miapaca-2

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

KRASG12D-IN-5 (Compound 241) is an orally active KRAS(G12D) inhibitor with an IC50 of 11 nM. It demonstrates potent anticancer activity without significant cytotoxicity to BxPC-3 cells (wild-type), KRAS-mutant AsPC-1 cells (G12D), and MIAPaCa-2 cells (G12C), with CC50 values of 10.37, 0.76, and 0.3 μM, respectively. KRASG12D-IN-5 is applicable in cancer studies, including lung, pancreatic, and colorectal cancers.

9β-Hydroxyhexahydrocannabinol is a synthetic cannabinoid derivative. It exhibits cytotoxicity against various tumor cell lines, including HCT-116, MCF-7, K562, MIAPaCa-2, PANC-1, A549, PC-3, and SW-620, with IC50 values ranging from 15.23 to 33.74 μM. This compound can be utilized in cancer research.

S100A2-p53-IN-1 (compound 51), an inhibitor of S100A2-p53 interactions, targets S100A2, a Ca 2+ binding protein involved in cell signaling and commonly upregulated in pancreatic cancer, and effectively inhibits the growth of the MiaPaCa-2 pancreatic cancer cell line, showing a growth inhibition (GI 50) range of 1.2-3.4 μM [1].

HIF-1α-IN-2 hydrochloride is a potent HIF-1α inhibitor exhibiting anticancer activity, with IC50 values of 28 nM in MDA-MB-231 cells and 15 nM in MiaPaCa-2 cells, effectively suppressing HIF-1α expression by inhibiting transcription and protein translation [1].