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.

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

Disitamab vedotin (RC-48) is a newly developed antibody-active molecule conjugate (ADC) targeting human epidermal growth factor receptor 2 (HER2), consisting of hertuzumab coupled to monomethyl auristatin E (MMAE) via a cleavable linker. Disitamab vedotin showed anti-tumor and anti-proliferative activities in gastric cancer cells with different HER-2 expression levels and inhibited the expression of HER-2 protein in gastric cancer cells.

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

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.

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 .

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.

HSP90-IN-22 (Compound 35) is an Hsp90 inhibitor with antiproliferative activity, exhibiting IC50 values of 3.65 μM in MCF7 breast cancer cells and 2.71 μM in SKBr3 breast cancer cells.

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

PI3K-IN-49 is a powerful inhibitor of PI3K, demonstrating antiproliferative effects on Avg T-47D and Avg SKBR3 cells (WO2023239710A1; example 29) [1].

Anticanceragent 249 (Compound 89) is an inhibitor of Hsp90β, exhibiting an IC50 of 16.5 μM in PC3MM2 cells. It suppresses the proliferation of various cancer cell lines including MCF-7, T47D, MDA-MB-231, MDA-MB-468, and SKBr3, with IC50 values ranging from 1.8 to 5.3 μM. Additionally, Anticanceragent 249 induces apoptosis in MDA-MB-231 cells and demonstrates antitumor activity in mice.

KU004, a potent dual EGFR HER2 inhibitor, exhibits anticancer properties. It inhibits the proliferation of human breast cancer SKBR3 cells by inducing G1 phase arrest. KU004 blocks the activation of HER2, EGFR, and the downstream Akt and Erk pathways, primarily inducing apoptosis (Apoptosis) through the extrinsic pathway. Additionally, KU004 is a novel quinazoline derivative.