Y-27632 dihydrochloride (Y-27632 2HCl) is an orally potent, ATP-competitive inhibitor of ROCK-I and ROCK-II. Y-27632 dihydrochloride also inhibits isolation-induced apoptosis in mouse prostate stem or progenitor cells.

Tepotinib hydrochloride(1 : x) is an orally bioavailable, mesenchymal-epithelial transition (MET) TKI developed mainly for selected NSCLC patients with METex14 skipping mutations.

AXL-IN-13 is a potent and orally active AXL inhibitor with an IC50 value of 1.6 nM and a Kd value of 0.26 nM.AXL-IN-13 exhibits anticancer activity, reverses TGF-β1-induced epithelial-mesenchymal transition (EMT) and inhibits cancer cell migration and invasion.

DT-6, a potent TGF-β1 inhibitor, impedes M2 macrophage-induced epithelial-to-mesenchymal transition and the invasive migration of cancer cells, thereby showing potential for cancer research applications [1].

CPF-7 (Caerulein precursor fragment), an insulinotropic peptide, promotes insulin secretion and drives epithelial-mesenchymal transition via Snai1 upregulation in PANC-1 ductal cells. Moreover, it induces exocrine plasticity through Ngn3 upregulation, with applications in type 2 diabetes research [1] [2].

CAY10736 is an anticancer compound.1 It inhibits proliferation in a panel of melanoma and breast, pancreatic, and lung cancer cell lines (IC50s = 0.827-9.89 μM). CAY10736 inhibits migration and epithelial-to-mesenchymal transition (EMT) of A375 and B16/F10 melanoma cells in vitro in a concentration-dependent manner. It reduces the viability of spheroid A375 and B16/F10 cells (IC50s = 2.4 and 1.59 μM, respectively) and increases the production of reactive oxygen species (ROS) in these cells in a concentration-dependent manner. CAY10736 (5 mg/kg) reduces tumor growth in B16/F10 melanoma and Lewis lung carcinoma mouse models and an A375 mouse xenograft model.References1. Liu, X., Li, B., Zhang, Z., et al. Synthesis and discovery novel anti-cancer stem cells compounds derived from the natural triterpenoic acids. J. Med. Chem. 61(23), 10814-10833 (2018). CAY10736 is an anticancer compound.1 It inhibits proliferation in a panel of melanoma and breast, pancreatic, and lung cancer cell lines (IC50s = 0.827-9.89 μM). CAY10736 inhibits migration and epithelial-to-mesenchymal transition (EMT) of A375 and B16/F10 melanoma cells in vitro in a concentration-dependent manner. It reduces the viability of spheroid A375 and B16/F10 cells (IC50s = 2.4 and 1.59 μM, respectively) and increases the production of reactive oxygen species (ROS) in these cells in a concentration-dependent manner. CAY10736 (5 mg/kg) reduces tumor growth in B16/F10 melanoma and Lewis lung carcinoma mouse models and an A375 mouse xenograft model. References1. Liu, X., Li, B., Zhang, Z., et al. Synthesis and discovery novel anti-cancer stem cells compounds derived from the natural triterpenoic acids. J. Med. Chem. 61(23), 10814-10833 (2018).

19-Hydroxybufalin is a natural product, inhibits epithelial-mesenchymal transition and attenuates the migration and invasion of PC3 cells.

Anticancer Agent 93, a 4-Hydroxycoumarin derivative, inhibits the invasion and migration of lung cancer cells through modulation of epithelial-mesenchymal transition (EMT) effector expression [1].

Anticancer agent 94, a 4-Hydroxycoumarin derivative, inhibits lung cancer cell invasion and migration by modulating the expression of epithelial-mesenchymal transition (EMT) effectors [1].

FL118 is a novel survivin inhibitor that inhibits cancer stem cell-like properties.FL118 is a novel camptothecin analog with anticancer activity that inhibits epithelial-mesenchymal transition through the Wnt/β-catenin signaling pathway, thereby inhibiting migration and invasion of human breast cancer cells.

PI3K/AKT-IN-2, a dual inhibitor of PI3K and AKT, prevents the epithelial-mesenchymal transition (EMT) and promotes apoptosis. Additionally, it impedes tubulin polymerization.

Antitumor agent-77 inhibits the growth and migration of cancer cells and has anticancer effects. antitumor agent-77 inhibits GPx-4 and enhances COX2-induced iron sagging. antitumor agent-77 activates the intrinsic apoptotic pathway (Bax-Bcl-2-caspase-3) in tumor cells and prevents tumor cell epithelialization. Antitumor agent-77 activates the tumour cell intrinsic apoptotic pathway (Bax-Bcl-2-caspase-3) and blocks the epithelial mesenchymal transition (EMT) process.

Sotevtamab (16B5), a humanized IgG2 monoclonal antibody (mAb) targeting clusterin, acts as an inhibitor of the epithelial to mesenchymal transition, making it a valuable agent for cancer research [1] [2] [3].

