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21

抑制剂 & 化合物

2

天然产物

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Cat. No. Product Name Target Signaling Pathways
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。
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。
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。
T27163 DHNQ

DHNQ is a novel inhibitor of the PI3K enzyme activity and transcriptional as well as translational expression levels in colorectal cancer (CRC).
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].
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.
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.
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。
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...
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。
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。
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。
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。
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。
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 ...
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)。
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。

化合物

Sulindac
Cat.No: T0459
Synonym: Arthrocine,MK-231,舒林酸,Clinoril,Sulindac sulfoxide
Target: COX, Autophagy
TNIK-IN-3
Cat.No: T9556
Synonym:
Target: Wnt/beta-catenin
FC-116
Cat.No: T77519
Synonym: FC116
Target: Apoptosis, Microtubule Associated
Labetuzumab
Cat.No: T9901A-004
Synonym: IMMU-14,hMN-14,IMMU-100
Target:
SFI003
Cat.No: T72068
Synonym:
Target: Apoptosis, ROS
Petosemtamab
Cat.No: T76890
Synonym: MCLA 158
Target: EGFR
Cyclosomatostatin Acetate
Cat.No: T21567L
Synonym: Cyclosomatostatin Acetate (84211-54-1 Free base)
Target: Somatostatin
DHNQ
Cat.No: T27163
Synonym:
Target:
CDK5 inhibitor 20-223
Cat.No: T36742
Synonym: CDK5 inhibitor 20-223
Target:
GB1874
Cat.No: T71624
Synonym:
Target:
YB-0158
Cat.No: T38519
Synonym: Wnt pathway inhibitor 2,YB-0158
Target:
BLM-IN-2
Cat.No: T73391
Synonym:
Target:
Rineterkib hydrochloride
Cat.No: T36676
Synonym:
Target:
Cyclosomatostatin TFA
Cat.No: T75842
Synonym:
Target:
NCT02
Cat.No: T60030
Synonym:
Target:
Favezelimab
Cat.No: T82414
Synonym: MK-4280
Target:
Sulindac sodium
Cat.No: T61585
Synonym:
Target:
hCAIX-IN-12
Cat.No: T61896
Synonym:
Target:
Lifirafenib HCl
Cat.No: T69985
Synonym:
Target:
CXCR4-IN-2
Cat.No: T78879
Synonym:
Target: CXCR
CPT2
Cat.No: T78569
Synonym: Carnitine palmitoyltransferase 2
Target: Apoptosis
Cat. No. Product Name Target Signaling Pathways
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。
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

Liensinine Perchlorate
Cat.No: T3055
Synonym:
Target: Apoptosis, Others
(−)-N-Hydroxyapiosporamide
Cat.No: T79933
Synonym: NHAP
Target: NF-κB
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