ductal

Mycro 3 is potent and selective for c-Myc in whole cell assays.

BRD7552 is an inducer of transcription factor PDX1, which increases insulin expression. BRD7552 increases PDX1 expression in mouse αTC cells but not βTC cells.

GOT1 inhibitor-1 (GOT1 inhibitor 2c) is a novel, potent and non-covalent inhibitor of glutamate oxaloacetate transaminase 1 (GOT1) with an IC50 of 8.2 uM.

Almorexant (ACT 078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively.

Almorexant hydrochloride (ACT 078573 hydrochloride) is an orally active dual orexin receptor antagonist that blocks the intracellular Ca2+ signaling pathway and, to a certain extent, blocks the excitatory effects of methamphetamine. Almorexant hydrochloride Induces apoptosis and can be used to study sleep disorders.

Uridine triphosphate (UTP) is a purine nucleotide P2U receptor agonist with potential use in lung cancer treatment. By activating P2Y2 receptors, it enhances the proliferation of human cancerous ductal epithelial cells. Additionally, UTP induces fibrotic responses in cardiac fibroblasts through P2Y2 receptor activation and prolongs the action potential duration of guinea pig papillary muscles via the P2Y2 purinergic receptor.

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.

FAK-IN-22 (Compound 26) is an inhibitor of FAK, JAK3, and Aurora B, with IC50 values of 50.94 nM, 9.99 nM, and 0.49 nM, respectively, effectively suppressing tumorigenesis and metastasis in pancreatic ductal adenocarcinoma (PDAC). It inhibits proliferation in PANC-1 cells with an IC50 of 0.15 μM. FAK-IN-22 induces apoptosis and G2/M phase arrest in PANC-1 cells by inhibiting the FAK/PI3K/Akt signaling pathway.

ROCK/HDAC-IN-2 (Compound C-9) is a dual inhibitor of ROCK/HDAC, characterized by IC50 values of 0.185 µM for HDAC6, 0.8 µM for ROCK1, and 0.7 µM for ROCK2. It effectively induces apoptosis and mitochondrial membrane potential alterations in cancer cells and demonstrates notable antitumor activity, making it useful for research in pancreatic ductal adenocarcinoma (PDAC) and triple-negative breast cancer (TNBC).

CDK2/FLT4/PDGFRA-IN-1 (Compound 4a) is a potent inhibitor of CDK2/cyclin A, FLT4 (VEGFR3), and PDGFRA, with IC50 values of 1.672, 0.554, and 0.629 μM respectively. This compound demonstrates significant antiproliferative effects on cancer cells, including lung cancer EBC-1, pancreatic ductal adenocarcinoma AsPC-1, and colorectal cancer HT-29 cells. Additionally, CDK2/FLT4/PDGFRA-IN-1 can induce apoptosis in these cancer cells.

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).

PI3K-IN-60 (Compound 34) is a selective PI3Kγ inhibitor for studying autoimmune diseases and cancers such as multiple sclerosis, breast cancer, and pancreatic ductal adenocarcinoma.

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.

Fentomycin is a dual-functional lipolysis-targeting chimera (LIPTAC). It specifically targets plasma membrane phospholipids and, following endocytosis, activates lysosomal iron, which promotes phospholipid oxidation and degradation leading to ferroptosis. This compound effectively kills primary sarcoma and pancreatic ductal adenocarcinoma cells, particularly those subpopulations that are metastatic, drug-resistant, and exhibit high CD44 expression. Fentomycin shows antitumor activity.

KRASG12D-IN-7 is a selective inhibitor of KRASG12D. It exhibits strong binding affinity to KRASG12D in both GDP-bound and GTP-bound states, with Kd values of 1.12 nM and 1.86 nM, respectively. This compound inhibits the proliferation of KRASG12D-bearing AsPC-1 cells with an IC50 of 10 nM and disrupts MAPK signaling. In AsPC-1 cells, KRASG12D-IN-7 induces G0/G1 phase arrest and apoptosis (apoptosis), and significantly suppresses colony formation. The inhibitor is applicable for research on cancers with KRASG12D mutations, particularly pancreatic ductal adenocarcinoma (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).

