colorectal cancer (crc)

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 small-molecule inhibitor and an SRSF3 inhibitor with favorable pharmacokinetic properties, bioavailability, and tumor distribution capacity, inducing apoptosis in colorectal cancer cells through the SRSF3/DHCR24/ROS axis and exhibiting potent antitumor activity.

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].

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.

LRK-4189 is an orally active, selective PIP4K2C PROTAC degrader with a DC50 <500 nM in MOLT-4 cells. It induces endogenous apoptosis and activates the interferon signaling pathway, exhibiting antitumor activity against microsatellite stable (MSS) colorectal cancer (CRC) cells.

FC-116 is a potent Tubulin inhibitor with antitumour activity and inhibits tumour growth in mice. FC-116 induces apoptosis in colorectal cancer (CRC) cells and promotes protein degradation.

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).

PXB17 inhibits CSF1R activation (IC50= 1.7 nM) by blocking the PI3K/AKT/mTORC1 signaling pathway. It is effective orally, significantly suppresses the growth of colorectal cancer (CRC), enhances the efficacy of PD-1 monoclonal antibodies (PD-1mAb), and reduces the recurrence of CRC tumors.

Antibacterialagent 166 is a derivative of Nitishinone, functioning as a selective and orally active inhibitor of Fusobacterium nucleatum with an MIC50 of 1 μg/mL. It effectively reduces the migration capability of MC-38 cells induced by Fusobacterium nucleatum. Antibacterialagent 166 is a promising lead compound for studying colorectal cancer (CRC) due to its anti-F. nucleatum properties.

Antitumor agent-174 (Compound 10) directly binds to the N-terminal site of Hsp90, promoting the degradation of β-catenin and thereby inhibiting Wnt/β-catenin signaling. This compound effectively suppresses the proliferation of colorectal cancer (CRC) cells, induces S and G2/M phase arrest, and prevents cell colony formation. It downregulates proteins such as CDK1, Cyclin D1, c-Myc, Cyclin B1, and Cyclin A2, while upregulating P21. Antitumor agent-174 exhibits significant antitumor activity against CRC, offering excellent pharmacokinetics and low toxicity.

Indolimine-214 is a metabolite of M. morganii. It elevates γH2AX levels in HeLa cells and is applicable in research on inflammatory bowel disease (IBD) and colorectal cancer (CRC).

SVC112 is a translation elongation inhibitor that obstructs the periodic dissociation of EF2 from the ribosome, thereby inhibiting the elongation phase of translation. It demonstrates inhibitory activity in multiple cancer cell lines, including acute myeloid leukemia (AML), multiple myeloma, colorectal cancer (CRC), and head and neck squamous cell carcinoma (HNSCC). SVC112 preferentially impedes ribosomal processing of mRNA, reducing cancer stem cell (CSC)-related proteins such as Myc and Sox2. In hematological cancer cell lines, it induces apoptosis, whereas in colorectal cancer lines, the phosphorylation of c-Myc correlates with sensitivity to SVC112. The compound effectively inactivates HNSCC stem cells in vitro and prevents tumor regrowth in mouse HNSCC xenograft models. SVC112 is applicable for research on head and neck squamous cell carcinoma.

MMP-9-IN-12 is an inhibitor of matrix metalloproteinase-9 (MMP-9) with an IC50 value of 6.57 μM. It demonstrates an IC50 of 1.54 μM in HCT-116 cells and can induce apoptosis, reactive oxygen species (ROS) generation, and mitochondrial depolarization. Additionally, MMP-9-IN-12 inhibits cell migration and disrupts cell cycle progression, making it useful for colorectal cancer (CRC) research.

Z17544625 is a potent Fascin inhibitor with a strong binding affinity to Fascin, effectively inhibiting Actin bundling. It significantly reduces the proliferation and migration of colorectal cancer (CRC) cells. This compound is applicable in cancer research, particularly for studying colorectal cancer (CRC).

Z118298144 is a Fascin inhibitor that binds strongly to Fascin, effectively inhibiting Actin bundling. This compound significantly reduces the proliferation of colorectal cancer (CRC) cells and impedes their migration, making it valuable for cancer research, particularly in studies related to colorectal cancer (CRC).

MM927 is a potent NVL inhibitor with an IC50 value of 0.053 μM. It disrupts the biosynthesis of the 60S ribosomal subunit within the nucleolus, induces halfmer polysome formation, causes cell cycle arrest at the G1/S and G2/M phases, and triggers apoptosis (apoptosis). Demonstrating antitumor activity in both MOLM-13 acute myeloid leukemia (AML) and HCT116 colorectal cancer (CRC) xenograft models, MM927 can be utilized for studying AML and CRC cancers.

Ferroptosisinducer-9 is an agent that induces ferroptosis and acts as a microtubule polymerization inhibitor at the colchicine binding site. It inhibits MCF-7 cell growth with an IC50 of 14 nM and reduces [3H]colchicine binding. The compound decreases GPX4 and FTH expression while increasing COX2 and ACSL4 levels; it also lowers GSH, NADP+, and NADPH, and raises LPO, MDA, and Fe(II) concentrations, alongside reducing SOD levels. Ferroptosisinducer-9 demonstrates significant antitumor efficacy in HCT116 CRC xenograft models and is applicable in the study of triple-negative breast cancer (TNBC) and colorectal cancer (CRC).

HJ-4 is a derivative of Piperine. It effectively inhibits the proliferation of colorectal cancer (CRC) cells by reducing colony formation and DNA synthesis in a dose-dependent manner. HJ-4 notably impairs the adhesion, migration, and invasion of CRC cells and induces apoptosis. In a chicken embryo chorioallantoic membrane (CAM) model with implanted HCT116/SW480 tumor spheroids, HJ-4 demonstrates antitumor efficacy. HJ-4 is applicable for colorectal cancer (CRC) research.

ZLMT-72 is an orally active dual inhibitor of CDK2 and CDK9, with IC50 values of 0.741 nM and 1.03 nM, respectively. It shows excellent selectivity in kinase profiling and cholinesterase inhibition activity assays. ZLMT-72 exhibits significant antiproliferative effects on colorectal cancer (CRC) cell line HCT116 (GI50 < 0.1 nM). This compound induces apoptosis by inhibiting the phosphorylation of retinoblastoma protein and RNA polymerase II, leading to the downregulation of anti-apoptotic proteins (Mcl-1 and XIAP). ZLMT-72 is suitable for colorectal cancer (CRC) research.

CC-M-1 is a potent and selective PI3K/mTOR inhibitor. It has IC50 values of 0.68, 1.02, 1.03, 8.03, and 15 nM for PI3Kα/β/γ/δ and mTOR, respectively. CC-M-1 inhibits the proliferation of colorectal cancer cell lines such as HCT-116 (IC50= 0.38 μM) and HT-29 (IC50= 1.70 μM). This compound is applicable in colorectal cancer (CRC) research.