tumor suppressor genes

By Targets:	Akt (2) Antibiotic (2) Apoptosis (4) Bcl-2 Family (1) Cannabinoid Receptor (1) Caspase (3) COX (5) DNA Methyltransferase (14) EGFR (1) Endogenous Metabolite (6) ERK (1) FXR (1) HDAC (1) HIF/HIF Prolyl-Hydroxylase (1) Histone Demethylase (6) Histone Methyltransferase (1) Isotope-Labeled Compounds (5) Liposome (1) MDM-2/p53 (2) Mitochondrial Metabolism (1) mRNA (1) mTOR (1) NO Synthase (5) p38 MAPK (1) Parasite (2) PDK-1 (1) PGE synthase (5) PI3K (1) Potassium Channel (4) PTEN (2) Reactive Oxygen Species (ROS) (5) Reference Standards (4) VEGFR (1)
By Research Areas:	Cancer (29) Cardiovascular Disease (8) Infection (2) Inflammation/Immunology (4) Metabolic Disease (1) Neurological Disease (7)
Oligonucleotides:	Cationic Lipids (1) mRNA (1)

Targets Recommended: Large Tumor Suppressor (LATS) TNF Receptor HRASLS BRK STING VISTA

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B0660

Eicosapentaenoic Acid 25+ Cited Publications EPA; Timnodonic acid	Endogenous Metabolite Histone Demethylase	Neurological Disease Cancer
Eicosapentaenoic Acid (EPA) is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic Acid can promote relaxation of vascular smooth muscle cells and vasodilation .

HY-13642

RG108 10+ Cited Publications N-Phthalyl-L-tryptophan	DNA Methyltransferase	Inflammation/Immunology Cancer
RG108 (N-Phthalyl-L-tryptophan) is a non-nucleoside DNA methyltransferases (DNMTs) inhibitor (IC₅₀=115 nM) that blocks the DNMTs active site. RG108 (N-Phthalyl-L-tryptophan) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences .

HY-B0464

Hydralazine hydrochloride 3 Publications Verification	PGE synthase NO Synthase Reactive Oxygen Species (ROS) DNA Methyltransferase COX	Cardiovascular Disease Inflammation/Immunology Cancer
Hydralazine hydrochloride is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine hydrochloride reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine hydrochloride inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGE_E2; meanwhile, Hydralazine hydrochloride scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine hydrochloride alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine hydrochloride directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine hydrochloride has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain .

HY-103397

Nanaomycin A 4 Publications Verification	Antibiotic DNA Methyltransferase Parasite	Infection Cancer
Nanaomycin A is the first selective DNMT3B inhibitor with an IC₅₀ of 500 nM. Nanaomycin A, a quinone antibiotics, reactivates silenced tumor suppressor genes in human cancer cells . Nanaomycin A inhibits in vitro growth of the human malaria parasite Plasmodium falciparum with an IC₈₀ value of 33.1 nM .

HY-A0084A

Procainamide 5+ Cited Publications Procaine amide; SP 100	DNA Methyltransferase Potassium Channel	Cardiovascular Disease Cancer
Procainamide (Procaine amide) is a specific and potent inhibitor of DNA methyltransferase 1 (DNMT1), which reactivates the expression of tumor suppressor factors by demethylating tumor suppressor genes. Procainamide induces vacuolization in various cell types and reduces cell proliferation and migration. Procainamide relaxes airway smooth muscle by activating potassium channels. Procainamide can be used in cancer and arrhythmia research .

HY-A0084

Procainamide hydrochloride 5+ Cited Publications Procaine amide hydrochloride; SP 100 hydrochloride	DNA Methyltransferase Potassium Channel	Cancer
Procainamide hydrochloride (Procaine amide hydrochloride) is a specific and potent inhibitor of DNA methyltransferase 1 (DNMT1), which reactivates the expression of tumor suppressor factors by demethylating tumor suppressor genes. Procainamide hydrochloride induces vacuolization in various cell types and reduces cell proliferation and migration. Procainamide hydrochloride relaxes airway smooth muscle by activating potassium channels. Procainamide hydrochloride can be used in cancer and arrhythmia research .

HY-B0464A

Hydralazine 3 Publications Verification	DNA Methyltransferase Reactive Oxygen Species (ROS) COX NO Synthase PGE synthase	Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
Hydralazine is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGE_E2; meanwhile, Hydralazine scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain .

HY-150229

306-N16B	Liposome	Cancer
306-N16B is a selective lung-targeted lipid nanoparticle that reversibly targets lung endothelial cells and specific immune cells through selective adsorption of a protein corona mediated by differences in tail structure (such as fibrinogen β/γ chain). 306-N16B binds to specific plasma proteins in the blood to form a protein corona, which guides the particles to be enriched in the lungs, releases mRNA and promotes target cell gene expression, exerts efficient lung cell transfection activity, and can precisely regulate gene delivery of different cell types in the lungs (such as endothelial cells and macrophages). 306-N16B can be used in gene therapy technologies for hereditary lung diseases including pulmonary lymphangioleiomyomatosis (LAM), restoring tumor suppressor function by delivering Tsc2 mRNA, and can also be used for lung-specific mRNA vaccines and gene editing therapies .

