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Osteosarcoma Inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (2) Apoptosis (7) Autophagy (2) CDK (4) COX (3) Cytochrome P450 (2) E1/E2/E3 Enzyme (1) Endogenous Metabolite (3) Fungal (1) Histone Acetyltransferase (1) IGF-1R (1) IKK (1) Isotope-Labeled Compounds (1) LIM Kinase (LIMK) (1) MDM-2/p53 (2) Mitophagy (2) MMP (2) NF-κB (2) PAI-1 (1) PDGFR (1) PI3K (1) RANKL/RANK (4) Toll-like Receptor (TLR) (4) Tyrosinase (1) VEGFR (1) Wnt (4) β-catenin (4)
By Research Areas:	Cancer (30) Infection (1) Inflammation/Immunology (12) Metabolic Disease (5)

Inhibitors & Agonists

Peptides

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Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-122714

SK-216	PAI-1	Cancer
SK-216 is a plasminogen activator inhibitor-1 (PAI-1) inhibitor that acts as an anti-metastatic agent for human osteosarcoma and inhibits lung metastasis of human osteosarcoma .

HY-162121

Antitumor agent-129	Others	Cancer
Antitumor agent-129 (Compound 68) is a thiazolidin-4-one sulfone derivative and an Osteosarcoma (OS) inhibitor with an IC₅₀ value of 0.217 μM, a half-life of 73.8 min (mouse liver microsome) and an excellent pharmacokinetic profile (in vivo bioavailability F = 115%, intraperitoneal administration). Antitumor agent-129 is a potential candidate for OS research .

HY-169296

IMPDH2-IN-4	VEGFR CDK	Cancer
IMPDH2-IN-4 (compound 2d), a Mycophenolic acid (HY-B0421) analogue, is a selective IMPDH2 inhibitor with a K_i of 1.8 μM. IMPDH2-IN-4 exhibits good cytotoxic activity against osteosarcoma cancer cell lines. IMPDH2-IN-4 possesses a high affinity for VEGFR-2, CDK2, and IMPDH .

HY-162970

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

HY-124144

MMV667492	Endogenous Metabolite	Cancer
MMV667492 is a potent Ezrin inhibitor with the activity to inhibit the invasion phenotype of osteosarcoma cells. MMV667492 exhibited potent anti-Ezrin activity in all biological assays and its compound properties were superior to NSC305787. MMV667492 was able to exhibit morphological defect phenotypes associated with Ezrin inhibition in zebrafish embryos. MMV667492 also showed the ability to inhibit the lung metastasis of osteosarcoma cells that highly expressed Ezrin .

HY-123369

BMI-1026	CDK Apoptosis	Cancer
BMI-1026 is a cyclin-dependent kinase 1 (Cdk1) inhibitor with IC₅₀ of 2.3 nM. BMI-1026 induces apoptosis by arresting the G2-M phase .

HY-P3730

Cdk2/Cyclin Inhibitory Peptide I	CDK	Cancer
Cdk2/Cyclin Inhibitory Peptide I (Tat-LFG), a CDK2 inhibitor, kills U2OS osteosarcoma cells in a dose-dependent manner .

HY-P3731

Cdk2/Cyclin Inhibitory Peptide II	CDK	Cancer
Cdk2/Cyclin Inhibitory Peptide II (Tat-LDL), a CDK2 inhibitor, kills U2OS osteosarcoma cells in a dose-dependent manner .

HY-169053

SU1261	IKK NF-κB	Cancer
SU1261 is an IKK inhibitor with K_i values of 10 nM and 680 nM for IKKα and IKKβ, respectively. SU1261 can inhibit non-canonical NF-κB signaling in U2OS osteosarcoma cells .

HY-161417

LIMK-IN-2	LIM Kinase (LIMK)	Cancer
LIMK-IN-2 (Compound 52) is an LIMK inhibitor. LIMK-IN-2 can suppress the cell migration of osteosarcoma and cervical cancer cells, demonstrating potential anti-angiogenic activity .

HY-12579

RO 2468	MDM-2/p53	Cancer
RO 2468 is a potent, orally active and selective p53-MDM2 inhibitor. RO 2468 has anti-proliferative active. RO 2468 suppresses c growth in SJSA1 osteosarcoma models without obvious toxicity .

