的 CRC 异种移植物的肿瘤体积，这些细胞具有增强的致瘤特性。
T6248	XL888	HSP	Cytoskeletal Signaling; Metabolism
	XL888 是一种 ATP 竞争性的 Hsp90 抑制剂，IC50值为 24 nM。
T3678	Entrectinib RXDX-101,恩曲替尼,NMS-E628	Trk receptor; ROS; ALK; Autophagy; ROS Kinase	Angiogenesis; Autophagy; Immunology/Inflammation; Tyrosine Kinase/Adaptors
	Entrectinib (RXDX-101) 是一种可口服的 Trk、ROS1和 ALK 抑制剂，具有抗肿瘤和中枢神经活性，抑制 TrkA、TrkB、TrkC、ROS1 和 ALK 的 IC50值分别为 1、3、5、12 和 7 nM。
T21831	UCM05 G28UCM	Fatty Acid Synthase	Metabolism
	UCM05 (G28UCM) (G28UCM) 是一种有效的脂肪酸合酶 (FASN) 抑制剂，对 HER2+ 乳腺癌异种移植物具有作用活性，且在抗 HER2 耐药细胞系中具有活性。UCM05 是一种丝状温度敏感蛋白 Z (FtsZ) 抑制剂，可抑制革兰氏阳性菌B. subtilis 生长，MIC 值为 100 μM，但对革兰氏阴性菌E. coli 缺乏活性。
T71867	PKM2 inhibitor 2825-0090
	PKM2 inhibitor 2825-0090 is a Novel pyruvate kinase M2 (PKM2) inhibitor, reducing tumor growth of NSCLC xenografts in vivo.
T34166	PROTAC_ERRalpha
	PROTAC_ERRalpha is a proteolysis targeting chimeras (PROTAC) which provides broad tissue distribution and knockdown of the targeted ERRalpha protein in tumor xenografts.
T26441	A 74932 A74932,A-74932
	A 74932 is a quinolone antibacterial agent and inhibitor of topoisomerase II enzyme. A-74932 possesses good activity in vivo against both systemic tumour, subcutaneously implanted murine solid tumours and human tumour xenografts.
T28215	NT113 NT 113,NT-113
	NT113 is a pan-ERBB inhibitor with high brain penetrance. NT113 is active against GBM xenografts in which wild-type EGFR or EGFRvIII is highly expressed. NT113 inhibits the growth of glioblastoma xenografts with EGFR amplification. NT113 has inhibitory ac
T34916	Transtinib
	Transtinib is an effective and irreversible EGFR tyrosine kinase inhibitor (EGFR-TKI) that is active against L858R/T790M mutated NSCLC cell lines and xenografts.
T14340	Atiratecan TP300	Others	Others
	Atiratecan (TP300) is a prodrug of camptothecin analog CH0793076. Atiratecan shows antitumor activity against both breast cancer resistance protein (BCRP)-positive and -negative xenografts in mouse xenograft models[1]. Atiratecan does not inhibit acetylch
T28203	NSC156529 NSC-156529,NSC 156529
	NSC156529 downregulates AKT1 signaling. NSC156529 efficiently decreases the proliferation of human cancer cells in vitro, and substantially inhibits the growth of prostate tumor xenografts in vivo.
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.
T70151	MeTC7
	MeTC7 is a VDR antagonist, which can be synthesized from 7-dehydrocholesterol (6) in two steps, inhibits VDR selectively, suppresses the viability of cancer cell-lines, and reduces the growth of the spontaneous transgenic TH-MYCN neuroblastoma and xenografts in vivo.
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...
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。
T71624	GB1874
	GB1874 inhibitor of the Wnt pathway that targets the β-cat-TCF4 PPI. GB1874 also affected the proliferation and stemness of Wnt-addicted colorectal cancer (CRC) cells in vitro. Encouragingly, GB1874 inhibited the growth of CRC tumor xenografts in vivo, thus demonstrating its potential for further development into therapeutics against Wnt-associated cancer indications.
T69922	EPZ020411 HCl
	EPZ020411 is a potent and selective PRMT6 inhibitor tool compound. EPZ020411 shows good bioavailability following subcutaneous dosing in rats making it a suitable tool for in vivo studies. EPZ020411 suppresses RCC1 arginine methylation and improves the cytotoxic activity of radiotherapy against GSC brain tumor xenografts.