HY-101508

GNA002	Histone Methyltransferase	Cancer
GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC₅₀ of 1.1 μM. GNA002 can specifically and covalently bind to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination. GNA002 efficiently reduces EZH2-mediated H3K27 trimethylation, reactivates polycomb repressor complex 2 (PRC2)-silenced tumor suppressor genes .

HY-B0660R

Eicosapentaenoic Acid (Standard) EPA (Standard); Timnodonic acid (Standard)	Reference Standards Endogenous Metabolite Histone Demethylase	Neurological Disease Cancer
Eicosapentaenoic Acid (Standard) is the analytical standard of Eicosapentaenoic Acid. This product is intended for research and analytical applications. Eicosapentaenoic Acid (EPA) is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic Acid can promote relaxation of vascular smooth muscle cells and vasodilation .

HY-106263B

Tyroserleutide hydrochloride	PTEN PDK-1 MDM-2/p53 Apoptosis Akt	Cancer
Tyroserleutide hydrochloride is a tripeptide isolated from the degradation products of porcine spleen with antitumor activity. Tyroserleutide hydrochloride can upregulate the expression of the tumor suppressor gene PTEN and inhibit the activity of AKT and PDK1. Tyroserleutide hydrochloride inhibits tumor cell proliferation and MDM2 phosphorylation by inhibiting the PI3K/AKT pathway, and also upregulates P21, P27, P53, and induces mitochondrial damage and cell apoptosis .

HY-B0464S1

Hydralazine-d5 hydrochloride	Isotope-Labeled Compounds PGE synthase NO Synthase Reactive Oxygen Species (ROS) DNA Methyltransferase COX	Cancer
Hydralazine-d₅ (hydrochloride) is deuterium-labeled Hydralazine (hydrochloride) (HY-B0464). Hydralazine hydrochloride is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine hydrochloride reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine hydrochloride inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGE_E2; meanwhile, Hydralazine hydrochloride scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine hydrochloride alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine hydrochloride directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine hydrochloride has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain .

HY-W011269

Eicosapentaenoic Acid sodium 25+ Cited Publications EPA sodium; Timnodonic acid sodium	Endogenous Metabolite Histone Demethylase	Cardiovascular Disease Metabolic Disease Cancer
Eicosapentaenoic Acid (EPA)sodium is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid sodium exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid sodium activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic Acid sodium can promote relaxation of vascular smooth muscle cells and vasodilation .

HY-13906

Largazole (+)-Largazole	HDAC	Neurological Disease Cancer
Largazole ((+)-Largazole) is a potent, selective, orally active and brain-penetrant class I HDAC inhibitor found in marine cyanobacteria. Largazole shows an IC₅₀ of 0.07 nM for HDAC2. Largazole releases its active form Largazole thiol (HY-170890) after hydrolysis. Largazole has a strong inhibitory effect on SF-268, SF-295 and SH-SY5Y cells, with IC₅₀ values of 62, 68 and 102 nM respectively Largazole can upregulate the tumor suppressor gene Pax6 to inhibit the proliferation, invasion and colony formation of glioblastoma cells. Largazole can significantly upregulated brain-derived neurotrophic factor BDNF, neuronal transcription factor Pax6, and μ-opioid receptor gene Oprm1. Largazole exerts antitumor and neuroprotective effects. Largazole can be used for researches of Glioblastoma and Alzheimer’s disease .

HY-B0464S

Hydralazine-d4 hydrochloride	Isotope-Labeled Compounds PGE synthase NO Synthase Reactive Oxygen Species (ROS) DNA Methyltransferase COX	Cardiovascular Disease
Hydralazine-d4 hydrochloride is the deuterium labeled Hydralazine hydrochloride. Hydralazine hydrochloride is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine hydrochloride reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine hydrochloride inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGE_E2; meanwhile, Hydralazine hydrochloride scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine hydrochloride alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine hydrochloride directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine hydrochloride has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain .

HY-103397R

Nanaomycin A (Standard)	Antibiotic Reference Standards DNA Methyltransferase Parasite	Infection Cancer
Nanaomycin A (Standard) is the analytical standard of Nanaomycin A. This product is intended for research and analytical applications. Nanaomycin A is the first selective DNMT3B inhibitor with an IC50 of 500 nM. Nanaomycin A, a quinone antibiotics, reactivates silenced tumor suppressor genes in human cancer cells[1]. Nanaomycin A inhibits in vitro growth of the human malaria parasite Plasmodium falciparum with an IC80 value of 33.1 nM[2].

