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Cerlapirdine (SAM-531, PF-05212365) is a selective and potent full antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor. Cerlapirdine has the potential for researching the Alzheimer's disease .
SAMβA TFA is conjugated to the cell permeable peptide TAT47-57. SAMβA TFA, a rationally designed selective antagonist of Mfn1-βIIPKC association. SAMβA TFA is a selective inhibitor of mitofusin 1-βIIPKC association improves heart failure outcome in rats .
SAMβA is conjugated to the cell permeable peptide TAT47-57. SAMβA, a rationally designed selective antagonist of Mfn1-βIIPKC association. SAMβA is a selective inhibitor of mitofusin 1-βIIPKC association improves heart failure outcome in rats .
Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo .
Delphinidin-3-sambubioside (Dp3‐Sam) chloride is an anthocyanin that has orally active anti-inflammatory activity. Delphinidin-3-sambubioside chloride inhibits LPS-induced inflammatory factors release. Delphinidin-3-sambubioside chloride also alleviates hepatic lipid accumulation in HFD rats. Delphinidin-3-sambubioside chloride can be isolated from Hibiscus sabdariffa L. .
ML353 is a selective ligand of mGlu5 silent allosteric modulator (SAM) with an Ki value of 18.2 nM. ML353 improves the affinity of common allosteric sites, 20-fold higher than the previous mGlu5 SAM tool compound 5mpep. ML353 has potential applications in solving the intrinsic activity of SAM in vivo or as a agent blocker . ML353 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
II399 is a potent, selective NNMT bisubstrate inhibitor containing an unconventional SAM mimic, with a Ki of 5.9 nM. II399 exhibits an explicit pattern of competitive inhibition for NAM. II399 occupies both the substrate and cofactor binding pockets. II399 has the potential for the research of cancers, metabolic, cardiovascular, and neurodegenerative diseases .
Y-29794 oxalate is a selective, orally active and blood-brain barrier permeable non-peptide prolyl endopeptidase inhibitor. Y-29794 oxalate blocks the IRS1-AKT-mTORC1 pathway and inhibits tumor growth. Y-29794 oxalate is also effective in inhibiting the progression of Aβ-like deposition in the hippocampus of aging-accelerated mice (SAM) .
BMS-984923, a potent mGluR5 silent allosteric modulator (SAM), with exquisite binding affinity (Ki = 0.6 nM), exhibits good oral bioavailability and BBB penetration. BMS-984923 potently inhibits the PrPC-mGluR5 interaction and prevents pathological Aβo signaling without affecting physiological glutamate signaling .
KMI169 is a potent and selective bi-substrate inhibitor targeting the SAM and substrate binding pockets of KMT9. KMI169 can be used for the research of prostate cancer .
SARS-CoV-2-IN-60 (compound 5a) is an S-adenosylmethionine (SAM)-competitive and irreversible SARS-CoV-2 nsp16-nsp10 methyltransferase activity inhibitor with an IC50 of 9 μM and a Ki of 26 μM. SARS-CoV-2-IN-60 can specifically occupy a newly identified pocket adjacent to the SAM-binding site on nsp16. SARS-CoV-2-IN-60 has the potential for pan-coronavirus therapeutics .
AGI-41998 is a potent inhibitor of methionine adenosyltransferase 2A (MAT2A). AGI-41998 is a brain-penetrant compound. AGI-41998 has the potential for exploring the effects of SAM modulation in the central nervous system (CNS) and research of cancer disease .
AGI-43192 is a potent inhibitor of methionine adenosyltransferase 2A (MAT2A). AGI-43192 is a potent, but limited brain-penetrant compound. AGI-43192 has the potential for exploring the effects of SAM modulation in the central nervous system (CNS) and research of cancer disease .
PRMT5-IN-33 (compound A8) is a selective, SAM-competitve PRMT5 inhibitors with IC50 of 10.9 nM. PRMT5-IN-33 induces apoptosis and inhibits proliferation of cells Z-138 and MOLM-13. PRMT5-IN-33 exhibits an antitumor activity .
FIDAS-3 is a stilbene derivative and is a potent Wnt inhibitor with an IC50 of 4.9 μM for methionine S-adenosyltransferase 2A (MAT2A). FIDAS-3 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-3 has anticancer activities .
