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37

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T10309	Amphethinile Amphetinile,CRC 82-07	Others	Others
	Amphethinile is an anti-tubulin agent. The Ka of Amphethinile with tubulin is 1.3 μM.
T40254	MRTX-1719	Histone Methyltransferase	Chromatin/Epigenetic
	MRTX-1719 是有效的PRMT5/MTA 复合体选择性抑制剂，其对PRMT5/MTAMTAPDELSDMA 细胞系的IC50值为 <10 nM。
T29168	XR-5000 NSC-601316,CRC8805,SN-22995,DACA,CRC-8805
	XR-5000 is a DNA topoisomerase I and II inhibitor.
T13176	TNO155 Batoprotafib	Phosphatase	Metabolism
	TNO155 是具有口服活性野生型SHP2的选择性变构抑制剂 (IC50= 0.011 µM)。它有研究 RTK 依赖性恶性肿瘤（尤其是晚期实体瘤）的潜力。
T0459	Sulindac Arthrocine,MK-231,舒林酸,Clinoril,Sulindac sulfoxide	COX; Autophagy	Autophagy; Immunology/Inflammation; Neuroscience
	Sulindac (Sulindac sulfoxide) 是一种非甾体类抗炎剂，可抑制COX-2的活性，也可抑制 COX-2 的过表达。它是一种亚磺酰基茚衍生物前药，具有潜在的抗肿瘤活性。
T82324	GGASCCLYCRCH
	GGASCCLYCRCH 是一种具有生物活性的肽，它能够抑制 SARS-CoV 复合物 nsp16/10 的 2-O-甲基转移酶活性。
T73593	PDS-0330	Others	Others
	PDS-0330是一种 claudin-1小分子抑制剂抑制。PDS-0330抑制 claudin-1依赖性 CRC 进展，以微摩尔亲和力直接和特异性地与claudin-1结合。PDS-0330通过抑制与转移性癌基因Src 的关联，表现出具有良好药代动力学特性的抗肿瘤和化学增敏活性。PDS-0330干扰claudin-1 / Src 关联以抑制CRC 进展和转移。
T9556	TNIK-IN-3	Wnt/beta-catenin	Cytoskeletal Signaling; Stem Cells
	TNIK-IN-3 is a highly potent and orally active inhibitor of Traf2- and Nck-interacting protein kinase (TNIK). It exhibits a strong selectivity for TNIK with an IC50 value of 0.026 μM. Additionally, TNIK-IN-3 demonstrates inhibitory activity against Flt4 (IC50 = 0.030 μM), Flt1 (IC50 = 0.191 μM), and DRAK1 (IC50 = 0.411 μM). This compound holds potential for carrying out research on colorectal cancer (CRC) [1].
T77519	FC-116 FC116	Apoptosis; Microtubule Associated	Apoptosis; Cytoskeletal Signaling
	FC-116 是一种有效的 Tubulin 抑制剂，具有抗肿瘤活性，抑制小鼠体内肿瘤的生长。FC-116 诱导大肠癌 (CRC) 细胞凋亡，可促进蛋白降解。
T9901A-004	Labetuzumab IMMU-14,hMN-14,IMMU-100
	Labetuzumab (hMN-14) 是一种人源化抗癌胚抗原 (CEA) 单克隆抗体，具有抗癌活性，可抑制肿瘤生长，可用于研究甲状腺癌和结直肠癌 (CRC)。
T72068	SFI003	Apoptosis; ROS	Apoptosis; Immunology/Inflammation
	SFI003是一种新型SRSF3抑制剂，通过调节SRSF3 / DHCR24 / ROS 轴对结直肠癌发挥抗癌活性，通过SRSF3 / DHCR24 /活性氧（ROS）轴驱动CRC 细胞凋亡。
T76890	Petosemtamab MCLA 158	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Petosemtamab (MCLA 158) 是一种高效的抗 EGFR (Kd: 0.22 nM) 和抗 LGR5 (Kd: 0.86 nM) 单克隆抗体。Petosemtamab 促使 LGR5+ 癌细胞中的 EGFR 信号传导中断和受体分解。Petosemtamab 可用于头颈部鳞状细胞癌 (HNSCC)、转移性结直肠癌 (CRC) 等实体瘤的研究。
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。
T21567L	Cyclosomatostatin Acetate Cyclosomatostatin Acetate （84211-54-1 Free base）	Somatostatin	GPCR/G Protein
	Cyclosomatostatin Acetate 是有效的生长抑素受体拮抗剂。Cyclosomatostatin Acetate 在直肠癌 (CRC) 细胞中可以抑制 SSTR1的信号传导，并降低结细胞增殖、ALDH+ 细胞群体大小和球形成。
T41180	JQAD1	Epigenetic Reader Domain	Chromatin/Epigenetic