HY-N7385

Nudol	MMP Apoptosis	Cancer
Nudol is a phenanthrene compound that has anti-cancer activity. Nudol inhibits cell proliferation, induces cell apoptosis. Nudol inhibits MMP-2M and MMP-9 activity (K_i: 988.9 nM, 1.76 μM, respectively). Nudol can be used in the research of cancers, such as osteosarcoma .

HY-12941

AM-7209	MDM-2/p53	Cancer
AM-7209 is a potent and selective MDM2-p53 interaction inhibitor with a K_d of 38 pM. AM-7209 inhibits the MDM2 amplified SJSA-1 osteosarcoma cell line with an IC₅₀ of 1.6 nM. AM-7209 shows antitumor activities .

HY-N6611

Chimaphilin	IGF-1R	Infection Inflammation/Immunology Cancer
Chimaphilin is an IGF-1R inhibitor (IC₅₀: 0.086 μM). Chimaphilin has antifungal, antioxidant and anticancer activities. Chimaphilin inhibits the growth of both drug-sensitive and drug-resistant osteosarcoma cell lines. Chimaphilin can induce cancer cell apoptosis. Chimaphilin is a main component of pyrola .

HY-163518

Antitumor agent-153	E1/E2/E3 Enzyme	Cancer
Antitumor agent-153 (compound 11b) is an optimized H2A histone ubiquitination inhibitor based on PRT4165 (HY-19817). Antitumor agent-153 inhibits the viability of human osteosarcoma U2OS cells and reduces histone H2A monoubiquitination, exhibiting anticancer activity .

HY-N0153

Naringin Maximum Cited Publications 13 Publications Verification Naringoside	Cytochrome P450 Autophagy Mitophagy Endogenous Metabolite	Inflammation/Immunology Cancer
Naringin is a major flavanone glycoside obtained from tomatoes, grapefruits, and many other citrus fruits. Naringin exhibits biological properties such as antioxidant, anti-inflammatory, and antiapoptotic activities. Naringin also inhibits proliferation and invasion and induces apoptosis in human osteosarcoma cells by inhibiting zinc finger E-box binding homeobox 1 (Zeb1) .

HY-N0153R

Naringin (Standard) Naringoside (Standard)	Endogenous Metabolite Cytochrome P450 Mitophagy Autophagy	Inflammation/Immunology Cancer
Naringin is a major flavanone glycoside obtained from tomatoes, grapefruits, and many other citrus fruits. Naringin exhibits biological properties such as antioxidant, anti-inflammatory, and antiapoptotic activities. Naringin also inhibits proliferation and invasion and induces apoptosis in human osteosarcoma cells by inhibiting zinc finger E-box binding homeobox 1 (Zeb1) .

HY-N2112

Glaucocalyxin A 2 Publications Verification	PI3K Akt Apoptosis	Cancer
Glaucocalyxin A, an ent-kauranoid diterpene from Rabdosia japonica var., induces apoptosis in osteosarcoma by inhibiting nuclear translocation of Five-zinc finger Glis 1 (GLI1) via regulating PI3K/Akt signaling pathway. Glaucocalyxin A has antitumor effect .

HY-144653

PDGFR-IN-1	PDGFR Apoptosis	Cancer
PDGFR-IN-1 (compound 7m) is a potent and orally active PDGFR (platelet-derived growth factor receptor) inhibitor, with IC₅₀ values of 2.4 and 0.9 nM for PDGFRα and PDGFRβ, respectively. PDGFR-IN-1 displays robust antitumor effects and low toxicity, and can be used to study osteosarcoma .

HY-134901

WM-3835 3 Publications Verification	Histone Acetyltransferase Apoptosis	Cancer
WM-3835 is a potent and high-specific HBO1 (KAT7 or MYST2) inhibitor and binds directly to the acetyl-CoA binding site of HBO1. WM-3835 activates apoptosis while inhibits osteosarcoma (OS) cell proliferation, migration and invasion. WM-3835 has antitumor activity and potently inhibits pOS-1 xenograft growth in mice .

