skbr3

Buformin hydrochloride (NSC-528218) is a potent AMPK activator,an oral antidiabetic drug of the biguanide class. Buformin delays the absorption of glucose from the gastrointestinal tract increases insulin sensitivity and glucose uptake into cells and inhibits synthesis of glucose by the liver. Biguanides may antagonize the action of glucagon, thus reducing fasting glucose levels.

PK11000 is a p53 targeting compound, has anti-tumor activities through activation of unstable p53.

TMBIM6 antagonist-1 (BAX-inhibitor-1) is a bax inhibitor

Disitamab vedotin (RC48) is an antibody-drug conjugate (ADC) and a HER2-targeted cytotoxic agent, consisting of an anti-HER2 monoclonal antibody conjugated to MMAE via a cleavable linker, used for the treatment of HER2-expressing solid tumors including gastric cancer, breast cancer, and urothelial carcinoma.

Calcitriol (1,25-Dihydroxyvitamin D3) is a metabolite of vitamin D and a vitamin D receptor (VDR) agonist (IC50=0.4 nM). Calcitriol increases intestinal absorption of calcium and phosphorus, and increases bone resorption with parathyroid hormone.

Lapatinib (GW572016) is an inhibitor of ErbB2 and EGFR (IC50=9.2/10.8 nM) with oral activity. Lapatinib has antitumor activity and can be used to treat advanced or metastatic breast cancer with HER2 overexpression.

Myricetin (Cannabiscetin) is a natural flavonoid and MEK1 inhibitor. Myricetin has hypoglycemic, antioxidant, hepatoprotective, anti-tumor and anti-inflammatory activities.

Nordihydroguaiaretic acid (NDGA) is a natural product, extracted from Pole Fork Kelaroa, and is a lipoxygenase (5-LOX) inhibitor (IC50=8 μM). Nordihydroguaiaretic acid possesses antioxidant and free radical scavenging properties.

C75 is a fatty acid synthase (FASN) inhibitor (IC50 = 35 μM in PC3 cells) with cell permeability and the ability to activate CPT1A. This compound possesses antitumor activity and is commonly used in cancer-related experimental research.

Dxd (OQM5SD32BQ) is a potent DNA topoisomerase I inhibitor (IC50= 0.31 μM). Dxd was used as a conjugate drug for HER2-targeted ADCs.

Exatecan-amide-cyclopropanol is an anticancer agent that potently inhibits the proliferation of SK-BR-3 breast cancer cells with an IC50 value of 0.12 nM, and it also suppresses the growth of U87 glioblastoma cells with an IC50 value of 0.23 nM,Exatecan-amide-cyclopropanol demonstrate robust cytotoxic potential across distinct cancer cell lines. Exatecan-amide-cyclopropanol is primarily used in research aimed at understanding DNA-topoisomerase inhibition mechanisms and their therapeutic implications in oncology.

Ligustroside is a natural product of phenolic glycosides from olive plants, which has antioxidant and anti-inflammatory activities. Ligustroside can up-regulate the mRNA expression of SIRT1, CREB1 and GPx1 in SH-SY5Y-APP695 cells. At the same time, the production of nitric oxide (NO) was significantly inhibited in RAW264.7 macrophages stimulated by lipopolysaccharide (LPS). Ligustroside has potential application value in cardiovascular and metabolic diseases related research.

28-Deoxonimbolide is a nimbolide-type limonoid natural product isolated from the seeds of Azadirachta indica. In vitro, it induces apoptosis in tumor cells (e.g., HL-60), with mechanisms involving mitochondrial pathways and potentially the participation of death receptor signaling. It is commonly used in studies of anticancer mechanisms.

DBCO-NHCO-PEG4-amine is a cleavable ADC linker used to conjugate MMAE and antibody (e.g., DBCO-VCpAB MMAE and DBCO-TRX MMAE with EC50s of 280 nM and 22 nM in SKBR3 cells, respectively) [1].

CZY43 is an HER3 degrader that effectively induces degradation of HER3 in breast cancer SKBR3 cells in a dose- and time-dependent manner. It efficiently inhibits HER3-dependent signaling and cancer cell growth, outperforming Bosutinib.

Hsp90-IN-39 (Compound 16t) is an HSP90 inhibitor with significant selectivity for the HSP90α isoform. It demonstrates notable antiproliferative activity across various cancer cell lines, including MCF-7, HCT116, SKBr3, K562, and A549. Hsp90-IN-39 is applicable for cancer research.

Hsp90-IN-38 (compound 20m) is an inhibitor of HSP90 (heat shock protein). It demonstrates a strong binding affinity to HSP90 with a Kd of 87 nM. The compound inhibits ATPase activity with an IC50 of 0.13 μM. Hsp90-IN-38 also shows inhibitory effects on HCT116, MCF-7, SKBr3, K562, and A549 cells with IC50 values of 0.187, 0.072, 0.105, 0.403, and 0.031 μM, respectively.

AKT1-IN-9 (4) is a selective inhibitor of the AKT1(E17K) mutation, exhibiting EC50 values of 9 nM in LAPC4-CR cells and 995 nM in SkBr3 cells.

DBCO-NHCO-PEG4-amine TFA is a PROTAC linker (PROTACLinker) belonging to the PEG class. It is a cleavable ADC linker used for conjugating MMAE and antibodies, such as in DBCO-VCpAB MMAE and DBCO-TRX MMAE, with EC50 values of 280 nM and 22 nM against SKBR3 cells, respectively.

4-Iodo-SAHA (1k), an orally active inhibitor of both class I and class II histone deacetylase (HDAC), exhibits EC50 values of 1.1, 0.95, 0.12, 0.24, 0.85, and 1.3 μM for Skbr3, HT29, U937, JA16, and HL60 cell lines, respectively. This compound holds potential for cancer research purposes [1].

CP-654577 is a selective p185(ErBB2) kinase inhibitor that reduces the level of the activated form of mitogen-activated protein kinase in SKBR3 human breast cancer cells.

Potent EGFR Degrader (DC50 values are 39.2 nM for wild-type EGFR in OVCAR8 cells and 736 nM for Exon20Ins mutated EGFR in HeLa cells). Also degrades HER2. Comprises the EGFR inhibitor lapatinib (Cat. No. 6811) joined by a linker to a von Hippel-Lindau (VHL) recruiting ligand. Inhibits proliferation of HER2-driven breast cancer cell lines (IC50 = 102 nM for SKBr3 cells).

1. Furanodienone has effects on MCF-7 cells are mediated, at least in part, by inhibiting ERα signaling. 2. Furanodienone inhibits EGFR/HER2 signaling pathway in BT474 and SKBR3 cells, the effect is specifically dependent on the expression of HER2 but not EGFR .

HSP90-IN-22 is a potent HSP90 inhibitor targeting the ATP-binding site. It induces the degradation of oncogenic client proteins, used for broad-spectrum cancer and drug resistance research.