FIDAS-5 is a potent and orally active methionine S-adenosyltransferase 2A (MAT2A) inhibitor with an IC50 of 2.1 μM. FIDAS-5 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-5 has anticancer activities .
5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis . 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis .
TAT-SAMβA is the peptide consist of RNAENFDRF (SAMβA; HY-P3429) conjugated to the cell penetrating TAT protein-derived peptide TAT47–57. TAT-SAMβA is a selective antagonist of Mfn1-βIIPKC association. TAT-SAMβA protects mouse embryonic fibroblast cells (MEFs) against oxidative stress-induced cytotoxicity .
ICMT-IN-48 (compound 1) is an ICMT inhibitor that is competitive (Km=13 μM) for the prenylated methyl acceptor, the first substrate of ICMT. ICMT-IN-48 inhibits ICMT activity with IC50s affected by the concentration of the second substrate S-adenosylmethinine (SAM), and the IC50s are 3.5 μM (1×Km SAM) and 2.3 μM (10×Km SAM), respectively .
EZH2-IN-1 (compound 3) is a selective and SAM-competitive EZH2 and EZH1 inhibitor with an IC50s of 32 nM, 197 nM and 213 nM for EZH2wt, EZH2 Y641N mutant and EZH1, respectively. EZH2-IN-1 reduces bulk H3K27me3 and H3K27me2 levels. EZH2-IN-1 has the potential for diffuse large B cell lymphoma research .
YB-0158 (Wnt pathway inhibitor 2) is a reverse-turn peptidomimetic and a potent colorectal cancer stem cell (CSC) targeting agent. YB-0158 disrupts Sam68-Src interactions and induces apoptosis in CRC cells. Anti-cancer activities .
JQEZ5 is a potent and selective EZH2 lysine methyltransferase inhibitor. JQEZ5 SAM-competitively inhibits polycomb repressive complex 2 (PRC2) with an IC50 of 80 nM. JQEZ5 has anti-tumor effects .
NSC 288387 is a pan-flavivirus MTase inhibitor. NSC 288387 binds to the SAM-binding pocket. NSC 288387 inhibits ZIKV with an IC50 of 0.2 μM. NSC 288387 also inhibits viral replication in cell culture .
BRK inhibitor P21d hydrochloride is a potent breast tumor kinase (BRK/PTK6) inhibitor with an IC50 of 30 nM. BRK inhibitor P21d hydrochloride inhibits p-SAM68 with an IC50 of 52 nM. BRK inhibitor P21d hydrochloride can be used to evaluate the in vivo activity of BRK inhibitors in xenograft breast tumor models .
mRNA Cap 2'-O-methyltransferase uses S-adenosylmethionine (SAM) as a methyl donor to add a methyl group at the 2'-O position of the first nucleotide at the 5’ end of Cap-0 mRNA, resulting in Cap-1 structure. Cap-1 structure promotes translation efficiency, increasing subsequent protein expression .
5'-Methylthioadenosine- 13C6 is the 13C-labeled 5'-Methylthioadenosine. 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis[1]. 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis[2].
PRMT5-IN-19 (Compound 41) is an selective orally active non-nucleoside PRMT5 inhibitor with IC50 values of 23.9 nM (radioactive biochemical assay) and 47 nM (AlphaLISA assay). PRMT5-IN-19 can occupy the SAM-binding pocket in PRMT5 and block methyltransferase activity, which displays good selectivity over other PRMTs and PKMTs. PRMT5-IN-19 inhibits cell proliferation by inducing cell apoptosis, and can be used for cancer-related research .
5'-Methylthioadenosine-d3 is the deuterium labeled 5'-Methylthioadenosine[1]. 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis. 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis[2][3][4].
DS-437 is a dual PRMT5/7 inhibitor (IC50s of PRMT5/7=6 μM). DS-437 is selective for PRMT5 and PRMT7 over 29 other human protein-, DNA-, and RNA-methyltransferases. DS-437 is a S-adenosylmethionine (SAM)-competitive inhibitor of PRMT5. DS-437 also inhibits DNMT3A and DNMT3B, with IC50s of 52 and 62 μM, respectively. DS-437 inhibits the methylation of FOXP3 .