	JQAD1是一种有效的、选择性的组蛋白乙酰转移酶 EP300降解剂（PROTAC；DC50≤31.6nM）；其包含 EP300抑制剂A485，通过连接体连接至脑啡肽E3连接酶配体。JQAD1以蛋白酶体依赖的方式导致神经母细胞瘤细胞系中EP300的降解。JQAD1抑制H3K27ac 和EP300的表达水平并诱导细胞凋亡。JQAD1抑制Kelly 细胞异种移植的NSG 小鼠的肿瘤生长。CRC 和MYCN 基因表达水平在JQAD1治疗的肿瘤中下调。JQAD1在诱导EP300降解的浓度下对共活化剂CBP 没有显著影响。
T73391	BLM-IN-2
	BLM-IN-2是一种针对布鲁姆氏综合征蛋白(BLM)的抑制剂，IC50为0.8 μM。该化合物能够有效抑制结直肠癌(CRC)细胞的增殖、侵袭、诱导细胞周期阻滞及凋亡，因此适用于结直肠癌的研究。
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.
T36742	CDK5 inhibitor 20-223 CDK5 inhibitor 20-223
	CDK5 inhibitor 20-223, a potent inhibitor of CDK2 and CDK5, demonstrates IC50 values of 6.0 nM and 8.8 nM, respectively. It serves as an effective agent against colorectal cancer (CRC)[1].
T27163	DHNQ
	DHNQ is a novel inhibitor of the PI3K enzyme activity and transcriptional as well as translational expression levels in colorectal cancer (CRC).
T16406	Orvepitant maleate GW823296 maleate	Neurokinin receptor	GPCR/G Protein; Neuroscience
	Orvepitant maleate is an effective, selective, and well-tolerated neurokinin-1 receptor (NK-1) antagonist (pKi: 10.2 for human neurokinin-1 receptor). Orvepitant maleate has the potential for depressive disorder and chronic refractory cough (CRC) treatmen
T38519	YB-0158 Wnt pathway inhibitor 2,YB-0158
	YB-0158 (Wnt pathway inhibitor 2) is a powerful peptidomimetic compound that effectively targets colorectal cancer stem cells (CSCs) by disrupting the interaction between Sam68 and Src proteins. This compound acts as a reverse-turn agent, inducing apoptosis in CRC cells and displaying strong anti-cancer activities.
T70312	AZ1366
	AZ1366 is a potent tankyrase inhibitor that enhances irinotecan activity in tumors that exhibit elevated tankyrase and irinotecan resistance. Combination AZ1366 and irinotecan achieved greater anti-tumor effects compared to monotherapy. Activity was limited to CRC explants that displayed irinotecan resistance and increased protein levels of tankyrase and NuMA.
T72355	KRAS G12D inhibitor 16
	KRAS G12D inhibitor 16 是一种 KRAS G12D 抑制剂。KRAS G12D inhibitor 16 对 KRAS G12D 和 KRAS G12D 突变具有抑制活性，IC50值分别为 0.7 nM 和 0.35 μM。KRAS G12D inhibitor 16 可用于多种恶性肿瘤的研究，如胰腺导管腺癌（PDAC）、结肠直肠癌（CRC）、非小细胞肺癌（NSCLC）。
T21762	LDN-211904
	LDN-211904 oxalate (compound 32) 是一种有效的选择性EphB3抑制剂，IC50为 0.079 μM。LDN-211904 oxalate 在小鼠肝微粒体中具有良好的代谢稳定性。LDN-211904 oxalate 与西妥昔单抗联用可有效抑制 STAT3 激活的 CSC 干性和 CRC 中的西妥昔单抗耐药性。
T75842	Cyclosomatostatin TFA
	Cyclosomatostatin TFA 作为一种有效的生长抑素(SST)受体拮抗剂，在直肠癌(CRC)细胞中通过抑制1型生长抑素受体(SSTR1)的信号传导，有效降低结细胞增殖、ALDH+细胞群体的大小以及球形成。
T82414	Favezelimab MK-4280
	Favezelimab（MK-4280）为人源化抗LAG-3单克隆抗体，能够抑制LAG-3与其配体MHC II类结合。该抗体联合PD-L1抑制剂Pembrolizumab在结直肠癌（CRC）治疗研究中展现出应用前景。
T60030	NCT02
	NCT02 是一种细胞周期蛋白 K 降解剂，可诱导细胞周期蛋白 K (CCNK) 的泛素化和 CCNK 及其复合物 CDK12 的蛋白酶体降解。NCT02具有研究转移性结直肠癌 (CRC) 的潜力。
T39792	AMPC