T69589	PX-316
	PX-316 is a AKT inhibior. PX-316, when administered intraperitoneally to mice at 150 mg/kg, inhibits Akt activation in HT-29 human tumor xenografts up to 78% at 10 h with recovery to 34% at 48 h. PX-316 has antitumor activity against early human MCF-7 breast cancer and HT-29 colon cancer xenografts in mice. PX-316 formulated in 20% hydroxypropyl-beta-cyclodextrin for intravenous administration is well tolerated in mice and rats with no hemolysis and no hematological toxicity. Thus, PX-316 is the...
T71426	STA-1474
	STA-1474 is a water soluble prodrug of ganetespib (formerly STA-9090). STA-1474 will metabolized to Ganetespib, which is a potent HSP90 inhibitor previously shown to kill canine tumor cell lines in vitro and inhibit tumor growth in the setting of murine xenografts. The purpose of the following study was to extend these observations and investigate the safety and efficacy of STA-1474 in dogs with spontaneous tumors.
T28271	OSI-296
	OSI-296 is a potent and dual inhibitor of cMET and RON kinases (IC50 value are 42 nM and 200 nM for cMet and sfRon respectively) . OSI-206 shows in vivo efficacy and is well tolerated in tumor xenografts models upon oral dosing. OSI-296 also reduces tumou
T9665	Esuberaprost Sodium
	Famitinib (SHR1020) is a potent orally active multi-targeted kinase inhibitor that effectively inhibits the activity of c-kit, VEGFR-2, and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM, and 6.6 nM, respectively [1]. It demonstrates remarkable antitumor properties in human gastric cancer cells and xenografts, inducing apoptosis [2].
T36192	CAY10682
	(±)-Nutlin-3 blocks the interaction of p53 with its negative regulator Mdm2 (IC50 = 90 nM), inducing the expression of p53-regulated genes and blocking the growth of tumor xenografts in vivo. CAY10682 is a pyrrolo[3,4c]pyrazole derivative that inhibits the p53-Mdm2 interaction as potently as (±)-nutlin-3 (Ki = 83 nM) and also dose-dependently reduces activation of the NF-κB pathway. It specifically prevents phosphorylation of IκBα by the kinases IKKα, IKKβ, and IKK (IC50s = 80.5, 78.2, and 57.1...
T36458	CAY10701 CAY10701
	CAY10701 is a 7-deazahypoxanthine analog that prevents microtubule formation, blocking the proliferation of HeLa and MCF-7 cells (GI50s = 22 and 38 nM, respectively). It also inhibits the growth of several different colorectal cancer cell lines (GI50 values range from 9 to 17 nM), while being at least 1,500-fold less effective against normal human fibroblast WI38 cells. CAY10701 is effective in vivo, reducing tumor volume in colorectal cell xenografts in mice without significantly altering body ...
T62877	RET-IN-7
	RET-IN-7 在体外显示出强大的 RET 激酶抑制作用，在体内对 RET 驱动的肿瘤异种移植物具有强大的疗效。
T28216	NTRC 0066-0 NTRC-0066-0,NTRC-00660,NTRC00660,NTRC0066-0
	NTRC-0066-0 is a a highly potent and selective inhibitor of TTK. NTRC 0066-0 inhibits the phosphorylation of a TTK substrate and induces chromosome missegregation. NTRC 0066-0 inhibits tumor growth in MDA-MB-231 xenografts as a single agent after oral app
T76506	Coibamide A
	Coibamide A 是一种 N-甲基稳定的细胞毒性缩酚肽，具有强大的抗增殖活性。Coibamide A 通过mTOR 独立机制诱导自噬体积累。Coibamide A 诱导细胞凋亡。Coibamide A 抑制VEGFA/VEGFR2表达并抑制胶质母细胞瘤异种移植物中的肿瘤生长。
T70345	JAS239