HY-149412

MHJ-627	ERK	Cancer
MHJ-627 is a potent ERK5 (MAPK7) inhibitor (IC₅₀: 0.91 μM). MHJ-627 promotes the mRNA expression of tumor suppressors and anti-metastatic genes, and promotes cancer cell death .

HY-100443

PX20606 PX-102	FXR	Cancer
PX20606 is an orally active agonist for farnesoid X receptor (FXR), with EC₅₀ 220 nM (mFXR) and 50 nM (hFXR), measured by Gal4-FXR assay. PX20606 induces the expression of tumor suppressor gene NDRG2, inhibits the tumor growth and metastasis in mouse HCC model. PX20606 exhibits hepatoprotective efficacy .

HY-B0660S1

Eicosapentaenoic acid 1,2,3,4,5-13C5 EPA 1,2,3,4,5-13C, FA 20:5-¹³C₅	Isotope-Labeled Compounds Endogenous Metabolite Histone Demethylase	Neurological Disease Cancer
Eicosapentaenoic acid 1,2,3,4,5- ¹³C₅ (EPA 1,2,3,4,5- ¹³C, FA 20:5- ¹³C₅) is ¹³C labeled Eicosapentaenoic Acid. Eicosapentaenoic Acid (EPA) is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic Acid can promote relaxation of vascular smooth muscle cells and vasodilation .

HY-A0084AR

Procainamide (Standard) Procaine amide (Standard); SP 100 (Standard)	Reference Standards DNA Methyltransferase Potassium Channel	Cardiovascular Disease Cancer
Procainamide (Standard) is the analytical standard of Procainamide. This product is intended for research and analytical applications. Procainamide (Procaine amide) is a specific and potent inhibitor of DNA methyltransferase 1 (DNMT1), which reactivates the expression of tumor suppressor factors by demethylating tumor suppressor genes. Procainamide induces vacuolization in various cell types and reduces cell proliferation and migration. Procainamide relaxes airway smooth muscle by activating potassium channels. Procainamide can be used in cancer and arrhythmia research .

HY-174511

Human TP53 mRNA	mRNA	Cancer
Human TP53 mRNA encodes the human tumor protein p53 (TP53) protein, a tumor suppressor protein containing transcriptional activation, DNA binding, and oligomerization domains. TP53 responds to diverse cellular stresses to regulate expression of target genes, thereby inducing cell cycle arrest, apoptosis, senescence, DNA repair, or changes in metabolism.

HY-159938

p38α inhibitor 6	p38 MAPK Apoptosis Bcl-2 Family MDM-2/p53 Caspase	Cancer
p38α inhibitor 6 (compound 19) is a p38α inhibitor with the IC₅₀ of 0.68 μM. p38α inhibitor 6 induces cell apoptosis and arrests cell cycle at G0 and G2/M phase. p38α inhibitor 6 decreases the TNF-α concentration as well as increased the expression of tumor suppressor gene p53, Bax/BCL-2 ratio and caspase 3/7 .

HY-168338

CB2 receptor agonist 8	Cannabinoid Receptor Caspase	Cancer
CB2 receptor agonist 8 (Compound 17) is an agonist for cannabinoid receptor 2 (CB2 receptor). CB2 receptor agonist 8 exhibits cytotoxicity in cells U87, RPMI 8226, HL-60, and L929 with IC₅₀s of 91.03, 16.29, 23.51 and 564.6 μM, respectively. CB2 receptor agonist 8 activates caspase 3/7, increases the expressions of pro-apoptotic genes BAX, BAD, BIM and tumor suppressor genes p53, and induces apoptosis in U87. CB2 receptor agonist 8 inhibits the migration of U87 .

HY-B0660A

Eicosapentaenoic acid metformin EPA metformin; Timnodonic acid metformin	Endogenous Metabolite Histone Demethylase	Neurological Disease Cancer
Eicosapentaenoic Acid (EPA) metformin is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic acid metformin exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). EEicosapentaenoic acid metformin activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic acid metformin can promote relaxation of vascular smooth muscle cells and vasodilation .

HY-B0464R

Hydralazine hydrochloride (Standard)	Reference Standards PGE synthase NO Synthase Reactive Oxygen Species (ROS) DNA Methyltransferase COX	Cardiovascular Disease Inflammation/Immunology Cancer
Hydralazine (hydrochloride) (Standard) is the analytical standard of Hydralazine (hydrochloride). This product is intended for research and analytical applications. Hydralazine hydrochloride is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine hydrochloride reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine hydrochloride inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGE_E2; meanwhile, Hydralazine hydrochloride scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine hydrochloride alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine hydrochloride directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine hydrochloride has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain .

HY-A0084AS

Procainamide-d4 Procaine amide-d₄; SP 100-d₄	Isotope-Labeled Compounds Potassium Channel DNA Methyltransferase	Cardiovascular Disease Cancer
Procainamide-d₄ (Procaine amide-d₄) is the deuterium labeled Procainamide (HY-A0084A). Procainamide (Procaine amide) is a specific and potent inhibitor of DNA methyltransferase 1 (DNMT1), which reactivates the expression of tumor suppressor factors by demethylating tumor suppressor genes. Procainamide induces vacuolization in various cell types and reduces cell proliferation and migration. Procainamide relaxes airway smooth muscle by activating potassium channels. Procainamide can be used in cancer and arrhythmia research .

HY-181097

EGFR-IN-192	Apoptosis EGFR VEGFR mTOR HIF/HIF Prolyl-Hydroxylase PI3K Akt PTEN	Cancer
EGFR-IN-192 is an anticancer agent. EGFR-IN-192 inhibits EGFR (IC₅₀: 0.12 μM), downregulates the HIF-VEGF and PI3K/AKT/mTOR pathways, upregulates the tumor suppressor gene PTEN, and induces cell cycle arrest and apoptosis in tumor cells. EGFR-IN-192 exhibits antitumor activity and can be used in tumor research .

HY-182009

DNMT-IN-6	DNA Methyltransferase Apoptosis Caspase Mitochondrial Metabolism	Cancer
DNMT-IN-6 is a DNA methyltransferase inhibitor with activity against DNMT1, DNMT3A, and DNMT3B. DNMT-IN-6 drives demethylation, and restores TMS1 tumor suppressor gene expression. DNMT-IN-6 induces apoptosis, causes G2/M phase arrest, disrupts mitochondrial integrity, and activates the intrinsic caspase cascade (3/7/9). DNMT-IN-6 inhibits tumor growth, and improves survival in xenograft models. DNMT-IN-6 can be used for the research of cancer, such as diffuse large B-cell lymphoma .

HY-13642G

RG108	DNA Methyltransferase	Cancer
RG108 (GMP) is RG108 (HY-13642) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. RG108 (N-Phthalyl-L-tryptophan) is a non-nucleoside DNA methyltransferases (DNMTs) inhibitor (IC₅₀=115 nM) that blocks the DNMTs active site. RG108 (N-Phthalyl-L-tryptophan) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences .

HY-B0660S2

Eicosapentaenoic acid-d10 EPA-d₁₀; Timnodonic acid-d₁₀	Isotope-Labeled Compounds Endogenous Metabolite Histone Demethylase	Neurological Disease Cancer
Eicosapentaenoic acid-d₁₀ (EPA-d₁₀) is the deuterium labeled Eicosapentaenoic acid (HY-B0660). Eicosapentaenoic Acid (EPA) is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic Acid can promote relaxation of vascular smooth muscle cells and vasodilation .

Cat. No.	Product Name

HY-L083

Anti-Cancer Metabolism Compound Library	3,552 compounds
Mutations in oncogenes and tumor suppressor genes can modify multiple signaling pathways and in turn cell metabolism, which facilitates tumorigenesis. The paramount hallmark of tumor metabolism is “aerobic glycolysis” or the Warburg effect, coined by Otto Warburg in 1926, in which cancer cells produce most of energy from glycolysis pathway regardless of whether in aerobic or anaerobic condition. Usually, cancer cells are highly glycolytic (glucose addiction) and take up more glucose than do normal cells from outside. The increased uptake of glucose is facilitated by the overexpression of several isoforms of membrane glucose transporters (GLUTs). Likewise, the metabolic pathways of glutamine, amino acid and fat metabolism are also altered. Recent trends in anti-cancer drug discovery suggests that targeting the altered metabolic pathways of cancer cells result in energy crisis inside the cancer cells and can selectively inhibit cancer cell proliferation by delaying or suppressing tumor growth. MCE provides a unique collection of 3,552 compounds which cover various tumor metabolism-related signaling pathways. These compounds can be used for anti-cancer metabolism targets identification, validation as well anti-cancer drug discovery.

Anti-Cancer Metabolism Compound Library

3,552 compounds

Mutations in oncogenes and tumor suppressor genes can modify multiple signaling pathways and in turn cell metabolism, which facilitates tumorigenesis. The paramount hallmark of tumor metabolism is “aerobic glycolysis” or the Warburg effect, coined by Otto Warburg in 1926, in which cancer cells produce most of energy from glycolysis pathway regardless of whether in aerobic or anaerobic condition. Usually, cancer cells are highly glycolytic (glucose addiction) and take up more glucose than do normal cells from outside. The increased uptake of glucose is facilitated by the overexpression of several isoforms of membrane glucose transporters (GLUTs). Likewise, the metabolic pathways of glutamine, amino acid and fat metabolism are also altered. Recent trends in anti-cancer drug discovery suggests that targeting the altered metabolic pathways of cancer cells result in energy crisis inside the cancer cells and can selectively inhibit cancer cell proliferation by delaying or suppressing tumor growth.

