mda-468

CADD522 (MFCD00167693) is a potent inhibitor of runt-related transcription factor-2 (RUNX2)-DNA binding with an IC50 of 10 nM, with antitumor activity

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

Rapamycin (AY 22989) is a natural product of macrolides, an mTOR inhibitor with specificity (HEK293 cells: IC50=0.1 nM). Rapamycin has immunosuppressive activity and induces autophagy.

AZD8055 is an ATP-competitive mTOR inhibitor (IC50: 0.8 nM in MDA-MB-468 cells). It is ~1,000-fold selective for mTOR over all PI3K isoforms.

GW9662 (TIMTEC-BB SBB006523) is a PPARγ antagonist (IC50=3.3 nM) with selectivity. GW9662 can be used to study the pathogenesis of metabolic diseases, such as obesity and diabetes, by inhibiting the activity of PPARγ. GW9662 can be used to study the pathogenesis of inflammatory diseases, such as atherosclerosis and rheumatoid arthritis. GW9662 has anti-tumor effect.

S63845 is a selective myeloid leukemia 1(MCL1) inhibitor that binds to human MCL1 with a Kd of 0.19 nM.

Talazoparib (LT-673) is a new-type PARP inhibitor (IC50: 0.58 nM), It similarly binds to PARP1/2 (Kis: 1.2/0.85 nM).

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.

Eicosapentaenoic Acid is an ω-3 fatty acid and an inhibitor of fatty acid synthase (FASN). Eicosapentaenoic Acid promotes DNA demethylation in the reexpression of the tumor suppressor gene CCAAT/ enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates the RAS/ERK/C/EBPβ pathway in U937 leukemia cells through demethylation of the CpG island of H-RAS intron 1. Eicosapentaenoic Acid promotes the relaxation of vascular smooth muscle cells and vasodilation.

Antiproliferative agent-22 is an anticancer compound that shows antiproliferative activity on MCF-7, MDA-MB-231, and MDA-MB-468 cells.Antiproliferative agent-22 is used in cancer research.

GW 610 is an antitumor benzothiazole that shows growth-inhibitory activity against several cancer cell lines. In MCF-7 and MDA 468 human cancer cell lines, potent antiproliferative activity (growth inhibition (GI50) < 0.1 nM) was observed.

Demethoxydeacetoxypseudolaric acid B analog has potent activities against HMEC-1, HL-60, A-549, MB-MDA-468, BEL-7402, HCT116, and Hela cells with IC50s ranging from 0.136 to 1.162 μM. and is semi-synthesized by efficient routines from Pseudolaric acid B.

PROTAC PIN1 degrader-1, a targeted PROTAC for PIN1, effectively degrades PIN1 protein in MDA-MB-468 triple-negative breast cancer cells with a DC50 value of 0.018 μM. This compound is utilized in tumor research.

GPX4-IN-15 (Compound C1) is an inhibitor of GPX4, demonstrating an inhibition rate of 19.8% at a concentration of 1 μM. This compound effectively inhibits the proliferation of cancer cell lines MDA-MB-468, BT-549, and MDA-MB-231, with IC50 values of 0.86 μM, 0.96 μM, and 0.48 μM respectively.

ERK1 2 inhibitor 13 (Compound 21y) is an orally bioavailable ERK inhibitor that targets ERK1 and ERK2, with IC50 values of 91.71 nM and 97.87 nM, respectively. It effectively suppresses the proliferation of cancer cell lines MCF-7, 4T1, MDA-MB-468, and HCC1970 with IC50 values of 0.67 μM, 2.76 μM, 2.15 μM, and 1.68 μM, respectively. Additionally, it inhibits cancer cell migration, induces apoptosis and autophagy in MCF-7 cells, and demonstrates anti-tumor and anti-metastatic effects in a 4T1 xenograft mouse model.

Antitumor agent-195 (compound 16c) is a dual-targeting agent that simultaneously targets STAT3 and NQO1. At a concentration of 1 μM, it significantly inhibits the phosphorylation of STAT3 at the Tyr705 site and effectively induces apoptosis in MDA-MB-231 and MDA-MB-468 breast cancer cells. As a substrate of NQO1, Antitumor agent-195 markedly increases ROS production, causing severe DNA damage in a dose-dependent manner. It also demonstrates strong antitumor properties in MDA-MB-231 xenograft models.

MS9024 is a degrader of DNA methyltransferase 1 (DNMT1), facilitating its degradation in HCT116 cells via the ubiquitin-proteasome pathway, with a DC50 of 35 nM (DC50 values are 254 nM in MDA-MB-468 and 101 nM in H1299). Additionally, MS9024 inhibits DNMT1 with an IC50 of 0.43 μM.

(S)-PI3K-IN-2 is the enantiomer of PI3K-IN-2, functioning as a ΡΙ3Κβ/δ inhibitor with IC50 values of 0.198 and 0.282 μM, respectively. It can also inhibit the phosphorylation of AKT(ser473) in MDA-MB-468 cells, with an IC50 of 27 nM.

JNN-5 is an effective JAK2 selective inhibitor with an IC50 of 0.41 nM. It demonstrates strong antiproliferative activity in TNBC cell lines [MDA-MB-468, MDA-MB-213, HCC70, MDA-MB-157].

CDK7-IN-28 (CDK7-1276) is a potent CDK7 inhibitor with an IC50 of less than 5 nM. It exerts antiproliferative effects on the MDA-MB-468 cell line by blocking the cell cycle and inhibiting DNA replication.

Thailanstatin A cyclohexane diamine formic is an analogue of Spliceostatin. It effectively inhibits the proliferation of various cells, including N87 (IC50 = 0.33 μM), BT474 (IC50 = 0.34 μM), MDA-MB-361-DYT2 (IC50 = 0.88 μM), and MDA-MB-468 (IC50 = 0.27 μM). Additionally, Thailanstatin A cyclohexane diamine formic can be utilized as a drug-linker conjugate in ADC (antibody-drug conjugate) molecules.

PROTACFAKdegrader 2 (Compound F2) is a PROTAC degrader targeting focal adhesion kinase (FAK), with DC50 values for total FAK and phosphorylated p-FAK of 27.72 nM and 60.1 nM, respectively. It inhibits the viability of cancer cell lines 4T1, MDA-MB-231, MDA-MB-468, and MDA-MB-435, with IC50 values ranging from 0.73 to 5.84 μM. Additionally, PROTACFAKdegrader 2 counteracts multidrug resistance (MDR) by inhibiting the AKT and ERK signaling pathways. In HCT/8 xenograft mouse models, it demonstrates anti-tumor efficacy.

Zelavespib formic (PU-H71 formic) is a potent Hsp90 inhibitor, exhibiting an IC50 value of 51 nM in MDA-MB-468 cells.

YD277 is a small molecule derived from ML264, a KLF5 inhibitor that elicits cytotoxic effects in colon cancer cell lines. YD277 significantly induced G1 cell cycle arrest and apoptosis in MDA-MB-231 and MDA-MB-468 TNBC cells, independent of KLF5 inhibitio