	JAS239 is a novel carbocyanine dye that binds and competitively inhibits choline kinase (ChoK) intracellularly. JAS239 attenuated choline phosphorylation and viability in a panel of human breast cancer cell lines. Antibody blockade prevented cellular retention of JAS239 indicating direct interaction with ChoKα independent of the choline transporters and catabolic choline pathways. In mice bearing orthotopic MCF7 breast xenografts, optical imaging with JAS239 distinguished tumors overexpressing C...
T39553	TAK-960 monohydrochloride
	TAK-960 monohydrochloride is an orally available compound that selectively inhibits polo-like kinase 1 (PLK1) with an IC 50 of 0.8 nM. It also demonstrates inhibitory activity against PLK2 (IC 50 of 16.9 nM) and PLK3 (IC 50 of 50.2 nM). Moreover, TAK-960 monohydrochloride effectively suppresses the proliferation of various cancer cell lines and exhibits significant efficacy against multiple tumor xenografts.
T60661	CP681301
	CP681301 是CDK5的有效抑制剂，具有抗增殖活性。CP681301 在果蝇中表现出抗肿瘤活性。CP681301 降低神经胶质瘤干细胞中 CD133、OLIG2、SOX2、KI67、pCDK5 蛋白水平的表达。CP681301 减少小鼠胶质瘤异种移植物的自我更新。
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
T71111	Famitinib malate SHR1020 malate
	Famitinib (SHR1020) malate 是一种有效的，具有口服活性的多靶点激酶抑制剂，抑制 c-kit，VEGFR-2和 PDGFRβ的活性，IC50值分别为 2.3 nM、4.7 nM 和 6.6 nM。Famitinib malate 诱导细胞凋亡 (apoptosis)。Famitinib malate 具有抗肿瘤活性，可用于癌症的研究。
T76940	Cantuzumab ravtansine
	Cantuzumab ravtansine (IMGN242; huC242-DM4) 是一种 ADC，由一种人源化单克隆抗体 huC242，通过二硫键与 DM4 (DM4) 共价连接。Cantuzumab ravtansine 对一系列 CanAg 阳性人肿瘤异种移植物具有广泛的抗肿瘤功效。
T76558	Onvitrelin ucalontide
	Onvitrelin ucalontide ([Phor18-LHRH (338613)]) 是一种 LHRH (黄体生成素释放激素) 的类似物，展现出抗肿瘤特性。这一化合物是一个具备序列 KFAKFAKKFAKFAKKFAKQHWSYGLRPG 的肽，能在小鼠模型上有效地抑制乳腺癌、卵巢癌和前列腺癌的异种移植物生长。
T72269	TAK-960 dihydrochloride
	TAK-960 dihydrochloride 是一种有效的口服选择性polo-like kinase1 (PLK1) 抑制剂，其IC50 值为0.8 nM。同时，对PLK2 和PLK3 也表现出抑制活性，其IC50 分别为16.9 nM 和50.2 nM。此化合物能够抑制多种肿瘤细胞系的增殖，并对多种肿瘤异种移植显示出显著疗效。
T64216	TAK-960 hydrochloride
	TAK-960 hydrochloride 是一种有效的、选择性的、口服具有活力的 polo-like kinase 1 (PLK1) 抑制剂 (IC50: 0.8 nM)。TAK-960 hydrochloride 也能够抑制 PLK2 (IC50: 16.9 nM) 和 PLK3 (IC50: 50.2 nM)。TAK-960 hydrochloride 能够抑制多种肿瘤细胞系的增殖，显著治疗多种肿瘤异种移植。
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...
T68324	KCN1
	KCN1, a novel synthetic sulfonamide, is a HIF pathway inhibitor with potential anticancer activity in vitro and in vivo anti-pancreatic cancer activities and preclinical pharmacology. KCN1 specifically inhibited HIF reporter gene activity in several glioma cell lines at the nanomolar level. KCN1 also downregulated transcription of endogenous HIF-1 target genes, such as VEGF, Glut-1, and carbonic anhydrase 9, in a hypoxia-responsive element (HRE)-dependent manner. KCN1 potently inhibited the grow...
T64204	NU5455
	NU5455 是一种选择性的、有效的、口服具有活力的 DNA-PKcs 抑制剂。NU5455 能够提高肝肿瘤异种移植物中局部释放的多柔比星的效果，且不引起任何不良反应。NU5455 能够提高肠胃外给药的拓扑异构酶抑制剂的功效和毒性。
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.
T37018	OH-Chol
	OH-Chol is a cationic cholesterol derivative.1 OH-Chol, as a component of lipoplexes with DOPE , has been used for siRNA delivery and gene silencing in MCF-7 cells, as well as in mice via intravenous injection, resulting in lipoplex accumulation in the liver. It has also been used in cationic nanoparticles in combination with Tween 80 to transfect pDNA and siRNA into PC3 mouse xenografts via intratumoral injection and with Tween 80 and folate-PEG2000-DSPE in a KB mouse xenograft model for intrat...