MCE provides a unique collection of 3,552 compounds which cover various tumor metabolism-related signaling pathways. These compounds can be used for anti-cancer metabolism targets identification, validation as well anti-cancer drug discovery.

HY-L015

PI3K/Akt/mTOR Compound Library	1,049 compounds
The PI3K/Akt/mTOR pathway controls many cellular processes that are important for the formation and progression of cancer, including apoptosis, transcription, translation, metabolism, angiogenesis, and cell cycle progression. Every major node of this signaling network is activated in a wide range of human tumors. Mechanisms for the pathway activation include activation of receptor tyrosine kinases (RTKs) upstream of PI3K, mutation or amplification of PIK3CA encoding p110α catalytic subunit of PI3K, mutation or loss of PTEN tumor suppressor gene, and mutation or amplification of Akt1. Once the pathway is activated, signaling through Akt can stimulate a series of substrates including mTOR which is involved in protein synthesis. Thus, inhibition of this pathway is an attractive concept for cancer prevention and/or therapy. Currently some mTOR inhibitors are approved for several indications, and there are several novel PI3K/Akt/mTOR inhibitors in clinical trials. MCE owns a unique collection of 1,049 compounds that can be used for PI3K/Akt/mTOR pathway research. PI3K/Akt/mTOR Compound Library also acts as a useful tool for anti-cancer drug discovery.

PI3K/Akt/mTOR Compound Library

1,049 compounds

The PI3K/Akt/mTOR pathway controls many cellular processes that are important for the formation and progression of cancer, including apoptosis, transcription, translation, metabolism, angiogenesis, and cell cycle progression. Every major node of this signaling network is activated in a wide range of human tumors. Mechanisms for the pathway activation include activation of receptor tyrosine kinases (RTKs) upstream of PI3K, mutation or amplification of PIK3CA encoding p110α catalytic subunit of PI3K, mutation or loss of PTEN tumor suppressor gene, and mutation or amplification of Akt1. Once the pathway is activated, signaling through Akt can stimulate a series of substrates including mTOR which is involved in protein synthesis. Thus, inhibition of this pathway is an attractive concept for cancer prevention and/or therapy. Currently some mTOR inhibitors are approved for several indications, and there are several novel PI3K/Akt/mTOR inhibitors in clinical trials.

MCE owns a unique collection of 1,049 compounds that can be used for PI3K/Akt/mTOR pathway research. PI3K/Akt/mTOR Compound Library also acts as a useful tool for anti-cancer drug discovery.

HY-L101

Anti-Liver Cancer Compound Library	2,838 compounds
Liver cancer is one of the leading malignancies which occupies the second position in cancer deaths worldwide, becoming serious threat to human health. Hepatocellular carcinoma (HCC), also known as hepatoma is the most common type accounting for approximately 90% of all liver cancers. Current evidence indicates that during hepatocarcinogenesis, two main pathogenic mechanisms prevail: (1) cirrhosis associated with hepatic regeneration after tissue damage caused by hepatitis infection, toxins or metabolic influences, and (2) mutations occurring in single or multiple oncogenes or tumor suppressor genes. Both mechanisms have been linked with alterations in several important cellular signaling pathways. These include the RAF/MEK/ERK pathway, PI3K/AKT/mTOR pathway, WNT/b-catenin pathway, insulin-like growth factor pathway, c-MET/HGFR pathway , etc. MCE offers a unique collection of 2,838 compounds with identified and potential anti-liver cancer activity. MCE anti-liver cancer compound library is a useful tool for anti-liver cancer drugs screening and other related research.

Anti-Liver Cancer Compound Library

2,838 compounds

Liver cancer is one of the leading malignancies which occupies the second position in cancer deaths worldwide, becoming serious threat to human health. Hepatocellular carcinoma (HCC), also known as hepatoma is the most common type accounting for approximately 90% of all liver cancers.

Current evidence indicates that during hepatocarcinogenesis, two main pathogenic mechanisms prevail: (1) cirrhosis associated with hepatic regeneration after tissue damage caused by hepatitis infection, toxins or metabolic influences, and (2) mutations occurring in single or multiple oncogenes or tumor suppressor genes. Both mechanisms have been linked with alterations in several important cellular signaling pathways. These include the RAF/MEK/ERK pathway, PI3K/AKT/mTOR pathway, WNT/b-catenin pathway, insulin-like growth factor pathway, c-MET/HGFR pathway , etc.

MCE offers a unique collection of 2,838 compounds with identified and potential anti-liver cancer activity. MCE anti-liver cancer compound library is a useful tool for anti-liver cancer drugs screening and other related research.

