tumor cells

Epacadostat (INCB 024360) is an oral-available inhibitor of indoleamine 2, 3-dioxygenase (IDO1), increasing the proliferation and activation of various immune cells and reducing tumor-associated regulatory T cells.

Fedratinib (TG-101348) (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.

Erastin is an ferroptosis activator that acts on the mitochondrial VDAC in a ROS- and iron-dependent manner. Erastin has anti-tumor activity and acts selectively on tumor cells with RAS-carcinogenic mutations. The product is unstable in solution and is recommended to be dispensed now.

SX-682 is a potent, selective and orally bioavailable inhibitor of CXCR1/2 ,has the potential to treat castration-resistant prostate cancer.

MRTX1133 is a KRAS G12D inhibitor (KD=0.2 pM) that is potent, selective, and non-covalent. MRTX1133 exhibits inhibitory activity against KRAS G12D-mutated tumors, but not against KRAS wild-type tumors.

Quizartinib (AC220) is an inhibitor of FLT3 (Kd: 1.6 nM) and demonstrates high selectivity for FLT3 when tested against a panel of 227 additional kinases.

RSL3 (RSL3 1S) is an inhibitor of GPX4, and inhibits system xc- that blocks GSH synthesis (IC50=100 nM). RSL3 is a VDAC-independent activator of ferroptosis that is selective for tumor cells carrying oncogenic RAS.

Elesclomol (STA-4783) is an oxidative stress inducer and a highly lipophilic copper ion carrier. Elesclomol induces apoptosis in tumor cells and is used in copper death related studies. Elesclomol also inhibits FDX1-mediated Fe-S cluster biosynthesis.

Osimertinib (AZD-9291) is an EGFR third-generation inhibitor that inhibits the T790M resistance mutation produced by second-generation EGFR inhibitors with irreversible and oral activity. Osimertinib has antitumor activity for the treatment of EGFR-mutated non-small-cell lung cancer.

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.

Theophylline monohydrate (Quibron) appears to inhibit phosphodiesterase and prostaglandin production, regulate calcium flux and intracellular calcium distribution, and antagonize adenosine. Theophylline monohydrate is a natural alkaloid derivative of xanthine isolated from the plants Camellia sinensis and Coffea arabica. Physiologically, this agent relaxes the bronchial smooth muscle, produces vasodilation (except in cerebral vessels), stimulates the CNS, stimulates the cardiac muscle, induces diuresis, and increases gastric acid secretion; it may also suppress inflammation and improve contractility of the diaphragm.

Perillyl Alcohol is a naturally occurring monoterpene related to limonene with antineoplastic activity. Perillyl alcohol (Isocarveol) inhibits farnesyl transferase and geranylgeranyl transferase, thereby preventing post-translational protein farnesylation and isoprenylation and activation of oncoproteins such as p21-ras, and arresting tumor cells in the G1 phase of the cell cycle.

HLY78 (4-Ethyl-5-methyl-5,6-dihydro-[1,3]dioxolo[4,5-j]phenanthridine) targets the DIX domain of Axin, is an activator of the Wnt/β-catenin signaling pathway and can enhance Axin-LRP6 binding to promote Wnt signaling.

Zingerone (Vanillylacetone) is a nontoxic methoxyphenol isolated from Zingiber officinale, with potent anti-inflammatory, antidiabetic, antidiarrhoeic, antilipolytic, antispasmodic and anti-tumor properties. Zingerone(Gingerone) alleviates oxidative stress and inflammation, down-regulates NF-κB mediated signaling pathways. Zingerone(Gingerone) acts as an anti-mitotic agent, and inhibits the growth of neuroblastoma cells.

Sodium dichloroacetate (BCA) , a specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively, has been shown to derepress a mitochondrial potassium-ion channel axis, trigger apoptosis in cancer cells, and inhibit tumor growth.