化合物

Cat.No: T4400

Synonym: CDIM8

Target: Apoptosis, Others

Cat.No: T23861

Synonym: CAY-10526,BTH,CAY 10526

Target: Prostaglandin Receptor

Cat.No: T7698

Synonym: (2S,3S)-3-[[3-(异丙基)-7-[(苯基甲基)氨基]吡唑并[1,5-A]嘧啶-5-基]氨基]-1,2,4-丁三醇

Target: CDK

Cat.No: T15030

Target: Others

TH287 hydrochloride

Cat.No: T2069L

Target: DNA/RNA Synthesis, MTH1

Cat.No: T3469

Synonym: PCI27483

Target: Others

Cat.No: T33467

Target: PI3K

Cat.No: T80725

Target: Others

CIA-1 (Free base)

Cat.No: T71534L

Synonym: CIA-1(Free base）

Target: Gamma-secretase

Cat.No: T6695

Synonym: 他喹莫德,ABR-215050

Target: HDAC

Cat.No: T63049

Target: Others

Cat.No: T6248

Target: HSP

Cat.No: T3678

Synonym: RXDX-101,恩曲替尼,NMS-E628

Target: Trk receptor, ROS, ALK, Autophagy, ROS Kinase

Cat.No: T21831

Synonym: G28UCM

Target: Fatty Acid Synthase

PKM2 inhibitor 2825-0090

Cat.No: T71867

PROTAC_ERRalpha

Cat.No: T34166

Cat.No: T26441

Synonym: A74932,A-74932

Cat.No: T28215

Synonym: NT 113,NT-113

Cat.No: T34916

Cat.No: T14340

Synonym: TP300

Target: Others

Cat.No: T28203

Synonym: NSC-156529,NSC 156529

Cat.No: T69479

Cat.No: T70151

Cat.No: T68875

Cat.No: T36674

Target: Apoptosis, ERK

Cat.No: T71624

Cat.No: T69922

Cat.No: T69589

Cat.No: T71426

Cat.No: T28271

Esuberaprost Sodium

Cat.No: T9665

Cat.No: T36192

Cat.No: T36458

Synonym: CAY10701

Cat.No: T62877

Cat.No: T28216

Synonym: NTRC-0066-0,NTRC-00660,NTRC00660,NTRC0066-0

Cat.No: T76506

Cat.No: T70345

TAK-960 monohydrochloride

Cat.No: T39553

Cat.No: T60661

Cat.No: T27866

Synonym: LXY 6090,LXY-6090

Famitinib malate

Cat.No: T71111

Synonym: SHR1020 malate

Cantuzumab ravtansine

Cat.No: T76940

Onvitrelin ucalontide

Cat.No: T76558

TAK-960 dihydrochloride

Cat.No: T72269

TAK-960 hydrochloride

Cat.No: T64216

Cat.No: T36191

Cat.No: T68324

Cat.No: T64204

Cat.No: T68861

Cat.No: T37018

Cat. No.	Product Name	Target	Signaling Pathways
TN1853	Lariciresinol (+)-落叶松树脂醇	VEGFR; Antifection	Angiogenesis; Microbiology/Virology; Tyrosine Kinase/Adaptors
	Lariciresinol 是一种肠木脂素前体，它通过破坏真菌质膜具有杀真菌活性，并具有作为治疗人类真菌感染性疾病的新型抗真菌剂的治疗潜力。膳食 lariciresinol 可以减缓乳腺肿瘤的生长并降低人 MCF-7 乳腺癌异种移植物和致癌物诱导的大鼠乳腺肿瘤的血管密度。
T39071	Thailanstatin D
	Thailanstatin D, an analogue of Thailanstatin A, inhibits AR-V7 gene splicing by disrupting the interaction between U2AF65 and SAP155, hindering their binding to the polypyrimidine tract situated between the branch point and the 3' splice site. This compound displays potent tumor inhibitory properties in human castration-resistant prostate cancer (CRPC) xenografts, resulting in cellular apoptosis.
T36961	Malformin C
	Malformin C is a natural fungus-derived bicyclic pentapeptide that has antibacterial properties, particularly against species of Bacillus. Malformin C potently blocks the ability of bleomycin to induce G2 arrest in human T-cell leukemia-derived Jurkat cells (IC50 = 0.9 nM). It less potently abrogates colchicine-induced M phase arrest in Jurkat cells (IC50 = 24 nM). Malformin C inhibits cell growth dose-dependently in Colon 38 and HCT 115 cancer cells (IC50s = 0.27 and 0.18 μM, respectively) but ...
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

Cat.No: TN1853

Synonym: (+)-落叶松树脂醇

Target: VEGFR, Antifection

Thailanstatin D

Cat.No: T39071

Cat.No: T36961

Cat.No: T36954

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