colorectal cancer (crc)

Sulindac (Sulindac sulfoxide) is a sulfinylindene derivative prodrug with potential antineoplastic activity. Converted in vivo to an active metabolite, sulindac, a nonsteroidal anti-inflammatory drug (NSAID), blocks cyclic guanosine monophosphate-phosphodiesterase (cGMP-PDE), an enzyme that inhibits the normal apoptosis signal pathway; this inhibition permits the apoptotic signal pathway to proceed unopposed, resulting in apoptotic cell death.

GSK484 hydrochloride (GTPL8577) is a reversible peptidyl-arginine deiminase 4 (PAD4) inhibitor. It binds to PAD4 with high affinity, with IC50 of 250 and 50 nM in the presence and absence of 2 mM calcium, respectively. GSK484 promotes the radiosensitivity of colorectal cancer (CRC) and inhibits NET formation in vitro and in vivo.

SFI003 is a novel SRSF3 inhibitor that exerts anticancer activity against colorectal cancer by modulating the SRSF3 DHCR24 ROS axis and driving apoptosis in CRC cells through the SRSF3 DHCR24 reactive oxygen species (ROS) axis.

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].

Liensinine is the active constituent of plumula nelambinis with anti-hypertension.

XSJ05, a derivative of camptothecin (CPT), exhibits anti-cancer activity by inhibiting topoisomerase I (Topo I). This compound induces DNA double-strand breaks, leading to DNA damage. Furthermore, XSJ05 stifles the growth of colorectal cancer (CRC), halts the cell cycle in the G2 M phase, and induces apoptosis.

CRC-IN-1 (compound (-) -15h) is an effective agent against colorectal cancer (CRC) both in vitro and in vivo, and it is a derivative of the anticancer substance Evodiamine.

LZ9 is an ATP-competitive inhibitor of CDK1 and CDK2, with potential applications in colorectal cancer (CRC) research.

p38α inhibitor9 (Compound 2015) is a p38α inhibitor that effectively blocks the enzyme activity of p38α, with an IC50 of less than 20 nM. It inhibits MK2T334 phosphorylation and activates Cdc25b and Cdc25c while inactivating Wee1, leading to mitotic catastrophe, aneuploidy or polyploidy, and DNA damage. Additionally, p38α inhibitor9 can suppress colorectal cancer (CRC) metastasis.

Mal-N(Me)-C6-N(Me)-PNU-159682 (Compound 27) is an active molecular conjugate used in antibody-drug conjugates (ADCs), consisting of the ADC linker Mal-N(Me)-C6-N(Me) and the potent cytotoxin PNU-159682. This compound selectively delivers its payload to cells expressing CD46 and releases PNU-159682 through cathepsin B cleavage of the linker, inducing DNA damage and apoptosis. Mal-N(Me)-C6-N(Me)-PNU-159682 has demonstrated sustained tumor regression in patient-derived xenograft (PDX) models of non-small cell lung cancer (NSCLC) and colorectal cancer (CRC).

RS47 is a potent and specific inhibitor of the non-canonical NF-κB signaling pathway, with a Kd value of 1.1 μM, acting by blocking the binding of RelB to target DNA. Studies indicate that RS47 can inhibit the growth of colorectal cancer (CRC) cells and B lymphomas, making it a promising research tool for targeting cancers driven by hyperactive non-canonical NF-κB signaling.

Cyclosomatostatin Acetate is an effective antagonist of the somatostatin receptor.Cyclosomatostatin Acetate inhibits SSTR1 signaling and decreases cell proliferation, ALDH+ cell population size, and sphere-formation in colorectal cancer cells.

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

Rineterkib hydrochloride (compound B) is an orally active RAF and ERK1 2 inhibitor used in treating proliferative diseases characterized by activating mutations in the MAPK pathway, particularly KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC), and KRAS-mutant ovarian cancer[1].

CDK5 inhibitor 20-223 （CP668863） is a potent CDK2 CDK5 inhibitor with IC50 values of 6.0 nm and 8.8 nM, respectively, with anti-Colorectal Cancer (CRC) potential, inhibiting cell migration and inducing cell cycle arrest in multiple CRC cell lines.

YB-0158 (Wnt pathway inhibitor 2) is a potent peptidomimetic compound that targets colorectal cancer stem cells (CSCs) by disrupting the interaction between Sam68 and Src proteins. As a reverse-turn agent, it induces apoptosis in CRC cells and exhibits strong anti-cancer activity.

NCT02, a cyclin K degrader, promotes the ubiquitination and proteasomal degradation of cyclin K (CCNK) and its complex partner CDK12, showing promise for metastatic colorectal cancer (CRC) research[1].

Sulindac (sodium) (MK-231) is an orally active nonsteroidal anti-inflammatory agent. Sulindac (sodium) is used to reduce pain, swelling, and joint stiffness from arthritis. Sulindac is also used for the research of arthritis of the spine, gouty arthritis. Sulindac (sodium), as an immunomodulatory agent, can downregulate PD-L1 through the blockade of NF-κB signaling and modulates the response of pMMR colorectal cancer (CRC) to anti-PD-L1 immunotherapy, inhibits the development and progression of colorectal cancer CRC. Sulindac (sodium) also inhibits TGF-β1- induced epithelial-mesenchymal transition (EMT) and suppresses lung cancer cell migration and invasion via downregulation of SIRT1 [1] [2].

hCAIX-IN-12 is an effective hCAIX inhibitor, IC50 for CAIX and CAII is 0.74 and 10.78 μM , respectively. hCAIX-IN-12 inhibits cell proliferation and induces apoptosis. HCAIX-IN-12 can increase the generation of ROS. HCAIX-IN-12 has research potential in colorectal cancer (CRC).

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 reactivation of EGFR and EGFR-mediated cell proliferation. In vivo, BGB-283 treatment leads to dose-dependent tumor growth inhibition accompanied by partial and complete tumor regressions in both cell-line derived and primary human colorectal tumor xenografts bearing B-RAFV600E mutation. BGB-283 as a potent antitumor drug candidate with clinical potential for treating CRC harbouring B-RAFV600E mutation.

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.

BLM-IN-2, a Bloom's Syndrome Protein (BLM) inhibitor, exhibits an IC50 of 0.8 μM and shows efficacy in suppressing proliferation, invasion, cell cycle arrest, and apoptosis in colorectal cancer (CRC) cells, making it a potential candidate for CRC research.

Cyclosomatostatin TFA, a potent somatostatin (SST) receptor antagonist, inhibits type 1 somatostatin receptor (SSTR1) signaling, reducing cell proliferation, the size of the ALDH+ cell population, and sphere-formation in colorectal cancer (CRC) cells [1].

Petosemtamab (MCLA 158) is a highly potent monoclonal antibody against EGFR (Kd: 0.22 nM) and LGR5 (Kd: 0.86 nM). Petosemtamab promotes EGFR signaling disruption and receptor breakdown in LGR5+ cancer cells. Petosemtamab can be used in the study of solid tumors such as head and neck squamous cell carcinoma (HNSCC) and metastatic colorectal cancer (CRC).