paca-2

MM41 is a human telomeric and gene promoter DNA quadruplex stabilizer with an IC50 of <10 nM against the MIA PaCa-2 pancreatic cancer cell line.

Gemcitabine (LY188011) is a synthetic cytosine nucleoside derivative and an inhibitor of DNA synthesis. Gemcitabine has antitumor and antimetabolic activities. Gemcitabine induces autophagy and apoptosis.

Adagrasib (MRTX849) is an orally active and selective covalent inhibitor of KRAS G12C. Adagrasib binds to the GDP state of the inactive conformation of KRAS G12C and inhibits KRAS and its downstream signaling. Adagrasib exhibits inhibitory activity against KRAS G12C mutant tumors.

3-Methyladenine (3-MA) is a PI3K inhibitor that selectively inhibits class IB PI3Kγ (IC50 = 60 μM) and class III VPS34 (IC50 = 25 μM). 3-Methyladenine inhibits autophagy.

Bleomycin sulfate is a glycopeptide antibiotic with antitumor activity. It is commonly used as a DNA-damaging agent and DNA synthesis inhibitor. It functions by inducing DNA strand breaks without affecting RNA strands. Bleomycin sulfate is widely used in cancer research and for establishing pulmonary fibrosis animal models.

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

Sodium Oxamate (Oxamic acid sodium salt) is an LDH inhibitor that specifically inhibits LDHA. Sodium Oxamate has antitumor activity and induces cell cycle arrest and apoptosis.

3-Hydroxypyridine exhibits inhibitory activity against DNA topoisomerase 2-beta (Topo IIβ) and HIV-1 replication in Sup-T1 cells, making it useful for studying the HIV-1 virus.

LXH254 is a B/C RAF inhibitor with IC50 values of 0.2 nM and 0.07 nM for inhibiting BRAF and CRAF.

BN82002 (CDC25 Phosphatase Inhibitor I) is a synthetic inhibitor of CDC25 phophatases

GW284543 (UNC10225170) is a selective inhibitor of MEK5.

C75 is an inhibitor synthetic fatty-acid synthase (FASN) and inhibits prostate cancer cells PC3 (IC50: 35 μM).C75 increases CPT1 activity and reduces DIO.

Chromomycin A3 is an antibiotic produced by Streptomyces sp that binds to gc-rich DNA sequences in the presence of divalent cations and inhibits DNA replication and transcription; it is also used as a fluorescent DNA stain and assay; and it has anticancer activity against diseases such as Hodgkin's, lung adenocarcinomas, melanomas, and breast cancer.

Oxythiamine (Hydroxythiamin) is an antivitamin of thiamine and a transketolase (TK) inhibitor. Oxythiamine inhibits cancer cell proliferation and induces cell cycle arrest. Oxythiamine has potential anticancer activity, inhibits non-oxidative synthesis of ribose, and induces apoptosis.

Tributyrin (Glyceryl tributyrate), a neutral short-chain fatty acid triglyceride, is a stable and rapidly absorbed prodrug of Butyric Acid. It diffuses through biological membranes and is metabolized by intracellular lipases, releasing effective butyrate directly into cells in vivo, exhibiting potent proapoptotic, antiproliferative, and differentiation-inducing effects.

Amsilarotene (TAC101) inhibits the phosphorylation of retinoblastoma gene product (RB) and increases the presence of 2 cyclin-dependent kinases (CDK) inhibitors resulting in cell cycle arrest. This agent also causes a cytotoxic decline in the thymidylate synthase and cyclin A expression.

Alisertib (MLN 8237) is a specific Aurora A inhibitor (IC50: 1.2 nM). The selectivity of Alisertib(MLN 8237) is >200-fold higher for Aurora A than Aurora B.

HIF-1α-IN-2 is a novel and highly potent HIF-1α inhibitor with anticancer and antitumor activity that inhibits the expression of HIF-1α and VEGF in a dose-dependent manner and inhibits cell migration.

3-Deazaneplanocin A (DZNep) is a dual inhibitor of histone methyltransferase (EZH2) and S-adenosylhomocysteine hydrolase (AHCY) with antipoxidative activity that inhibits hepatic, renal, peritoneal, and airway fibrosis by inducing proteasomal degradation of its targets and reducing toxicity in animal models.

TEPP-46 (ML265) is an activator of pyruvate kinase M2 (PKM2) (AC50=92 nM), selective for PKM1, PKL and PKR. TEPP-46 has antitumor activity.

Royleanone possesses cytotoxic activity against the human pancreatic cancer cell line MIA PaCa-2.

HedgehogIN-7 (Compound 8g), a purine derivative, acts as an inhibitor of the Hedgehog signaling pathway by reducing the expression of Hedgehog genes and inhibiting signal transmission. This compound exhibits significant cytotoxicity and selectivity towards Mia-PaCa-2 pancreatic cancer cells that are dependent on the Hedgehog pathway, making it useful for research in pancreatic cancer.

MEK/RAF-IN-1 (Compound 16b) serves as an inhibitor targeting both MEK and RAF, demonstrating potent efficacy with IC 50 values reported at 28 nM for MEK1, and 3 nM for both BRAF and BRAFV600E. This compound exhibits significant antitumor capabilities, effectively curbing cell proliferation in vitro in MIA PaCa-2 (G12C KRAS), HCT116 (G13D KRAS), and C26 (G12D KRAS) cells. Furthermore, MEK/RAF-IN-1 significantly restricts tumor growth in xenograft mouse models employed in the study of colorectal cancer.