HY-L045

Oxygen Sensing Compound Library	4,029 compounds
Oxygen homeostasis regulation is the most fundamental cellular process for adjusting physiological oxygen variations, and its irregularity leads to various human diseases, including cancer. Hypoxia is closely associated with cancer development, and hypoxia/oxygen-sensing signaling plays critical roles in the modulation of cancer progression. Hypoxia-inducible factor 1 (HIF-1) is a transcription factor that functions as a master regulator of oxygen homeostasis. A variety of HF-1 target genes have been identified thus far which encode proteins that play key roles in critical developmental and physiological processes including angiogenesis/vascular remodeling, erythropoiesis, glucose transport, glycolysis, iron transport, and cell proliferation/survival. HIF-1 is a heterodimeric transcription factor consisting of a constitutively expressed β-subunit and an oxygen-regulated α-subunit. The unique feature of HIF-1 is the regulation of HIF-1α expression and activity based upon the cellular O₂ concentration. Under normoxic conditions, hydroxylation of HIF-1α on these different proline residues is essential for HIF proteolytic degradation by promoting interaction with the von Hippel-Lindau tumor-suppressor protein (pVHL) through hydrogen bonding to the hydroxyproline-binding pocket in the pVHL β-domain. As oxygen levels decrease, hydroxylation of HIF decreases; HIF-1α then no longer binds pVHL, and becomes stabilized, allowing more of the protein to translocate to the cell’s nucleus, where it acts as a transcription factor, upregulating (often within minutes) the production of proteins that stimulate blood perfusion in tissues and thus tissue oxygenation. MCE offers a unique collection of 4,029 oxygen sensing related compounds targeting HIF/HIF Prolyl-Hydroxylase, MAPK/ERK, PI3K/AKT signaling pathways, etc. MCE Oxygen Sensing Compound Library is a useful tool to study hypoxia, oxidative stress and discover new anti-cancer drugs.

Oxygen Sensing Compound Library

4,029 compounds

Oxygen homeostasis regulation is the most fundamental cellular process for adjusting physiological oxygen variations, and its irregularity leads to various human diseases, including cancer. Hypoxia is closely associated with cancer development, and hypoxia/oxygen-sensing signaling plays critical roles in the modulation of cancer progression.

Hypoxia-inducible factor 1 (HIF-1) is a transcription factor that functions as a master regulator of oxygen homeostasis. A variety of HF-1 target genes have been identified thus far which encode proteins that play key roles in critical developmental and physiological processes including angiogenesis/vascular remodeling, erythropoiesis, glucose transport, glycolysis, iron transport, and cell proliferation/survival.

HIF-1 is a heterodimeric transcription factor consisting of a constitutively expressed β-subunit and an oxygen-regulated α-subunit. The unique feature of HIF-1 is the regulation of HIF-1α expression and activity based upon the cellular O₂ concentration. Under normoxic conditions, hydroxylation of HIF-1α on these different proline residues is essential for HIF proteolytic degradation by promoting interaction with the von Hippel-Lindau tumor-suppressor protein (pVHL) through hydrogen bonding to the hydroxyproline-binding pocket in the pVHL β-domain. As oxygen levels decrease, hydroxylation of HIF decreases; HIF-1α then no longer binds pVHL, and becomes stabilized, allowing more of the protein to translocate to the cell’s nucleus, where it acts as a transcription factor, upregulating (often within minutes) the production of proteins that stimulate blood perfusion in tissues and thus tissue oxygenation.

MCE offers a unique collection of 4,029 oxygen sensing related compounds targeting HIF/HIF Prolyl-Hydroxylase, MAPK/ERK, PI3K/AKT signaling pathways, etc. MCE Oxygen Sensing Compound Library is a useful tool to study hypoxia, oxidative stress and discover new anti-cancer drugs.

Cat. No.	Product Name	Type

HY-13642G

RG108	Fluorescent Dyes
RG108 (GMP) is RG108 (HY-13642) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. RG108 (N-Phthalyl-L-tryptophan) is a non-nucleoside DNA methyltransferases (DNMTs) inhibitor (IC₅₀=115 nM) that blocks the DNMTs active site. RG108 (N-Phthalyl-L-tryptophan) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences .

RG108

Fluorescent Dyes

RG108 (GMP) is RG108 (HY-13642) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. RG108 (N-Phthalyl-L-tryptophan) is a non-nucleoside DNA methyltransferases (DNMTs) inhibitor (IC₅₀=115 nM) that blocks the DNMTs active site. RG108 (N-Phthalyl-L-tryptophan) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences .

Cat. No.	Product Name	Type

HY-150229

306-N16B	Biochemical Assay Reagents
306-N16B is a selective lung-targeted lipid nanoparticle that reversibly targets lung endothelial cells and specific immune cells through selective adsorption of a protein corona mediated by differences in tail structure (such as fibrinogen β/γ chain). 306-N16B binds to specific plasma proteins in the blood to form a protein corona, which guides the particles to be enriched in the lungs, releases mRNA and promotes target cell gene expression, exerts efficient lung cell transfection activity, and can precisely regulate gene delivery of different cell types in the lungs (such as endothelial cells and macrophages). 306-N16B can be used in gene therapy technologies for hereditary lung diseases including pulmonary lymphangioleiomyomatosis (LAM), restoring tumor suppressor function by delivering Tsc2 mRNA, and can also be used for lung-specific mRNA vaccines and gene editing therapies .

