osteosarcoma

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

AZ-Dyrk1B-33 (3-(2-Methyl-4-pyrimidinyl)-1-(phenylmethyl)-1H-pyrrolo[2,3-c]pyridine) is a potent and selective Dyrk1B kinase inhibitor with an IC50 of 7 nM.

DC_AC50 is a dual inhibitor of Atox1 and CCS (copper chaperones), aimed at reducing or preventing acquired chemotherapy resistance by inhibiting intracellular copper chaperones. It binds to Atox1 and CCS, thereby reducing cancer cell proliferation and tumor growth.

Raddeanin A is a natural triterpenoid saponin from Cyperus japonicus that inhibits histone deacetylase and is also a potent immunogenic cell death inducer with strong anti-angiogenic and anti-tumor activities.

WM-3835 is a novel and high-specific small molecule inhibitor of Lysine Acetyltransferase 7 (KAT7, MYST2, HBO1) , able to potently suppressed OS cell proliferation and migration, and leads to apoptosis activation.

S 14063 is a potent 5-HT1A receptor antagonist devoid of beta-adrenoceptor blocking properties.

Mifamurtide is a drug against osteosarcoma, is an immunomodulator with antitumor effects.

Deracoxib (SC 46) is a non-steroidal, non-narcotic anti-inflammatory drug. It is also a selective cyclooxygenase-2 inhibitor, and IC50 Value: 70 to 150 μM(inhibition of 3 osteosarcoma cell lines).

Columbamine (Columbamin) shows strong activity with IC5 48.1 μM.Columbamine exerts anti-proliferative and anti-vasculogenic effects on metastatic human osteosarcoma U2OS cells with low toxicity.

TMPyP4 tosylate (TMP 1363) is a quadruplex-specific ligand and telomerase inhibitor that exhibits antitumor effects in osteosarcoma cell lines.

Seocalcitol is an analog of vitamin D, binds vitamin D receptor protein from human osteosarcoma MG-63 cells(Kd : 0.27 nM).

SU1261, an IKK inhibitor, exhibits Ki values of 10 nM for IKKα and 680 nM for IKKβ. It effectively inhibits non-canonical NF-κB signaling in U2OS osteosarcoma cells.

IMPDH2-IN-4 (compound 2d) is a Mycophenolic acid analog and a selective IMPDH2 inhibitor with a Ki of 1.8 μM. It exhibits potent cytotoxic activity against osteosarcoma cancer cell lines. Additionally, IMPDH2-IN-4 demonstrates high affinity for VEGFR-2, CDK2, and IMPDH.

XD23 is a potent osteosarcoma inhibitor that functions by downregulating DKK1 and activating the WNT/β-catenin signaling pathway.

MC3343, a DNMT inhibitor with IC50 values of 5.7 μM for DNMT1 and 1.7 μM for DNMT3a, affects tumor proliferation by blocking osteosarcoma cells in the G1 or G2/M phase and induces osteogenic differentiation by specifically re-expressing genes that regulate this physiological process, and is able to show synergistic effects in combination with adriamycin and cisplatin (CDDP).

TRF2-IN-1 (compound F2) is a potent inhibitor of telomere repeat-binding factor 2 (TRF2). It exhibits antiproliferative activity and induces apoptosis. TRF2-IN-1 binds directly to the TRF2TRFH domain, selectively inhibiting TRF2 protein expression and telomere localization. Additionally, TRF2-IN-1 possesses anticancer properties and shows potential for osteosarcoma research.

Wntpathway inhibitor 5 (Compound 28) is an effective wntpathway inhibitor with an IC50 value of less than 0.003 μM. This compound can suppress various types of cancers such as ovarian teratoma, breast cancer, osteosarcoma, and head and neck squamous cell carcinoma.

OPB-3206 is a selective inhibitor of matrix metalloproteinases (MMPs). It inhibits stromelysin, collagenase, gelatinase A (MMP-2), and gelatinase B (MMP-9) with IC50 values of 7×10^-7 M, 5×10^-6 M, 5×10^-7 M, and 2×10^-6 M, respectively. OPB-3206 reversibly binds to the zinc-binding site of MMPs, blocking the activation of MMP-9 and reducing the degradation of the extracellular matrix, thereby inhibiting tumor lung metastasis. OPB-3206 shows potential for research in osteosarcoma lung metastasis.

Antitumor agent-129 (Compound 68) is a derivative of thiazolidine-4-thione and an inhibitor of osteosarcoma (OS), with an IC50 value of 0.217 μM against OS cell activity. It has a half-life of 73.8 minutes in mouse liver microsomes and exhibits favorable pharmacokinetic properties with an in vivo bioavailability (F) of 115% following intraperitoneal administration. Antitumor agent-129 is a potential candidate for OS research.

Antitumor agent-153 (compound 11b) is an inhibitor of H2A histone ubiquitination, optimized from PRT4165. It can reduce the viability of human osteosarcoma U2OS cells and decrease monoubiquitination of histone H2A, demonstrating anticancer activity.

Anticanceragent 274 (Compound 1) is a Sorafenib analog that inhibits tumor cell growth, with IC50 values of 0.034 μM and 0.042 μM for SaOS-2 and MNNG-HOS cells, respectively. It exhibits low toxicity to normal cells and can be utilized in osteosarcoma and other tumor research.

DDD2 is a selective and efficient VHL-mediated PROTAC degrader specifically targeting NUDT5. It effectively induces substantial degradation of NUDT5. DDD2 consists of the warhead TH10184 and the VHL-recruiting ligand VH032, connected via a saturated aliphatic eight-carbon linker. DDD2 is applicable in cancer research, including studies on lymphocytic leukemia and osteosarcoma.

G721-0282 is an orally active inhibitor of CHI3L1 that reduces the expression of inflammatory proteins and cytokines. It suppresses the activation of the NF-κB signaling pathway, inhibits neuroinflammation, and decreases anxiety-related behaviors. Additionally, G721-0282 significantly curtails the proliferation of osteosarcoma (OS) cells by inhibiting the STAT3 signaling pathway and induces apoptosis in OS cells by upregulating pro-apoptotic protein levels while downregulating anti-apoptotic protein levels. This compound is useful in the study of neuroinflammatory diseases and cancer.

NEP162 is a BRD4 PROTAC degrader with DC50 values of 1.2 μM in SW480 cells and 1.6 μM in U2OS cells. NEP162 exhibits antiproliferative activity, effectively inhibiting tumor growth and inducing apoptosis. It is applicable in research on cancers such as osteosarcoma, colorectal cancer, and non-small cell lung cancer.