EMT Inhibitor-2, targeting both CYP3A4 testosteron and CYP2C9, exhibits inhibitory effects with IC50 values of 49.72 and 5.54 μM, respectively. Furthermore, it effectively impedes the epithelial-mesenchymal transition (EMT) process, induced by immunocyte-released agents like IL-1β and TGF-β.

KY-05009 is a chemical compound that effectively suppresses TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in human lung adenocarcinoma cells, reduces TNIK protein expression and the transcriptional activity of Wnt target genes, and promotes apoptosis in cancer cells, displaying anti-cancer properties. Furthermore, it functions as an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with a Ki of 100 nM.

1. Ecliptasaponin A (Echinocystic acid-3-o-glucoside) has protective effects against the pulmonary fibrosis induced by bleomycin via reducing the oxidative stress, lung tissue inflammation, and the subsequent epithelial-mesenchymal transition.

CT1-3 is a potent anti-cancer agent. CT1-3 regulates the JNK/Bcl-2/Bax/XIAP pathway, which induces mitochondria-mediated apoptosis. CT1-3 regulates the E-cadherin/Snail axis to inhibit epithelial mesenchymal transition (EMT) potentials in human cancer cells (HCCs) and suppresses tumourigenesis. CT1-3 has anti-tumour effects in mouse models and does not show significant hepatotoxicity or nephrotoxicity.

Phthalazinone pyrazole is potent, selective, and orally bioavailable inhibitor of Aurora-A kinase. Aurora-A is overexpressed in a variety of tumor types and displays oncogenic activity.

Sulindac (Sulindac sulfoxide) is a sulfinylindene derivative prodrug with potential antineoplastic activity. Converted in vivo to an active metabolite, sulindac, a nonsteroidal anti-inflammatory drug (NSAID), blocks cyclic guanosine monophosphate-phosphodiesterase (cGMP-PDE), an enzyme that inhibits the normal apoptosis signal pathway; this inhibition permits the apoptotic signal pathway to proceed unopposed, resulting in apoptotic cell death.

Methacycline hydrochloride (Rondomycin) is a broad-spectrum semisynthetic antibiotic related to TETRACYCLINE but excreted more slowly and maintaining effective blood levels for a more extended period.

CPUL1, a TrxR inhibitor, exhibits proliferation-inhibitory and anti-metastatic effects on A549 cells by modulating epithelial-mesenchymal transition (EMT) through the induction of ROS-mediated ERK/JNK signaling, achieved by inhibiting TrxR1 enzyme activity. The efficacy of CPUL1 is enhanced when used in conjunction with α-Lipoic Acid or Dithiodipropionic acid [1].

Sulindac (sodium) (MK-231) is an orally active nonsteroidal anti-inflammatory agent. Sulindac (sodium) is used to reduce pain, swelling, and joint stiffness from arthritis. Sulindac is also used for the research of arthritis of the spine, gouty arthritis. Sulindac (sodium), as an immunomodulatory agent, can downregulate PD-L1 through the blockade of NF-κB signaling and modulates the response of pMMR colorectal cancer (CRC) to anti-PD-L1 immunotherapy, inhibits the development and progression of colorectal cancer CRC. Sulindac (sodium) also inhibits TGF-β1- induced epithelial-mesenchymal transition (EMT) and suppresses lung cancer cell migration and invasion via downregulation of SIRT1 [1] [2].

β-Carboline-1-carboxylic acid is an alkaloid that has been found in P. quassioides and has diverse biological activities. It reduces LPS-induced increases in MCP-1, TNF-α, IL-6, and IL-1β levels in RAW 264.7 cells when used at a concentration of 15 µg/ml and inhibits the epithelial-to-mesenchymal transition (EMT) induced by TGF-β1 in A549 cells. β-Carboline-1-carboxylic acid induces cytotoxicity in CT26.WT, K562, and SGC-7901 cells (IC50s = 14.96, 22.11, and 19.7 µg/ml, respectively) but not HepG2 or A549 cells (IC50s = 36.41 and 41.51 µg/ml, respectively). It also inhibits cAMP phosphodiesterase with an IC50 value of 96 µM.

EW-7195 is a selective and potent inhibitor of ALK5 (TGFβR1) with an IC50 value of 4.83 nM.EW-7195 has an affinity for ALK5 that is more than 300-fold higher than that of p38α.EW-7195 has an inhibitory effect on TGF-β1-induced Smad signaling, epithelial mesenchymal transition (EMT), and breast cancer metastasis to the lungs.

Escin IA (Escin IA;Aescin IA) is a triterpene saponin isolated from horse chestnut, which inhibits HIV-1 protease with IC50 values of 35 μM. Escin IA has anti-TNBC metastasis activity, and its action mechanisms involved inhibition of epithelial-mesenchymal transition process by down-regulating LOXL2 expression[1][2].

hCAIX-IN-8 (compound 7i) is a highly potent and selective inhibitor of hCAIX, demonstrating potent inhibitory activity against CAIX with an IC50 value of 0.024 μM. It also exhibits inhibitory activity against CAII and CAVA with IC50 values of 1.99 μM and 1.10 μM, respectively. Furthermore, hCAIX-IN-8 exhibits anti-proliferative effects and low toxicity. It effectively reduces the occurrence of epithelial-to-mesenchymal transitions and promotes apoptosis. Additionally, hCAIX-IN-8 effectively inhibits cell migration and colonization potential [1].

