FOXM1 Inhibitor

Thiostrepton is a thiazole antibiotic which selectively inhibits FOXM1. FOXM1 binds to YAP/TEAD complex. YAP/TEAD/FOXM1 complex binding at regulatory regions of genes governing cell cycle may impact cell proliferation.

FDI-6 is an inhibitor of FOXM1. FDI-6 binds directly to FOXM1 protein, to displace FOXM1 from genomic targets in MCF-7 breast cancer cells, and induce concomitant transcriptional down-regulation.

RCM-1 is a forkhead box M1 (FOXM1) inhibitor with an EC₅₀ of 0.72 μM in U2OS cells. RCM-1 blocks the nuclear localization and increased the proteasomal degradation of FOXM1. RCM-1 can be used for asthma and other chronic airway diseases research.

STL001 is potent and selective FOXM1 inhibitor. STL001 induces the translocation of nuclear FOXM1 to the cytoplasm and promotes its autophagic degradation. STL001 sensitizes human cancers to a broad-spectrum of cancer therapies.

YX-2-107 is a PROTAC (IC₅₀= 4.4 nM) that selectively degrades CDK6. YX-2-107 effectively inhibits RB phosphorylation and FOXM1 expression in vitro and inhibits the development of Ph⁺ ALL in rats. YX-2-107 can be used in the study of Ph chromosome-positive (Ph⁺) acute lymphoblastic leukemia (ALL).

ARF(26-44), cell-permeable acetate is a cell-penetrating peptide derived from a specific amino acid sequence of the p14ARF tumor suppressor protein. As a functional inhibitor of FoxM1, ARF(26-44) cell-permeable acetate shows significant anti-tumor activity in the treatment of mouse hepatocellular carcinoma (HCC), significantly increasing tumor cell apoptosis and reducing tumor cell proliferation and angiogenesis. ARF(26-44), cell-permeable acetate can be used in research on tumor therapy.

FOXM1-IN-3 is a potent FOXM1 inhibitor. FOXM1-IN-3 downregulates FOXM1 expression at protein and mRNA levels, suppressing downstream effectors CCNB1 and CDC25. FOXM1-IN-3 induces G2/M cell cycle arrest and apoptosis in colorectal cancer cells. FOXM1-IN-3 inhibits colony formation and cell migration in colorectal cancer cells. FOXM1-IN-3 targets the cancer stem cell phenotype in colorectal cancer cells, reducing cancer stem cell marker expression. FOXM1-IN-3 reduces tumor growth in a zebrafish xenograft model. FOXM1-IN-3 can be used for the research of colorectal cancer.

5-HT7 modulator-1 hydrochloride is a selective 5-HT₇ receptor antagonist with a K_i of 92 nM. 5-HT7 modulator-1 hydrochloride blocks 5-HT₇ receptor signaling to reduce FOXM1, phosphorylated FOXM1, cyclin B1, and cdc25B levels. 5-HT7 modulator-1 hydrochloride acts as an antiproliferative, clonogenic inhibitor, and cell cycle inhibitor that induces G₂/M arrest, reduces G₀/G₁ population. 5-HT7 modulator-1 hydrochloride can be used for the research of triple-negative breast cancer.

FOXM1-IN-1 is a potent FOXM1 inhibitor with an IC₅₀ value of 2.65 µM. FOXM1-IN-1 shows antiproliferative activity. FOXM1-IN-1 decreases the the expression of FOXM1, PLK1, CDC25B protein.

Siomycin A is a thiopeptide antibiotic and is a Forkhead box M1(FOXM1) selective inhibitor without affecting other members of the Forkhead box family. Siomycin A has anti-tumor and promotes apoptosis.

ARF(26-44), cell-permeable is a cell-penetrating peptide derived from a specific amino acid sequence of the p14ARF tumor suppressor protein. As a functional inhibitor of FoxM1, ARF(26-44) cell-permeable shows significant anti-tumor activity in the treatment of mouse hepatocellular carcinoma (HCC), significantly increasing tumor cell apoptosis and reducing tumor cell proliferation and angiogenesis. ARF(26-44), cell-permeable can be used in research on tumor therapy.

KC12 is an inhibitor for FOXM1 transcription factor. KC12 exhibits cytotoxicity in cancer cell MDA-MB-231 with an IC₅₀ of 6.13 µM.

Hsp70/FoxM1-IN-1 (Compound 7d) is a potent heat shock protein 70 (Hsp70) and Forkhead box M1 (FoxM1) dual inhibitor. Hsp70/FoxM1-IN-1 demonstrates significant antiproliferative and pro-apoptotic effects in multiple solid tumor models (e.g., breast, colorectal cancer), particularly for tumors co-overexpressing Hsp70/FoxM1.

NOSH-aspirin (NBS-1120) is an orally active hybrid molecule that releases nitric oxide and hydrogen sulfide. NOSH-aspirin inhibits pancreatic cancer cell proliferation and induces apoptosis. NOSH-aspirin inhibits cancer cell growth and suppresses NF-κB and FoxM1 in a mouse model of pancreatic cancer. NOSH-aspirin also alleviates motor deficits and dopaminergic neuron degeneration in a rat model of Parkinson's disease. NOSH-aspirin reduces neuroinflammation caused by microglial and astrocytic activation. NOSH-aspirin can be used in research on cancers such as pancreatic cancer and neurological diseases such as Parkinson's disease.

LASSBio-2052 is a derivative of N-acylhydrazone with antitumor activity against hepatocellular carcinoma (HCC). LASSBio-2052 inhibits HCC cells HepG2 and Hep3B, with IC₅₀ of 18 and 41 μM. LASSBio-2052 arrests the cell cycle at G2/M phase, through downregulation of FOXM1. LASSBio-2052 induces apoptosis in HCC cells.

FOXM1-IN-2 is a FOXM1 inhibitor, with antineoplastic activity.

STL427944 is a potent and selective FOXM1 inhibitor. STL427944 has the potential for the research of overcoming tumor chemoresistance.

Gangaleoidin is a FOXM1 inhibitor with an IC₅₀ of 2.8 μM. Gangaleoidin inhibits interaction between FOXM1’s DNA-binding domain and target DNA sequence, downregulates FOXM1 and downstream target gene CCNB1 at the transcriptional level. Gangaleoidin suppresses proliferation of FOXM1-overexpressing breast cancer cells. Gangaleoidin can be used for the research of breast cancer.