306-N16B

Biochemical Assay Reagents

306-N16B is a selective lung-targeted lipid nanoparticle that reversibly targets lung endothelial cells and specific immune cells through selective adsorption of a protein corona mediated by differences in tail structure (such as fibrinogen β/γ chain). 306-N16B binds to specific plasma proteins in the blood to form a protein corona, which guides the particles to be enriched in the lungs, releases mRNA and promotes target cell gene expression, exerts efficient lung cell transfection activity, and can precisely regulate gene delivery of different cell types in the lungs (such as endothelial cells and macrophages). 306-N16B can be used in gene therapy technologies for hereditary lung diseases including pulmonary lymphangioleiomyomatosis (LAM), restoring tumor suppressor function by delivering Tsc2 mRNA, and can also be used for lung-specific mRNA vaccines and gene editing therapies .

HY-13642G

RG108	Biochemical Assay Reagents
RG108 (GMP) is RG108 (HY-13642) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. RG108 (N-Phthalyl-L-tryptophan) is a non-nucleoside DNA methyltransferases (DNMTs) inhibitor (IC₅₀=115 nM) that blocks the DNMTs active site. RG108 (N-Phthalyl-L-tryptophan) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences .

RG108

Biochemical Assay Reagents

RG108 (GMP) is RG108 (HY-13642) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. RG108 (N-Phthalyl-L-tryptophan) is a non-nucleoside DNA methyltransferases (DNMTs) inhibitor (IC₅₀=115 nM) that blocks the DNMTs active site. RG108 (N-Phthalyl-L-tryptophan) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences .

Cat. No.	Product Name	Target	Research Area

HY-106263B

Tyroserleutide hydrochloride	PTEN PDK-1 MDM-2/p53 Apoptosis Akt	Cancer
Tyroserleutide hydrochloride is a tripeptide isolated from the degradation products of porcine spleen with antitumor activity. Tyroserleutide hydrochloride can upregulate the expression of the tumor suppressor gene PTEN and inhibit the activity of AKT and PDK1. Tyroserleutide hydrochloride inhibits tumor cell proliferation and MDM2 phosphorylation by inhibiting the PI3K/AKT pathway, and also upregulates P21, P27, P53, and induces mitochondrial damage and cell apoptosis .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-B0660

Eicosapentaenoic Acid 25+ Cited Publications EPA; Timnodonic acid	Human Gut Microbiota Metabolites Microorganisms Neurological Disease Classification of Application Fields Ketones, Aldehydes, Acids Endogenous metabolite Disease Research Fields Source Classification Cancer	Endogenous Metabolite Histone Demethylase
Eicosapentaenoic Acid (EPA) is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic Acid can promote relaxation of vascular smooth muscle cells and vasodilation .

HY-B0660R

Eicosapentaenoic Acid (Standard) EPA (Standard); Timnodonic acid (Standard)	Structural Classification Human Gut Microbiota Metabolites Microorganisms Ketones, Aldehydes, Acids Endogenous metabolite Source Classification	Reference Standards Endogenous Metabolite Histone Demethylase
Eicosapentaenoic Acid (Standard) is the analytical standard of Eicosapentaenoic Acid. This product is intended for research and analytical applications. Eicosapentaenoic Acid (EPA) is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic Acid can promote relaxation of vascular smooth muscle cells and vasodilation .

HY-W011269

Eicosapentaenoic Acid sodium 25+ Cited Publications EPA sodium; Timnodonic acid sodium	Cardiovascular Disease Classification of Application Fields Ketones, Aldehydes, Acids Endogenous metabolite Disease Research Fields Source Classification	Endogenous Metabolite Histone Demethylase
Eicosapentaenoic Acid (EPA)sodium is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid sodium exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid sodium activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic Acid sodium can promote relaxation of vascular smooth muscle cells and vasodilation .

HY-13906

Largazole (+)-Largazole	Structural Classification Natural Products Microorganisms Source Classification	HDAC
Largazole ((+)-Largazole) is a potent, selective, orally active and brain-penetrant class I HDAC inhibitor found in marine cyanobacteria. Largazole shows an IC₅₀ of 0.07 nM for HDAC2. Largazole releases its active form Largazole thiol (HY-170890) after hydrolysis. Largazole has a strong inhibitory effect on SF-268, SF-295 and SH-SY5Y cells, with IC₅₀ values of 62, 68 and 102 nM respectively Largazole can upregulate the tumor suppressor gene Pax6 to inhibit the proliferation, invasion and colony formation of glioblastoma cells. Largazole can significantly upregulated brain-derived neurotrophic factor BDNF, neuronal transcription factor Pax6, and μ-opioid receptor gene Oprm1. Largazole exerts antitumor and neuroprotective effects. Largazole can be used for researches of Glioblastoma and Alzheimer’s disease .