HY-B0012

Pamidronic acid 1 Publications Verification	RANKL/RANK Toll-like Receptor (TLR) Wnt β-catenin	Metabolic Disease Inflammation/Immunology Cancer
Pamidronic acid, the second-generation nitrogen-containing bisphosphonate, is an inhibitor of bone loss. Pamidronic acid significantly inhibits subchondral bone loss in early osteoarthritis by upregulating the expression of OPG in cartilage and subchondral bone, and inhibiting the expression of RANKL and MMP-9 in both tissues, as well as TLR-4 in cartilage, thereby alleviating cartilage degeneration. Additionally, Pamidronic acid can inhibit the signaling of Wnt and β-catenin, and is applicable for research on osteoporosis and osteosarcoma .

HY-B0012B

Pamidronic acid sodium	RANKL/RANK Toll-like Receptor (TLR) Wnt β-catenin	Metabolic Disease Inflammation/Immunology Cancer
Pamidronic acid sodium, the second-generation nitrogen-containing bisphosphonate, is an inhibitor of bone loss. Pamidronic acid sodium significantly inhibits subchondral bone loss in early osteoarthritis by upregulating the expression of OPG in cartilage and subchondral bone, and inhibiting the expression of RANKL and MMP-9 in both tissues, as well as TLR-4 in cartilage, thereby alleviating cartilage degeneration. Additionally, Pamidronic acid sodium can inhibit the signaling of Wnt and β-catenin, and is applicable for research on osteoporosis and osteosarcoma .

HY-17372

Rofecoxib 3 Publications Verification MK 966	COX	Inflammation/Immunology Cancer
Rofecoxib is a potent, specific and orally active COX-2 inhibitor, with IC₅₀s of 26 and 18 nM for human COX-2 in human osteosarcoma cells and Chinese hamster ovary cells, with a 1000-fold selectivity for COX-2 over human COX-1 (IC₅₀ > 50 μM in U937 cells and > 15 μM in Chinese hamster ovary cells).

HY-B0012A

Pamidronate disodium 1 Publications Verification CGP 23339A	RANKL/RANK Toll-like Receptor (TLR) Wnt β-catenin	Metabolic Disease Inflammation/Immunology Cancer
Pamidronate disodium, the second-generation nitrogen-containing bisphosphonate, is an inhibitor of bone loss. Pamidronate disodium significantly inhibits subchondral bone loss in early osteoarthritis by upregulating the expression of OPG in cartilage and subchondral bone, and inhibiting the expression of RANKL and MMP-9 in both tissues, as well as TLR-4 in cartilage, thereby alleviating cartilage degeneration. Additionally, Pamidronate disodium can inhibit the signaling of Wnt and β-catenin, and is applicable for research on osteoporosis and osteosarcoma .

HY-B0012AR

Pamidronate (disodium) (Standard)	RANKL/RANK Toll-like Receptor (TLR) Wnt β-catenin	Metabolic Disease Inflammation/Immunology Cancer
Pamidronate disodium (Standard) is the analytical standard of Pamidronate disodium.Pamidronate disodium (Standard), the second-generation nitrogen-containing bisphosphonate, is an inhibitor of bone loss. Pamidronate disodium (Standard) significantly inhibits subchondral bone loss in early osteoarthritis by upregulating the expression of OPG in cartilage and subchondral bone, and inhibiting the expression of RANKL and MMP-9 in both tissues, as well as TLR-4 in cartilage, thereby alleviating cartilage degeneration. Additionally, Pamidronate disodium (Standard) can inhibit the signaling of Wnt and β-catenin, and is applicable for research on osteoporosis and osteosarcoma .

HY-17372S

Rofecoxib-d5	Isotope-Labeled Compounds COX	Inflammation/Immunology Cancer
Rofecoxib-d₅ is the deuterium labeled Rofecoxib. Rofecoxib is a potent, specific and orally active COX-2 inhibitor, with IC50s of 26 and 18 nM for human COX-2 in human osteosarcoma cells and Chinese hamster ovary cells, with a 1000-fold selectivity for COX-2 over human COX-1 (IC50 > 50 μM in U937 cells and > 15 μM in Chinese hamster ovary cells)[1][2].

HY-N7135

Tropolone	Tyrosinase Fungal	Metabolic Disease Inflammation/Immunology Cancer
Tropolone is a seven-membered non-benzenoid aromatic compound, which is the precursor of many Azulene derivatives. Tropolone is a potent mushroom tyrosinase inhibitor with an IC₅₀ value of 0.4 μM. Its inhibitory effect can be achieved by dialysis or excess CU ²⁺ Reversa. Tropolone exhibits broad anti-viral and anti-fungal activity and is synergistic upon co-treatment with nucleos(t)ide analog drugs. Tropolone is a promising candidate for research in osteosarcoma .

