sarcoma

Osteosarcoma-IN-D14 is an inhibitor of migration and invasion of osteosarcoma cells mediated by p53, regulating EMT-related genes.

Tazemetostat (EPZ6438) is a histone methyltransferase EZH2 inhibitor (IC50=11 nM) that is orally active, selective, and SAM-competitive. Tazemetostat exhibits antitumor activity and may be used for the treatment of epithelioid sarcoma follicular lymphoma.

Sitravatinib (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα β, PDGFR, and Axl.

PF-562271 is an effective ATP-competitive, reversible inhibitor of FAK(IC50=1.5 nM) and Pyk2 kinase(IC50=13 nM).

PF-562271 hydrochloride (PF-562271 HCl) is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM in cell-free assays, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs.

Potent BRD9 degrader. Selectively binds BRD9 and elicits near complete degradation of BRD9 at nanomolar concentrations. Inhibits growth of synovial sarcoma cells in vitro and tumor progression in a synovial sarcoma xenograft mouse model.

FR 900490 is an immunoactive substance produced by a fungus Discosia sp. F-11809. In vitro FR-900490 restores the colony forming units in culture (cfu-c) in bone marrow cells, which were suppressed by immunosuppressive factor obtained from the serum of sa

[Ala2] Endothelin-3, human is a linear analog of endothelin-3 (ET-3) with Ala substituting for Cys residues. ET-3, a vasoactive peptide produced by human rhabdomyosarcoma cell lines and not expressed in non-muscle-origin human sarcoma cell lines, serves as a paracrine factor by promoting endothelial cell migration [1] [2].

Daunorubicin (Daunomycin) citrate, a potent anti-tumor anthracycline antibiotic, acts as a topoisomerase II inhibitor. It effectively inhibits DNA and RNA synthesis, diminishes cancer cell viability, and promotes apoptosis and necrosis. This cytotoxic compound is utilized in researching a range of cancers, such as leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, and Wilms' tumor, as well as infections [1] [2] [4] [5].

SHP2-IN-22, a potent SHP2 allosteric inhibitor, exhibits an IC50 value of 17.7 nM and effectively suppresses proliferation, migration, and invasion in MIA PaCa-2 pancreatic cancer cells. This compound is utilized in the study of Kirsten rat sarcoma viral oncogene (KRAS) mutant cancer research [1].

Seclidemstat (SP-2577) is an effective LSD1 inhibitor, with a mean IC50 of 127 nM.

Ulefnersen sodium is an inhibitor that targets the synthesis of RNA-binding protein fused-in sarcoma (FUS), and it is applicable for research in amyotrophic lateral sclerosis (ALS).

Bulleyanin shows strong inhibition of mouse ehrlich ascites carcinoma (ECA), mouse sarcoma S-180, and mouse liver ascites.

Trabectedin (Ecteinascidin 743) has potent antitumor activity and the potential for soft tissue sarcoma and ovarian cancer research. Trabectedin inhibits cell growth of MX-1, MCF7 and MCF7 DXR cells with IC50 values of 0.1 nM, 1.5 nM and 3.7 nM, respectively.

Compound 20, also known as LANA-DNA-IN-2, is an inhibitor of the interaction between latency-associated nuclear antigen (LANA) and DNA. It is employed in the study of Kaposi's sarcoma-associated herpesvirus (KSHV) infection [1].

Amikhellin HCl, an antimitotic drug, is a synthetic water-soluble derivative of khellin, an alkaloid extracted from seeds of Ammi Visnaga. Amikhellin has been used so far mostly as a vasodiator. Amikhellin binds to double-stranded DNA by an intercalation process. It inhibits the DNA-polymerase from murine sarcoma leukemia virus.

CBP-1008 is a dual-ligand peptide-drug conjugate (PDC) with MMAE, targeting folate receptor (FRα) and TRPV6. It exhibits high binding affinity to FRα and low affinity to TRPV6. CBP-1008 shows antitumor activity and can be utilized for research in advanced solid tumors such as colorectal cancer, breast cancer, non-small cell lung cancer, ovarian cancer, adrenocortical carcinoma, and follicular dendritic cell sarcoma.

DC 86M is an antitumor antibiotic isolated from the culture broth of Streptomyces luteogriseus DO-86. DC 86M is active against Gram-positive and Gram-negative bacteria and experimental murine sarcoma 180.

YW3-56 is an inhibitor of protein arginine deiminase 2 (PAD2) and PAD4 (IC50s = 0.5-1 and 1-5 μM, respectively).1It inhibits the growth of U2OS osteosarcoma cells (IC50= ~2.5 μM) in a p53-dependent mannerviainduction of SESN2 and subsequent inhibition of mTORC1. YW3-56 (10 mg kg) reduces tumor growth in an S-180 murine sarcoma tumor model. It also inhibits tumor growth in the 1883 MDA-MB-231 breast cancer bone metastasis mouse xenograft model.2 1.Wang, Y., Li, P., Wang, S., et al.Anticancer peptidylarginine deiminase (PAD) inhibitors regulate the autophagy flux and the mammalian target of rapamycin complex 1 activityThe Journal of Biological Chemisty287(31)25941-25952(2012) 2.Wang, S., Chen, X.A., Hu, J., et al.ATF4 gene network mediates cellular response to the anticancer PAD inhibitor YW3-56 in triple-negative breast cancer cellsMol. Cancer Ther.14(4)877-888(2015)

NSC635437 acts as an inhibitor of the EWS-FLI1 oncoprotein in Ewing's sarcoma.

RETRA is an agent of anticancer that acts by exerting anticancer activity in Ewing's sarcoma cells independent of their TP53 status.

Lucialdehyde C (Lucidal) exhibits potent cytotoxicity against LLC, T-47D, Sarcoma 180, and Meth-A tumor cells with ED(50) values of 10.7, 4.7, 7.1, and 3.8 microg/ml, respectively.

PMEDAP is a potent inhibitor of Moloney murine sarcoma virus (MSV)-induced tumor formation and mortality, as well as a human immunodeficiency virus (HIV) replication inhibitor with anti-murine cytomegalovirus (MCMV) activity.

Porcn-IN-2 (Example 107) is a potent Wnt pathway inhibitor with an IC50 of 0.05 nM, applicable in cancer research including sarcoma, melanoma, skin cancer, hematological tumors, lymphoma, carcinoma, and leukemia [1].