Cat. No.	Product Name	Chemical Structure

HY-B0464S1

Hydralazine-d5 hydrochloride

Hydralazine-d₅ (hydrochloride) is deuterium-labeled Hydralazine (hydrochloride) (HY-B0464). Hydralazine hydrochloride is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine hydrochloride reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine hydrochloride inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGE_E2; meanwhile, Hydralazine hydrochloride scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine hydrochloride alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine hydrochloride directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine hydrochloride has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain .

HY-B0464S

Hydralazine-d4 hydrochloride

Hydralazine-d4 hydrochloride is the deuterium labeled Hydralazine hydrochloride. Hydralazine hydrochloride is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine hydrochloride reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine hydrochloride inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGE_E2; meanwhile, Hydralazine hydrochloride scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine hydrochloride alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine hydrochloride directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine hydrochloride has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain .

HY-B0660S1

Eicosapentaenoic acid 1,2,3,4,5-13C5

Eicosapentaenoic acid 1,2,3,4,5- ¹³C₅ (EPA 1,2,3,4,5- ¹³C, FA 20:5- ¹³C₅) is ¹³C labeled Eicosapentaenoic Acid. Eicosapentaenoic Acid (EPA) is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic Acid can promote relaxation of vascular smooth muscle cells and vasodilation .

HY-A0084AS

Procainamide-d4

Procainamide-d₄ (Procaine amide-d₄) is the deuterium labeled Procainamide (HY-A0084A). Procainamide (Procaine amide) is a specific and potent inhibitor of DNA methyltransferase 1 (DNMT1), which reactivates the expression of tumor suppressor factors by demethylating tumor suppressor genes. Procainamide induces vacuolization in various cell types and reduces cell proliferation and migration. Procainamide relaxes airway smooth muscle by activating potassium channels. Procainamide can be used in cancer and arrhythmia research .

HY-B0660S2

Eicosapentaenoic acid-d10

Eicosapentaenoic acid-d₁₀ (EPA-d₁₀) is the deuterium labeled Eicosapentaenoic acid (HY-B0660). Eicosapentaenoic Acid (EPA) is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic Acid can promote relaxation of vascular smooth muscle cells and vasodilation .

Cat. No.	Product Name		Classification

HY-150229

306-N16B		Cationic Lipids
306-N16B is a selective lung-targeted lipid nanoparticle that reversibly targets lung endothelial cells and specific immune cells through selective adsorption of a protein corona mediated by differences in tail structure (such as fibrinogen β/γ chain). 306-N16B binds to specific plasma proteins in the blood to form a protein corona, which guides the particles to be enriched in the lungs, releases mRNA and promotes target cell gene expression, exerts efficient lung cell transfection activity, and can precisely regulate gene delivery of different cell types in the lungs (such as endothelial cells and macrophages). 306-N16B can be used in gene therapy technologies for hereditary lung diseases including pulmonary lymphangioleiomyomatosis (LAM), restoring tumor suppressor function by delivering Tsc2 mRNA, and can also be used for lung-specific mRNA vaccines and gene editing therapies .

HY-174511

Human TP53 mRNA		mRNA
Human TP53 mRNA encodes the human tumor protein p53 (TP53) protein, a tumor suppressor protein containing transcriptional activation, DNA binding, and oligomerization domains. TP53 responds to diverse cellular stresses to regulate expression of target genes, thereby inducing cell cycle arrest, apoptosis, senescence, DNA repair, or changes in metabolism.

Targets Recommended: Large Tumor Suppressor (LATS) TNF Receptor HRASLS BRK STING VISTA

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13642G

RG108	DNA Methyltransferase	Cancer
RG108 (GMP) is RG108 (HY-13642) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. RG108 (N-Phthalyl-L-tryptophan) is a non-nucleoside DNA methyltransferases (DNMTs) inhibitor (IC₅₀=115 nM) that blocks the DNMTs active site. RG108 (N-Phthalyl-L-tryptophan) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences .

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Remarks

Inhibitors & Agonists

Screening Libraries

Fluorescent Dyes

Biochemical Assay Reagents

Peptides

Natural
Products

Isotope-Labeled Compounds

Oligonucleotides

GMP Molecules

tumor suppressor genes

Inhibitors & Agonists

Screening Libraries

Fluorescent Dyes

Biochemical Assay Reagents

Peptides

NaturalProducts

Isotope-Labeled Compounds

Oligonucleotides

GMP Molecules

Natural
Products