1. Berberine (Umbellatine) is a potent oral hypoglycemic agent with beneficial effects on lipid metabolism. 2. Berberine may as a broad-spectrum anti-microbial medicine, a complementary therapeutic agent for HIV/AIDS. 3. Berberine seems to act as an herbal antidepressant and a neuroprotector against neurodegenerative disorders. 4. Berberine is used in histology for staining heparin in mast cells. As a natural dye, berberine has a colour index of 7516. 5. Berberine reduces hepatic fat content in rats with nonalcoholic fatty liver disease; also prevents proliferation of hepatic stellate cells (HSCs), which are central for the development of fibrosis during liver injury. 6. Berberine can ameliorate proinflammatory cytokines-induced intestinal epithelial tight junction damage in vitro, and berberine may be one of the targeted therapeutic agents that can restore barrier function in intestinal disease states. 7. Berberine has antineoplastic effects, including breast cancer, leukemia, melanoma, epidermoid carcinoma, hepatoma, pancreatic cancer, oral carcinoma, tongue carcinoma, glioblastoma, prostate carcinoma and gastric carcinoma, etc.

PARP-2-IN-3 is used as a potent PARP-2 inhibitor (IC50=0.07 μM) with anti-tumor activity that induces apoptosis and necrosis in cancer cells, and can be used for the study of breast cancer.CAS 번호128-52-56-8

CP 461 (UNII-68OJX9I7DT), a specific PDE2A inhibitor, is a novel pro-apoptotic compound that inhibits cyclic GMP phosphodiesterase but not cyclooxygenase-1 or -2. CP 461 inhibits the growth of a variety of human tumor cell lines in vitro and selectively induces apoptosis in cancer cell lines, but not in normal cells.

Rocepafant (LAU8080) is a platelet-activating factor (PAF) antagonist that attenuates hypoxic-ischemic brain damage in neonatal rats.Rocepafant inhibits tumor necrosis factor-Afa-mediated cytotoxicity in mouse L929 tumor cells.

Isomer-Turosteride (Isomer-Turosteride(Isomer-137099-09-3)) is a novel 5 alpha-reductase inhibitor.The antiprostatic effect of Isomer-Turosteride in adult rats is associated with the inhibition of the conversion of T to DHT.Isomer-Turosteride induces a decrease in prostate DHT independent of a secondary increase in T. Isomer-Turosteride has anticancer activity and inhibits the growth of tumor cells. Turosteride has anticancer activity and inhibits the growth of tumor cells. Translated with www.DeepL.com/Translator (free version)

CHK1-IN-4 hydrochloride is a potent inhibitor of checkpoint kinase 1 (chk1). CHK1-IN-4 hydrochloride potently inhibits chk1 phosphorylation in the tumor cells. CHK1-IN-4 hydrochloride has anti-tumor activity.

γ-1-MSH, amide acetate (72629-65-3 free base), a putative hormone in the N-terminal region of the ACTH/beta- endorphin (beta-EP) precursor protein, was studied by RIA with an antiserum against gamma 3-MSH in ACTH-producing mouse pituitary tumor cells, AtT-20/D16v.

Poziotinib hydrochloride irreversibly inhibits EGFR (HER1 or ErbB1), including EGFR mutants, HER2, and HER4, thereby inhibiting the proliferation of tumor cells that overexpress these receptors. It is an orally bioavailable, quinazoline-based pan epidermal growth factor receptor (EGFR or HER) inhibitor with potential antineoplastic activity.

2'-Hydroxychalcone is a drug synthesis intermediate for the synthesis of flavonoids. 2'-Hydroxychalcone loaded in nanoemulsion showed fungicidal activity against Coccidioides parapsilosis in Danio rerio model.2'-Hydroxychalcone induced cytotoxicity through oxidative stress in lipid-loaded Hepg2 cells.2'-Hydroxychalcone inhibited the induction of ICAM-1, VCAM-α, tumor necrosis factor-α, and tumor necrosis factor-alpha as determined by reverse transcription-polymerase chain reaction determined by tumor necrosis factor-alpha induces steady-state transcript levels of ICAM-1, VCAM-1, and E-selectin, and therefore may interfere with the transcription of their genes.