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).

BAS00602705 is an E-cadherin inhibitor that operates by disrupting the transmembrane interactions of E-cadherin molecules within the adhesion complex without permanently altering E-cadherin expression levels. It significantly suppresses the formation of invadopodia in pancreatic cancer cells. BAS00602705 can be used to investigate anti-invasive therapeutic strategies for cancers characterized by dysregulation of invadopodia activity mediated by E-cadherin, such as pancreatic ductal adenocarcinoma [PDAC].

(R)-DRF053 is a CDK inhibitor that suppresses Cdk5 and facilitates the formation of ductal progenitor β cells. Additionally, (R)-DRF053 inhibits the uptake of Dil-ox-LDL and the expression of the CD36 gene in U937 cells induced by advanced glycation end-products (AGEs).

EBET-1593 is a BETPROTAC degrader that facilitates the ubiquitination and degradation of BET proteins. It serves as the primary payload and can be utilized in the synthesis of ADCs, such as 84-EBET, which exhibits antitumor activity against pancreatic ductal adenocarcinoma.

Rintatolimod is a TLR3 agonist that serves dual functions by inhibiting the activity of pancreatic ductal adenocarcinoma cells and enhancing anti-tumor immune responses.

QD325 is a potent redox modulator for the Treatment of Pancreatic Ductal Adenocarcinoma. Nascent RNA sequencing following treatments with QD325 revealed induction of stress responses in the nucleus, endoplasmic reticulum, and mitochondria of pancreatic ca

TW9 is a dual inhibitor of bromodomain 2 (BD2) in bromodomain-containing protein 4 (BRD4) and histone deacetylase 1 (HDAC1; IC50s = 0.074 and 0.29 μM, respectively).1It is selective for BD2 over BD1 in BRD4 (IC50= 0.72 μM) and for HDAC1 over HDAC2 (IC50= 2.5 μM). TW9 (50 nM) induces apoptosis in, and inhibits proliferation of, MIA PaCa-2 pancreatic cancer cells. It induces cell cycle arrest at the G1phase in HPAC pancreatic cancer cells when used at a concentration of 2 μM. TW9 acts synergistically with gemcitabine to reduce the viability of HPAC cells. 1.Zhang, X., Zegar, T., Weiser, T., et al.Characterization of a dual BET/HDAC inhibitor for treatment of pancreatic ductal adenocarcinomaInt. J. Cancer147(10)2847-2861(2020)

Aspulvinone O is a fungal metabolite that has been found in P. variotti and has antioxidant and anticancer activities.1,2 It scavenges 2,2-diphenyl-1-picrylhydrazyl radicals in a cell-free assay (IC50 = 11.6 μM).1 Aspulvinone O inhibits aspartate transaminase 1 (GOT1; Kd = 3.32 μM) and is cytotoxic to PANC-1, AsPC-1, and SW1990 pancreatic cancer cells (IC50s = 20.54-26.8 μM).2 It reduces the oxygen consumption rate (OCR) and induces apoptosis in SW1990 cells. Aspulvinone O (2.5 and 5 mg/kg) reduces tumor growth in an SW1990 mouse xenograft model. |1. Zhang, P., Li, X.-M., Wang, J.-N., et al. New butenolide derivatives from the marine-derived fungus Paecilomyces variotii with DPPH radical scavenging activity. Phytochem. Lett. 11, 85-88 (2015).|2. Sun, W., Luan, S., Qi, C., et al. Aspulvinone O, a natural inhibitor of GOT1 suppresses pancreatic ductal adenocarcinoma cells growth by interfering glutamine metabolism. Cell Commun. Signal. 17(1), 111 (2019).