adenocarcinoma cell

3PO is a small-molecule inhibitor of PFKFB3 (IC50: 22.9 μM), inhibiting the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50: 1.4-24 μM). It suppresses glucose uptake, and decreases the intracellular concentration

Ellipticine (Elliptisine) is a potent antineoplastic agent exhibiting multiple mechanisms of action, IC50 of 0.67±0.06, 1.25±0.13, 1.25±0.13, 0.67±0.06, 0.27±0.02, 0.49±0.04, 0.44±0.03, and 1.48±0.62 μM for Leukemia HL-60, Breast adenocarcinoma MCF-7, Breast adenocarcinoma MCF-7, Leukemia HL-60, Neuroblastoma IMR-32, Neuroblastoma UKF-NB-4, Neuroblastoma UKF-NB-3, and Glioblastoma U87 mg cell, respectively.

Vinaxanthone (SM-345431) is a small molecule compound derived from Penicillium chrysogenum that acts as a selective and potent inhibitor of semaphorin3A, phospholipase C (PLC), and FabI, exhibiting antimicrobial activity by blocking intracellular fatty acid synthesis and inhibiting the growth of Staphylococcus aureus.

Bexlosteride (LY300502), a benzoquinolinone derivative, functions as a human type I 5α-reductase inhibitor. It demonstrates metabolic inhibition, antiproliferative, and antisecretory activities specifically in LNCaP human prostatic adenocarcinoma cell cultures, positioning it as a potent agent for prostate cancer research [1] [2].

LRH-1 Inhibitor-3 is an antagonist that inhibits LRH-1 transcriptional activity, reducing the expression of target genes associated with cell growth and proliferation, such as SHP (small heterodimer partner), cyclin E1 (CCNE1), and G0S2, and inhibiting the proliferation of human pancreatic, colon, and breast adenocarcinoma cells.

PARP-1-IN-2 is a potent PARP1 inhibitor that crosses the blood-brain barrier (IC50: 149 nM).PARP-1-IN-2 showed significant antiproliferative activity against the human lung adenocarcinoma epithelial cell line A549 in cellular assays.PARP-1-IN-2 induced apoptosis in A549 cells.

BPI-9016M is an effective, orally active, and selective dual inhibitor of c-Met and AXL tyrosine kinases. It suppresses tumor cell growth, invasion, and migration of lung adenocarcinoma.

SBI-797812 is structurally similar to active-site directed inhibitor of NAMPT(NAMPT with EC50 of 0.37 μM).

Chemically modified tetracyclines (CMTs) can inhibit MMPs, but lack antimicrobial activity. Nonantimicrobial derivative of tetracycline called incyclinide (COL-3, CMT-3). Incyclinide (CMT-3) has been shown to experimentally suppress prostate cancer, colon adenocarcinoma and melanoma invasiveness in cell culture and to inhibit tumor growth and metastasis.

PARP1-IN-31 (compound 11f) is a PARP1 inhibitor with an IC₅₀ of 97 nM. It induces apoptosis and inhibits proliferation in lung cancer cell lines (e.g., A549), while upregulating caspase-3 and caspase-9, making it suitable for lung adenocarcinoma research.

UNBS3157 is a novel naphthalimide derivative that is non-hematotoxic and exhibits significant antitumor activity through DNA intercalation and the poisoning of topoisomerase IIalpha. Unlike Amonafide, a related naphthalimide compound that showed activity in Phase II breast cancer trials but did not proceed to Phase III due to dose-limiting myelotoxicity, UNBS3157 has a maximum tolerated dose 3-4 times higher and does not cause hematotoxicity in mice at effective antitumor doses. In vivo models, including (i) L1210 mouse leukemia, (ii) MXT-HI mouse mammary adenocarcinoma, and (iii) human A549 non-small cell lung carcinoma and BxPC3 pancreatic cancer orthotopic models, demonstrate superior efficacy of UNBS3157 compared to Amonafide.

SBI-183 is an orally active QSOX1 inhibitor (Kd: 20 μM). It can inhibit the proliferation and invasion phenotypes of renal carcinoma cell lines, triple-negative breast cancer cell lines, lung adenocarcinoma cell lines, and pancreatic ductal adenocarcinoma. In vivo, SBI-183 suppresses tumor growth in two human renal cell carcinoma xenograft mouse models.

CHI-KAT8i5 is a selective inhibitor of KAT8 with a KD of 19.72 μM. It induces apoptosis (Apoptosis) in a dose-dependent manner. CHI-KAT8i5 can inhibit tumor growth in esophageal squamous cell carcinoma, colon cancer, melanoma, gastric cancer, non-small cell adenocarcinoma, and liver cancer.

Antiproliferative agent-66 (Compound B3) is an antiproliferative compound that induces apoptosis and causes cell cycle arrest. It demonstrates IC50 values ranging from 2.03 to 3.6 µM against SH-SY5Y neuroblastoma, HT-29 colorectal adenocarcinoma, and fibroblasts. Additionally, Antiproliferative agent-66 functions as a microtubule polymerization inhibitor with an IC50 of 0.79 µM.