4-[(2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]benzoic acid is a synthetic compound with potent antitumor activity, high efficiency and selectivity against tumor cells. However, it has poor solubility in water and is potentially toxic at high concentrations.

GDC0575 monohydrochloride (ARRY575) is a potent and selective inhibitor of cell cycle checkpoint kinase 1 (Chk1) with an IC50 of 1.2 nM. GDC-0575 specifically binds to and inhibits Chk1; this may result in tumor cells bypassing Chk1-dependent cell cycle arrest in the S and G2/M phases, which permits the cells to undergo DNA repair prior to entry into mitosis.

CCR-11 is a tannin-containing derivative with antimicrobial activity. CCR-11 inhibits the proliferation of B. subtilis and HeLa cells. CCR-11 inhibits bacterial proliferation and bacterial cytoplasmic division by inhibiting FtsZ assembly and GTPase activity. CCR-11 has potential anti-tumor activity and can be used to study breast cancer and pediatric myelodysplasia.

T-cell clones specific for this NY-BR-1 p904 A2 acetate(347142-73-8 free base) can recognize breast tumor cells expressing NY-BR-1.

4,7-DIHYDROXYCOUMARIN is a naturally occurring coumarin derivative found in a variety of plants, including parsley and chamomile. It has been found to inhibit the activity of several enzymes, including cytochrome P450, cyclooxygenase and lipoxygenase. It can also bind to DNA, regulate gene expression, and inhibit cell cycle progression. It can also induce apoptosis in tumor cells and reduce inflammation.

N4-Benzoyl-2′-deoxycytidine is a synthetic nucleoside analog of the natural nucleoside deoxycytidine (dC), a competitive inhibitor of DNA polymerase. In vitro studies have shown that it inhibits replication in viruses, bacteria and eukaryotic cells. It has also been shown to inhibit tumor cell growth in animal models.

9-hydroxy-4-androstene-3,17-dione is a steroid hormone. It has anti-tumor activity and can inhibit the growth of many types of cancer cells, including breast, prostate and lung cancer cells.

TMIFRY8XAG (4-oxo-1,4-dihydroquinoline-2-carboxylic acid) is a derivative of Zerumbone with potential anti-tumor effects towards HeLa cancer cells.

Antitumor agent-19 is a modulator of tumor-associated macrophages with EC50s of 17.18 μM and 18.87 μM in the RAW 264.7 cells and the BMDM cells.

Dimethylaminomicheliolide HCl has potential anti-inflammatory and anti-tumor activity and inhibits the proliferation of glioblastoma cells by targeting pyruvate kinase 2 (PKM2) and reconnecting aerobic cell populations.

Safingol hydrochloride (L-threo-dihydrosphingosine hydrochloride) is a specific inhibitor of protein kinase C. It induces autophagy in solid tumor cells and cancer cell death by inhibiting the PKC and PI3-kinase pathways.BIIB 722 Mesylate is a selective sodium-hydrogen exchange inhibitor. Safingol hydrochloride inhibits PKC and PI3k.

OTS186935 FA is a protein methyltransferase SUV39H2 inhibitor.OTS186935 FA inhibits tumor growth in MDA-MB-231 breast cancer cells and A549 lung cancer cells.

XL-413 is an orally bioavailable cell division cycle 7 homolog (CDC7) kinase inhibitor with potential antineoplastic activity. XL-413 binds to and inhibits the activity of CDC7, which may result in the inhibition of DNA replication and mitosis, the induct

6-HYDROXYLAMINOURACIL is a derivative of uracil, which induces DNA damage and apoptosis in tumor cells and inhibits tumor cell growth in vitro.

STAT3-IN-B9 (B9) is an inhibitor of abnormal STAT3 activation and inhibits the proliferation of tumor cells including MDA-MB-468, MDA-MB-231, and DU145.