	AMPC, a powerful and efficient inhibitor of TFF3, demonstrates inhibitory effects on cell proliferation, survival, oncogenicity, and CSC-like behavior in TFF3-positive CMS4 CRC cells. It acts as a promising standalone anti-cancer agent and also enhances the effects of 5-FU when used in combination, making it a valuable tool for cancer research.
T61896	hCAIX-IN-12
	hCAIX-IN-12 是有效的hCAIX 抑制剂，抑制 CAIX 和 CAII 的IC50分别为 0.74 和 10.78 μM。hCAIX-IN-12 抗细胞增殖并诱导凋亡 (apoptosis)。hCAIX-IN-12 可以增加ROS 的产生。hCAIX-IN-12在结直肠癌（CRC）中具有研究潜力。
T61585	Sulindac sodium
	Sulindac (sodium) (MK-231) 是一种非甾体抗炎剂，具有口服活性。Sulindac (sodium) 用于减轻疼痛，肿胀和关节僵硬的关节炎。Sulindac 还用于脊柱关节炎、痛风性关节炎的研究。Sulindac (sodium) 作为一种免疫调节剂，可通过阻断 NF-κB 信号通路下调 PD-L1，调节 pMMR CRC 对抗 PD-L1 免疫治疗的应答，抑制结直肠癌 CRC 的发生发展。 Sulindac 还可通过下调 SIRT1 抑制 TGF-β1-诱导的 EMT，抑制肺癌细胞的迁移和侵袭。
T36676	Rineterkib hydrochloride
	Rineterkib hydrochloride (compound B) is an orally active RAF and ERK1/2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer[1]. ERK-IN-1 (compound B) (50, 75 mg/kg, p.o., qd/q2d, 27 days) treatment significantly reduces the tumor volume in the C...
T78879	CXCR4-IN-2	CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation
	CXCR4-IN-2（compound A1）是一款具有抗癌活性的双功能氟化小分子，是CXCR4的强效抑制剂。它对小鼠结直肠癌(CRC)细胞展现出显著的细胞毒性（IC50：60 μg/mL；72小时）和抗增殖能力，能够引导细胞在G2/M期发生阻滞并诱导细胞凋亡(apoptosis)。
T35080	VU0456940 VU-0456940,VU 0456940
	VU0456940 is a potent M1 PAM with excellent selectivity (hM1 EC50 = 340 nM, 14-fold leftward shift of the ACh CRC; hM2–hM5 inactive). VU0456940 potentiated the excitation of a subthreshold concentration of CCh in MSNs. VU0456940 shifted APP processing and
T69985	Lifirafenib HCl
	Lifirafenib, also known as Beigene-283, is a Novel potent and selective RAF Kinase and EGFR inhibitor. BGB-283-displays Potent Antitumor Activity in B-RAF Mutated Colorectal Cancers. In vitro, BGB-283 potently inhibits B-RAFV600E-activated ERK phosphorylation and cell proliferation. It demonstrates selective cytotoxicity and preferentially inhibits proliferation of cancer cells harbouring B-RAFV600E and EGFR mutation/amplification. In B-RAFV600E CRC cell lines, BGB-283 effectively inhibits the ...
T63528	HSP90-IN-11
	HSP90-IN-11 是 HSP90 的有效抑制剂，诱导亚 G1 期群体的显着积累。 HSP90-IN-11 具有与 AUY-922 (Luminespib) 相当的有效 HSP90α 抑制作用。在 CRC 和 NSCLC 细胞中，HSP90-IN-11 具有显着的抗增殖活性，在两位数 nM 范围内。HSP90-IN-11 能够快速降解 NSCLC 细胞中客户蛋白 EGFR 和 Akt 。
T78569	CPT2 Carnitine palmitoyltransferase 2	Apoptosis	Apoptosis
	CPT2 (Carnitine palmitoyltransferase 2) 是一种脂肪酸氧化过程中的酶，它在结直肠癌 (CRC) 预后评估中作为生物标志物。CPT2 通过过表达激活p-p53并增加p53蛋白水平，这有助于抑制肿瘤生长和促进细胞的凋亡。CPT2 缺乏是长链脂肪酸氧化障碍相关的常见遗传性疾病，并且CPT2 的表达降低与多种癌症的发展密切相关，因此，在癌症研究领域具有研究价值。
T79226	AMPK activator 11	Mitochondrial Metabolism	Metabolism
	AMPK activator11 是一种抗肿瘤活性纳米级化合物，有效针对多种CRC。通过激活AMPK及上调OXPHOS（mitochondrial metabolism），该化合物能选择性抑制RKO异种移植物生长，应用于肿瘤和代谢性疾病研究领域。

