PANC-1

Metarrestin (ML246) is a first-in-class perinucleolar compartment inhibitor with a favorable PK profile, which effectively suppresses metastasis. Metarrestin disrupts the nucleolar structure and inhibits RNA polymerase (Pol) I transcription, at least in part by interacting with the translation elongation factor eEF1A2.

E3330 is a potent and selective APE1(Ref-1) inhibitor, which suppressed NF-kappa B DNA-binding activity.

NSAH (2-hydroxy-N'-[(E)-(2-hydroxynaphthalen-1-yl)methylidene]benzohydrazide) is a nonnucleoside inhibitor of human ribonucleotide reductase (hRR).with cell-free IC50 of 32 μM and cell-based IC50 of ~250 nM, respectively.

Triacetylresveratrol (Acetyl-trans-resveratrol) has anti-cancer activity,it inhibits the phosphorylation of STAT3 and NFκB, down-regulates Mcl-1, and up-regulates Bim and Puma in pancreatic cancer cells.

Supinoxin (RX-5902) is an orally active inhibitor of phosphorylated-p68 RNA helicase and a potent first-in-class anti-cancer agent, inducing cell apoptosis and inhibiting the growth of TNBC cancer cell lines (IC50s: 10 nM - 20 nM).

PRIMA-1 (NSC-281668) is a mutant p53 reactivator that induces apoptosis and inhibits the growth of human tumors with mutant p53.

BMS-191011 (BMS-A) is an activator of large-conductance calcium-activated potassium (BKCa) channels ,effective in stroke models

Metformin (1,1-Dimethylbiguanide) is an AMPK activator with blood-brain barrier permeability. Metformin may improve glycemic control by increasing insulin sensitivity and decreasing intestinal glucose uptake, and is commonly used in type 2 diabetes research.

LL-37, Human acetate is a 37-residue, amphipathic, cathelicidin-derived antimicrobial peptide, which exhibits a broad spectrum of antimicrobial activity.

3-arylisoquinolinamine derivative is a compound with antitumor activity.

Gemcitabine hydrochloride (LY 188011 hydrochloride) is a synthetic cytosine nucleoside derivative and an inhibitor of DNA synthesis. Gemcitabine has antitumor and antimetabolic activities. Gemcitabine induces autophagy and apoptosis.

Dapagliflozin (BMS-512148) is a selective sodium-glucose co-transporter subtype 2 (SGLT2) inhibitor with antihyperglycemic activity.

LB100 (LB-100) is a water soluble protein phosphatase 2A (PP2A) inhibitor.

CRT0066101 is a potent and orally active protein kinase D inhibitor with low-nanomolar activity against PKD1, PKD2, and PKD3, while also inhibiting PIM2, CRT0066101 demonstrates significant anti-inflammatory efficacy in lipopolysaccharide-induced lung injury models as well as anticancer activity, supporting its use in inflammation and oncology research.

HGC652 is a molecular glue targeting E3 ubiquitin ligase TRIM21 (KD=0.061 µM), promoting its formation of a ternary complex with NUP98 to induce degradation of NUP155 and nuclear pore complex proteins. HGC652 inhibits proliferation and induces cell death in multiple cancer cell lines.

AFMK (Formyl-N-acetyl-5-methoxykynurenamine) is an active metabolite of Melatonin with antioxidant and free radical scavenging activity. AFMK is a modulator of apoptosis and improves the anti-tumor effect of Gemcitabine in PANC-1 cells.

HM90822 is a novel synthetic apoptotic protein (IAP) antagonist that induces apoptosis in human pancreatic cancer cells through proteasome-dependent degradation of IAPs containing the BIR2/3 structural domain.HM90822 inhibits the expression of XIAP and cIAP1/2 proteins in HM822-sensitive Panc-1 and BxPC-3 cells, induces ubiquitylation of IAPs and promotes induces IAP ubiquitination and promotes proteasome-dependent IAP degradation.

Nic-15 (compound 4n) serves as an anti-constrictive agent targeting the low vascular characteristics of pancreatic tumors. These characteristics enable cancer cells to adapt to the nutrient-deficient tumor microenvironment and develop resistance to treatment. Nic-15 modulates the PI3K/Akt/mTOR pathway and alleviates ER stress induced by Gemcitabine. It significantly inhibits migration and colony formation in MIA PaCa-2 and PANC-1 pancreatic cancer cells. When used in combination with Gemcitabine, Nic-15 effectively addresses resistance issues in pancreatic tumors. In xenograft models in vivo, Nic-15 notably enhances the efficacy of Gemcitabine.

(Rac)-Glutipyran is a broad-spectrum GLUT inhibitor targeting both GLUT1 and GLUT3. This compound inhibits glucose uptake and significantly impedes the growth of various cancer cells, particularly demonstrating substantial inhibition of PANC-1 cell growth (IC50=1.8 μM) and glucose uptake (IC50=0.13 μM).

AKT-IN-25 (Compound 14a) is an inhibitor of Akt that prevents the phosphorylation of Akt, thereby hindering the PI3K/Akt/mTOR signaling pathway. It arrests the cell cycle at the G1 phase, inhibits the migration of PANC-1 cells, and suppresses the proliferation of cancer cells PANC-1, PATU-T, and SUIT-2, with IC50 values of 3.05, 1.32, and 3.85 μM, respectively.

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.

JR5-26B is an orally active apoptosis (apoptosis) inducer. It induces cell death via copper-mediated apoptosis and necroptosis (necroptosis). JR5-26B exhibits antiproliferative activity against MIA PaCa-2, PANC-1, PAN02, SU.86.86, and KPC-2 cells, with IC50 values of 0.6, 4.4, 8.0, 1.1, and 3.4 μM, respectively.

XSJ-10 is an HDAC inhibitor containing a RAS/RAF protein interference unit, with IC50 values of 0.05 μM in PANC-1 cells and 0.04 μM in HT-29 cells. It effectively induces cancer cell apoptosis and tumor inhibition by strongly suppressing the RAS-RAF-MEK-ERK signaling pathway and HDAC3 acetylation levels.

EpskA21 is an inhibitor of the PI3K/AKT signaling pathway and is capable of suppressing the proliferation of cancer cells including MCF-7, A549, MIA-PaCa-2, Panc-1, and HepG2, with an IC50 range of 1.3-7.24 μM. It can inhibit cell migration, arrest the cell cycle at the G2/M phase in MCF-7 cells and the S phase in MIA-PaCa-2 cells, and induce apoptosis in both MCF-7 and MIA-PaCa-2 cells. EpskA21 also leads to mitochondrial dysfunction.