LIB3S0280 is a potent inhibitor of TBK1, with an IC50 of 493.9 nM. It suppresses TBK1 downstream signaling by reducing the phosphorylation of IκBα and AKT. LIB3S0280 causes G2/M phase arrest and induces apoptosis in pancreatic cancer cells. Notably, it exhibits significant inhibitory effects on pancreatic cancer cell lines with high TBK1 expression, with a 96-hour IC50 value ranging from 6.64-10.98 μM. LIB3S0280 shows potential for research in pancreatic ductal adenocarcinoma (PDAC).

PKM2-IN-10 is a PKM2 inhibitor. It effectively suppresses the proliferation of A549 and HCC1833 cell lines with IC50 values of 3.36 μM and 9.20 μM, respectively. PKM2-IN-10 demonstrates antitumor activity in human non-small cell lung cancer (NSCLC) and mouse lung adenocarcinoma models. It is applicable for research in lung cancer.

CIDD-8633 is a potent inhibitor of DDR2 with an IC50 of 6.105 μM. It significantly suppresses the proliferation of MIA-PaCa-2 and AsPC-1 cells, with IC25 values of 4.0 and 5.5 μM, respectively. Additionally, CIDD-8633 hinders cell migration, arrests the cell cycle, induces apoptosis (apoptosis), and substantially reduces the growth of pancreatic ductal adenocarcinoma (PDAC) tumors. This compound is applicable in pancreatic cancer research, including studies on PDAC.

5-Methyl cromolyn (C5OH) disodium is a cromolyn analog that acts as an S100P inhibitor. It prevents the interaction between S100P and its receptor RAGE, hinders NF-κB activity and cell proliferation, and enhances apoptosis induced by Gemcitabine. In murine models with PDAC, 5-Methyl cromolyn disodium reduces tumor growth and metastasis, thereby extending survival. This compound is suitable for pancreatic cancer research, including studies on pancreatic ductal adenocarcinoma (PDAC).

LAG-3-IN-1 (Compound 11) is an inhibitor of LAG-3 with a dissociation constant (KD) of 0.41 μM. It disrupts the interaction between LAG-3 and MHCII, enhances IFN-γ secretion, and promotes tumor cell killing in co-cultures of PBMCs and cancer cells. LAG-3-IN-1 is applicable in research on cancers such as ovarian cancer, colon adenocarcinoma, and melanoma.

LDHA-IN-10 (Compound HP19) is an inhibitor of lactate dehydrogenase A (LDHA) with an IC50 value of 5.2 μM. It reduces lactate production and ATP levels, inhibiting the proliferation of the pancreatic cancer cell line PANC-1. Additionally, LDHA-IN-10 induces G1/S cell cycle arrest and promotes apoptosis, showing potential for research in pancreatic ductal adenocarcinoma (PDAC).

PDK1-IN-5 is a selective inhibitor of PDK1 that reduces phosphorylation levels to activate PDH. This compound effectively reverses the Warburg effect by increasing acetyl-CoA, reducing lactate, elevating mitochondrial ROS, and subsequently inducing apoptosis, shifting cellular energy metabolism from glycolysis to oxidative phosphorylation. PDK1-IN-5 strongly inhibits tumor growth in vivo without causing systemic toxicity and can be used in research on lung adenocarcinoma, human non-small cell lung adenocarcinoma, gastric cancer, and colorectal cancer.

STAT3-IN-51 is a STAT3 inhibitor that binds directly to the SH2 domain of STAT3. This compound induces apoptosis, ferroptosis, and immunogenic cell death (ICD), enhancing antitumor immunity. It suppresses STAT3 activation (phosphorylation, p-STAT3) and its downstream signaling, while prompting reactive oxygen species (ROS) generation, decreasing Bcl-2 expression, disrupting mitochondrial functions, inhibiting GPX4 activity, and promoting lipid peroxidation. STAT3-IN-51 is applicable in research on colorectal cancer, breast adenocarcinoma, non-small cell lung cancer (NSCLC), and cisplatin-resistant lung adenocarcinoma.

XMU-MP-8 (SKPer1) is a potent molecular glue degrader that targets the oncogenic protein SKP2. It interacts with the F-box domain of SKP2 (Kd≈ 36 μM) and the N-terminal TPR domain of the E3 ligase STUB1 (Kd≈ 2.5 μM), leading to the formation of a stable SKP2-SKPer1-STUB1 ternary complex (Kd≈ 8.9 nM). This interaction triggers the ubiquitination and proteasomal degradation of SKP2. XMU-MP-8 selectively eradicates cancer cells expressing SKP2 and exhibits notable tumor-suppressive effects in vivo along with a favorable safety profile. It is applicable in research on cancers such as non-small cell lung adenocarcinoma (NSCLC) and prostate adenocarcinoma.

PROTACALK degrader-4 (Compound B8) is an ALKPROTAC degrader with a DC50 of 445.25 nM. It demonstrates significant antiproliferative activity against NCI-H2228 and NCI-H3122 cell lines. This compound causes a substantial downregulation of 390 proteins, including IGF-1R and its downstream proteins, such as ERK1/2 and STAT3. PROTACALK degrader-4 is applicable in lung adenocarcinoma research.