HY-17372R

Rofecoxib (Standard)	COX	Inflammation/Immunology Cancer
Rofecoxib (Standard) is the analytical standard of Rofecoxib. This product is intended for research and analytical applications. Rofecoxib is a potent, specific and orally active COX-2 inhibitor, with IC₅₀s of 26 and 18 nM for human COX-2 in human osteosarcoma cells and Chinese hamster ovary cells, with a 1000-fold selectivity for COX-2 over human COX-1 (IC₅₀ > 50 μM in U937 cells and > 15 μM in Chinese hamster ovary cells).

HY-13777C

Zoledronate disodium CGP 42446 disodium; CGP42446A disodium; ZOL 446 disodium	Apoptosis	Cancer
Zoledronate (CGP 42446) disodium is a potent bisphosphonate that effectively inhibits osteoclastogenesis, reducing bone turnover and stabilizing the bone matrix. Zoledronate disodium has demonstrated notable effectiveness in managing Paget's disease of bone by suppressing metabolic activity and alleviating bone pain. Zoledronate disodium is being investigated in the ongoing ZiPP trial for its potential to prevent disease progression in patients with Paget's disease. Zoledronate disodium also exhibits diverse anti-tumor effects in osteosarcoma, further highlighting its multifunctional therapeutic applications.

HY-N3387

Licoricidin	Apoptosis NF-κB Akt MMP	Inflammation/Immunology Cancer
Licoricidin (LCD) is isolated from Glycyrrhiza uralensis Fisch, possesses anti-cancer activities. Licoricidin (LCD) inhibit SW480 cells (IC₅₀=7.2 μM) by inducing cycle arrest, apoptosis and autophagy, and is a potential chemopreventive or chemotherapeutic agent against colorectal cancer . Licoricidin (LCD) inhibits Lung Metastasis by inhibition of tumor angiogenesis and lymphangiogenesis as well as changes in the local microenvironment of tumor tissues the anticarcinogenic effect . Licoricidin enhanced gemcitabine-induced cytotoxicity in Osteosarcoma (OS) cells by inactivation of the Akt and NF-κB pathways in vitro and in vivo . Licoricidin blocks UVA-induced photoaging via ROS scavenging, limits the activity of MMP-1, it can be considered as an active ingredient in new topically applied anti-ageing formulations .

Cat. No.	Product Name	Target	Research Area

HY-P3730

Cdk2/Cyclin Inhibitory Peptide I	CDK	Cancer
Cdk2/Cyclin Inhibitory Peptide I (Tat-LFG), a CDK2 inhibitor, kills U2OS osteosarcoma cells in a dose-dependent manner .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0153

Naringin Maximum Cited Publications 13 Publications Verification Naringoside	Structural Classification Citrus × aurantium Linnaeus Flavonoids Classification of Application Fields Leguminosae Flavonones Rutaceae Plants Endogenous metabolite Glycyrrhiza uralensis Fisch. Disease Research Fields Cancer	Cytochrome P450 Autophagy Mitophagy Endogenous Metabolite
Naringin is a major flavanone glycoside obtained from tomatoes, grapefruits, and many other citrus fruits. Naringin exhibits biological properties such as antioxidant, anti-inflammatory, and antiapoptotic activities. Naringin also inhibits proliferation and invasion and induces apoptosis in human osteosarcoma cells by inhibiting zinc finger E-box binding homeobox 1 (Zeb1) .

HY-N2112

Glaucocalyxin A 2 Publications Verification	Structural Classification Classification of Application Fields Terpenoids Labiatae Source classification Diterpenoids Plants Glycyrrhiza lepidota Pursh Disease Research Fields Cancer	PI3K Akt Apoptosis
Glaucocalyxin A, an ent-kauranoid diterpene from Rabdosia japonica var., induces apoptosis in osteosarcoma by inhibiting nuclear translocation of Five-zinc finger Glis 1 (GLI1) via regulating PI3K/Akt signaling pathway. Glaucocalyxin A has antitumor effect .