ML327 is a MYC blocker. ML327 can also de-repress E-cadherin transcription and reverse Epithelial-to-Mesenchymal Transition (EMT).

STAT3-IN-15, a potent and orally active inhibitor targeting STAT3, effectively combats idiopathic pulmonary fibrosis (IPF) by hindering STAT3 phosphorylation. Additionally, it impedes TGF-β1-induced migration and deformation of epithelial cells and prevents epithelial-mesenchymal transition (EMT), offering a multifaceted approach against IPF.

CAY10735 is an anticancer compound.1 It inhibits proliferation in a panel of melanoma and breast, pancreatic, and lung cancer cell lines (IC50s = 0.674-11.56 μM). CAY10735 inhibits migration of and the epithelial-to-mesenchymal transition (EMT) in A375 and B16/F10 melanoma cells in vitro in a concentration-dependent manner. It reduces the viability of spheroid A375 and B16/F10 cells (IC50s = 3.04 and 1.24 μM, respectively) and increases production of reactive oxygen species (ROS) in these cells in a concentration-dependent manner. CAY10735 (5 mg/kg) reduces tumor growth in B16/F10 melanoma and Lewis lung carcinoma mouse models and an A375 mouse xenograft model.References1. Liu, X., Li, B., Zhang, Z., et al. Synthesis and discovery novel anti-cancer stem cells compounds derived from the natural triterpenoic acids. J. Med. Chem. 61(23), 10814-10833 (2018). CAY10735 is an anticancer compound.1 It inhibits proliferation in a panel of melanoma and breast, pancreatic, and lung cancer cell lines (IC50s = 0.674-11.56 μM). CAY10735 inhibits migration of and the epithelial-to-mesenchymal transition (EMT) in A375 and B16/F10 melanoma cells in vitro in a concentration-dependent manner. It reduces the viability of spheroid A375 and B16/F10 cells (IC50s = 3.04 and 1.24 μM, respectively) and increases production of reactive oxygen species (ROS) in these cells in a concentration-dependent manner. CAY10735 (5 mg/kg) reduces tumor growth in B16/F10 melanoma and Lewis lung carcinoma mouse models and an A375 mouse xenograft model. References1. Liu, X., Li, B., Zhang, Z., et al. Synthesis and discovery novel anti-cancer stem cells compounds derived from the natural triterpenoic acids. J. Med. Chem. 61(23), 10814-10833 (2018).

Antitumor agent-78 inhibits GPx-4 and elevates COX2, leading to ferroptosis. antitumor agent-78 activates the tumor cell intrinsic apoptotic pathway (Bax-Bcl-2-caspase-3) and inhibits the epithelial mesenchymal transition (EMT) process in tumor cells. Antitumor agent-78 exhibits antitumor effects and inhibits the growth and migration of cancer cells.

Irigenin mediates its antimetastatic effect by specifically and selectively blocking the α9β1 and α4β1 integrin binding sites on the C-C loop of the Extra Domain A domain. It can sensitize TRAIL-induced apoptosis by enhancing the expression of pro-apoptotic molecules in gastric cancer cells and has anti-cancer effects.

trans-Trimethoxyresveratrol (MR-3), a natural methoxylated analog of resveratrol, inhibits breast Y cell invasiveness by downregulation of PI3K/Akt and Wnt/β-catenin signaling cascades and reversal of epithelial-mesenchymal transition.

1. Oroxylin A (Baicalein 6-methyl ether) has various anti-tumor effects including apoptosis, cell cycle arrest, drug-resistant reversion. 2. Oroxylin A possesses abilities of inhibiting the ATRA-induced IL-6 production via modulation of LAP/LIP/CHOP in leukemia cell lines, which could providing a therapeutic strategy for RAS. 3. Oroxylin A inhibits UCP2s triggers the MPTP opening, and promotes the apoptosis in CaCo-2 cells; uncoupling protein 2 plays a key role in mitochondrial apoptotic pathway. 4. Oroxylin A inhibits N1ICD translocating to the nucleus and binding to epithelial-mesenchymal transition-related transcription factor Snail, thus suppressing the invasion and migration of MCF-7 cells. 5. Oroxylin A improves the sensitivity of K562/ADM cells by increasing apoptosis in leukemic cells and decreasing the expression of CXCR4 and PI3K/Akt/NF-κB pathway, and probably served as a most promising agent for CML treatment.

3,6-Dihydroxyflavone suppresses the epithelial-mesenchymal transition in breast cancer cells by inhibiting the Notch signaling pathway.

Batatasin III inhibits cancer migration and invasion by suppressing epithelial to mesenchymal transition and FAK-AKT signals and possesses anti-cancer activities. Batatasin III has a long-term inhibitory effect on whole-plant growth and shows germination