化合物

Cat.No: T10309

Synonym: Amphetinile,CRC 82-07

Target: Others

Cat.No: T40254

Target: Histone Methyltransferase

Cat.No: T29168

Synonym: NSC-601316,CRC8805,SN-22995,DACA,CRC-8805

Cat.No: T13176

Synonym: Batoprotafib

Target: Phosphatase

Cat.No: T0459

Synonym: Arthrocine,MK-231,舒林酸,Clinoril,Sulindac sulfoxide

Target: COX, Autophagy

Cat.No: T82324

Cat.No: T73593

Target: Others

Cat.No: T9556

Target: Wnt/beta-catenin

Cat.No: T77519

Synonym: FC116

Target: Apoptosis, Microtubule Associated

Cat.No: T9901A-004

Synonym: IMMU-14,hMN-14,IMMU-100

Cat.No: T72068

Target: Apoptosis, ROS

Cat.No: T76890

Synonym: MCLA 158

Target: EGFR

Cat.No: T63049

Target: Others

Cyclosomatostatin Acetate

Cat.No: T21567L

Synonym: Cyclosomatostatin Acetate （84211-54-1 Free base）

Target: Somatostatin

Cat.No: T41180

Target: Epigenetic Reader Domain

Cat.No: T73391

Cat.No: T71624

CDK5 inhibitor 20-223

Cat.No: T36742

Synonym: CDK5 inhibitor 20-223

Cat.No: T27163

Orvepitant maleate

Cat.No: T16406

Synonym: GW823296 maleate

Target: Neurokinin receptor

Cat.No: T38519

Synonym: Wnt pathway inhibitor 2,YB-0158

Cat.No: T70312

KRAS G12D inhibitor 16

Cat.No: T72355

Cat.No: T21762

Cyclosomatostatin TFA

Cat.No: T75842

Cat.No: T82414

Synonym: MK-4280

Cat.No: T60030

Cat.No: T39792

Cat.No: T61896

Sulindac sodium

Cat.No: T61585

Rineterkib hydrochloride

Cat.No: T36676

Cat.No: T78879

Target: CXCR

Cat.No: T35080

Synonym: VU-0456940,VU 0456940

Lifirafenib HCl

Cat.No: T69985

Cat.No: T63528

Cat.No: T78569

Synonym: Carnitine palmitoyltransferase 2

Target: Apoptosis

AMPK activator 11

Cat.No: T79226

Target: Mitochondrial Metabolism

Cat. No.	Product Name	Target	Signaling Pathways
T6212	Combretastatin A4 CA4,康普瑞汀,Z)-3,4,5,4',-四甲氧基-3'-羟基二苯乙烯,CRC 87-09	Microtubule Associated	Cytoskeletal Signaling
	Combretastatin A4 (CA4) 是一种微管靶向剂，可结合 β-tubulin，Kd 值为 0.4 μM。
T3055	Liensinine Perchlorate	Apoptosis; Others	Apoptosis; Others
	Liensinine Perchlorate 是元莲的成分，可诱导结直肠癌细胞凋亡，具有抗高血压和抗癌活性。
T4S1551	Cinnamaldehyde Cinnamic Aldehyde,肉桂醛	HIF	Angiogenesis; Chromatin/Epigenetic
	Cinnamaldehyde (Cinnamic Aldehyde) 具有解热作用。它是镇静剂。它抑制MDA-MB-435S 细胞的侵袭能力与下调miR-27a 的表达有关。它诱导活性氧的产生，发挥血管扩张和抗癌作用。它似乎是一种有希望的候选药物，可作为与 5-氟尿嘧啶 (5-FU) 和奥沙利铂 (OXA) 这两种用于 CRC 治疗的化疗药物联合治疗的辅助剂。其作用的可能机制可能涉及药物代谢基因的调节。它在抑制黑色素瘤的发生和发展方面具有一定的作用，其作用机制可能表现为抑制VEGF 和HIF-α的表达，从而使血管模拟和黑色素瘤细胞新生血管的形成，促进肿瘤的生长。
T79933	(−)-N-Hydroxyapiosporamide NHAP	NF-κB	NF-κB
	(−)-N-Hydroxyapiosporamide (NHAP)为生物碱类NF-κB抑制剂，表现出体外及体内抗肿瘤活性，常用于结直肠癌(CRC)研究。

天然产物

Combretastatin A4

Cat.No: T6212

Synonym: CA4,康普瑞汀,Z)-3,4,5,4',-四甲氧基-3'-羟基二苯乙烯,CRC 87-09

Target: Microtubule Associated

Liensinine Perchlorate

Cat.No: T3055

Target: Apoptosis, Others

Cat.No: T4S1551

Synonym: Cinnamic Aldehyde,肉桂醛

Target: HIF

(−)-N-Hydroxyapiosporamide

Cat.No: T79933

Synonym: NHAP

Target: NF-κB

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