HY-N7135

Tropolone	Olax imbricata Structural Classification Classification of Application Fields Ketones, Aldehydes, Acids Olacaceae Source classification Other Diseases Plants Disease Research Fields	Tyrosinase Fungal
Tropolone is a seven-membered non-benzenoid aromatic compound, which is the precursor of many Azulene derivatives. Tropolone is a potent mushroom tyrosinase inhibitor with an IC₅₀ value of 0.4 μM. Its inhibitory effect can be achieved by dialysis or excess CU ²⁺ Reversa. Tropolone exhibits broad anti-viral and anti-fungal activity and is synergistic upon co-treatment with nucleos(t)ide analog drugs. Tropolone is a promising candidate for research in osteosarcoma .

HY-N3387

Licoricidin	Structural Classification Natural Products Classification of Application Fields Leguminosae Source classification Phenols Polyphenols Plants Glycyrrhiza uralensis Fisch. Inflammation/Immunology Disease Research Fields	Apoptosis NF-κB Akt MMP
Licoricidin (LCD) is isolated from Glycyrrhiza uralensis Fisch, possesses anti-cancer activities. Licoricidin (LCD) inhibit SW480 cells (IC₅₀=7.2 μM) by inducing cycle arrest, apoptosis and autophagy, and is a potential chemopreventive or chemotherapeutic agent against colorectal cancer . Licoricidin (LCD) inhibits Lung Metastasis by inhibition of tumor angiogenesis and lymphangiogenesis as well as changes in the local microenvironment of tumor tissues the anticarcinogenic effect . Licoricidin enhanced gemcitabine-induced cytotoxicity in Osteosarcoma (OS) cells by inactivation of the Akt and NF-κB pathways in vitro and in vivo . Licoricidin blocks UVA-induced photoaging via ROS scavenging, limits the activity of MMP-1, it can be considered as an active ingredient in new topically applied anti-ageing formulations .

HY-N7385

Nudol	Orchidaceae Source classification Phenols Polyphenols Plants Epigeneium rotundatum (Lindl.) Summerh.	MMP Apoptosis
Nudol is a phenanthrene compound that has anti-cancer activity. Nudol inhibits cell proliferation, induces cell apoptosis. Nudol inhibits MMP-2M and MMP-9 activity (K_i: 988.9 nM, 1.76 μM, respectively). Nudol can be used in the research of cancers, such as osteosarcoma .

HY-N6611

Chimaphilin	Quinones Structural Classification Passifloraceae Source classification Passiflora incarnata L. Plants Naphthalene Quinones	IGF-1R
Chimaphilin is an IGF-1R inhibitor (IC₅₀: 0.086 μM). Chimaphilin has antifungal, antioxidant and anticancer activities. Chimaphilin inhibits the growth of both drug-sensitive and drug-resistant osteosarcoma cell lines. Chimaphilin can induce cancer cell apoptosis. Chimaphilin is a main component of pyrola .

HY-N0153R

Naringin (Standard) Naringoside (Standard)	Structural Classification Citrus × aurantium Linnaeus Classification of Application Fields Source classification Rutaceae Plants Endogenous metabolite Flavonoids Leguminosae Flavonones Glycyrrhiza uralensis Fisch. Disease Research Fields Cancer	Endogenous Metabolite Cytochrome P450 Mitophagy Autophagy
Naringin is a major flavanone glycoside obtained from tomatoes, grapefruits, and many other citrus fruits. Naringin exhibits biological properties such as antioxidant, anti-inflammatory, and antiapoptotic activities. Naringin also inhibits proliferation and invasion and induces apoptosis in human osteosarcoma cells by inhibiting zinc finger E-box binding homeobox 1 (Zeb1) .

Cat. No.	Product Name	Chemical Structure

HY-17372S

Rofecoxib-d5
Rofecoxib-d₅ is the deuterium labeled Rofecoxib. Rofecoxib is a potent, specific and orally active COX-2 inhibitor, with IC50s of 26 and 18 nM for human COX-2 in human osteosarcoma cells and Chinese hamster ovary cells, with a 1000-fold selectivity for COX-2 over human COX-1 (IC50 > 50 μM in U937 cells and > 15 μM in Chinese hamster ovary cells)[1][2].

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Osteosarcoma Inhibitor

Inhibitors & Agonists

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