DNA polymerase-IN-1, a DNA polymerase inhibitor, exhibited antiproliferative activity against tumor cells with a half-inhibitory concentration (IC50) of 20.7 μM. DNA polymerase-IN-1 inhibited Taq DNA polymerase with an IC50 of less than 250 μM. DNA polymerase-IN-1 was shown to inhibit Taq DNA polymerase by RT- DNA polymerase-IN-1 showed antiretroviral activity in vitro by RT-PCR assay and can be used to study oxidative damage and colorectal cancer.

CUR61414 hydrochloride is a potent and cell permeable inhibitor of Hedgehog signaling pathway (IC50 =100-200 nM). CUR61414 hydrochloride is a small-molecule aminoproline class compound. CUR61414 hydrochloride selectively binds to smoothened (Smo, Ki= 44 nM). CUR61414 hydrochloride can induce cancer cells apoptosis without affecting neighboring non-tumor cells.

LY 195448 (4-(3-(2-Hydroxy-2-phenyl)ethylamino-3-methylbutyl)benzamide) is a substance present in human blood and urine that shows antitumor activity in a mouse tumor model and blocks cells in the mid-stage.

CT-2584 is an anticancer agent that inhibits phospholipid signaling and kills tumor cells through the production of reactive oxygen intermediates. CT-2584 reduces NKEF-B expression in several tumor cell types. CT-2584 reduced tumor growth in SCID mice by causing shunting of ab initio phospholipid biosynthesis from phosphatidylcholine (PC) to phosphatidylinositol (PI) via PA.

LyP-1 acetate is a tumor homing peptide specifically binding to p32 receptors overexpressed in various tumor-associated cells.

[Tyr3]Octreotate is a long peptide compound containing 8 amino acids and is a functional DOTA chelating agent with covalent bonds. [Tyr3]Octreotate binds to transmembrane receptors of SSR2-active NETs and is actively transported into cells by endocytosis, which may increase the required double-stranded DNA breaks and is a potential drug for tumor treatment.

ZEN-3411 is an orally available and potent BET inhibitor that inhibits BRD4(BD1), BRD4(BD2), and BRD4(BD1BD2) and suppresses the growth of tumor cells overproducing BET proteins.

2-Keto-D-galactose inhibits DNA synthesis and inhibits the proliferation of in vitro grown Ehrlich ascites tumor cells.This compound is unstable in powder form and other related salt forms are recommended.

Cenisertib is A potent ATP-competitive multi-kinase inhibitor, showing inhibitory effects on the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5, FLT3, as well as kinase inhibitors of FER and its homolog. Cenisertib inhibits the growth of tumor mast cells (MCS) by inhibiting the activity of several different molecular targets. Cenisertib also inhibits tumor growth in pancreatic, breast, colon, ovarian and lung cancer and leukemia in xenograft models.

(S)-Coriolic acid (13(S)-HODE) is an important intracellular signaling agent, generated by the reaction of linoleic acid with plant and mammalian lipoxygenases, and is involved in cell proliferation and differentiation in various biological systems. (S)-Coriolic acid inhibits the adhesion of tumor cells to the vascular endothelium and down-regulates the expression of IRGpIIb/IIIa receptors at around 1 μM. (S)-Coriolic acid is a metabolite of 15-lipoxygenase (15-LOX), which often acts as an endogenous ligand to activate PPARγ. (S)-Coriolic acid induces mitochondrial dysfunction and airway epithelial damage.

Miclxin (DS37262926) is a novel MIC60 inhibitor that induces apoptosis through mitochondrial stress in mutant tumor cells via β-catenin.Miclxin is a potent inhibitor of mutant β-catenin, which is involved in the Wnt signaling pathway.Miclxin induces β-catenin-dependent apoptosis, leading to mitochondrial damage and loss of mitochondrial membrane. Miclxin has anti-tumor activity and kills tumors by targeting MIC60.