Antiproliferative agent-25 (Compound 3s4) is a selective PRMT5 inhibitor (IC50: 0.11 μM). Antiproliferative agent-25 up-regulates hnRNP E1 protein level. Antiproliferative agent-25 forms H-bond interactions with SAM and E444 residue of PRMT5. Antiproliferative agent-25 has antiproliferative effects against A549 cells by inducing apoptosis and inhibiting cell migration. Antiproliferative agent-25 has high clearances with T1/2 of only 21.8 and 4.7 min in human and rat liver microsomes .
mRNA Cap 2'-O-methyltransferase uses S-adenosylmethionine (SAM) as a methyl donor to add a methyl group at the 2'-O position of the first nucleotide at the 5’ end of Cap-0 mRNA, resulting in Cap-1 structure. Cap-1 structure promotes translation efficiency, increasing subsequent protein expression .
SAMβA TFA is conjugated to the cell permeable peptide TAT47-57. SAMβA TFA, a rationally designed selective antagonist of Mfn1-βIIPKC association. SAMβA TFA is a selective inhibitor of mitofusin 1-βIIPKC association improves heart failure outcome in rats .
SAMβA is conjugated to the cell permeable peptide TAT47-57. SAMβA, a rationally designed selective antagonist of Mfn1-βIIPKC association. SAMβA is a selective inhibitor of mitofusin 1-βIIPKC association improves heart failure outcome in rats .
TAT-SAMβA is the peptide consist of RNAENFDRF (SAMβA; HY-P3429) conjugated to the cell penetrating TAT protein-derived peptide TAT47–57. TAT-SAMβA is a selective antagonist of Mfn1-βIIPKC association. TAT-SAMβA protects mouse embryonic fibroblast cells (MEFs) against oxidative stress-induced cytotoxicity .
FAM-SAMS is a biological active peptide. (5-FAM labeled HY-P0136. This FAM labeled peptide (Abs/Em = 494/521 nm) can be used as a substrate for 5-AMP-activated protein kinase (AMPK) in in vitro kinase assays.)
MAIT-203, a cyclopentyalanin-derived peptidomimetic, potently inhibits the interaction of adenomatous polyposis coli (APC) and Asef (RhoGEF4), but not APC-Sam68 or APC-striatin interactions. MAIT-203 binds APC-ARM with a Ki of 0.015 μM and a Kd of 0.036 μM. MAIT-203 significantly represses the migration and invasion of colorectal cancer cells.
5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis . 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis .
Delphinidin-3-sambubioside (Dp3‐Sam) chloride is an anthocyanin that has orally active anti-inflammatory activity. Delphinidin-3-sambubioside chloride inhibits LPS-induced inflammatory factors release. Delphinidin-3-sambubioside chloride also alleviates hepatic lipid accumulation in HFD rats. Delphinidin-3-sambubioside chloride can be isolated from Hibiscus sabdariffa L. .
The FGFR-3 protein is a tyrosine protein kinase that serves as a cell surface receptor for fibroblast growth factors and controls cellular processes, including proliferation, differentiation, and apoptosis. It is essential for chondrocyte differentiation, proliferation, apoptosis and normal bone development functions. FGFR-3 Protein, Mouse (HEK293, His) is the recombinant mouse-derived FGFR-3 protein, expressed by HEK293 , with C-His labeled tag. The total length of FGFR-3 Protein, Mouse (HEK293, His) is 347 a.a., with molecular weight of 60-90 kDa.
The FGFR-3 protein is a tyrosine-protein kinase receptor for fibroblast growth factor that is critical for cellular processes, particularly in chondrocytes, osteoblasts, and inner ear development. Its effects span normal skeletal development and postnatal bone mineralization. FGFR-3 Protein, Human (P. pastoris, N-His) is the recombinant human-derived FGFR-3 protein, expressed by P. pastoris , with N-6*His labeled tag. The total length of FGFR-3 Protein, Human (P. pastoris, N-His) is 410 a.a., with molecular weight of 47.4 kDa.
FGFR-3 is a member of the fibroblast growth factor receptor family and is expressed in tissues such as cartilage, brain, intestine and kidney. FGFR-3 regulates chondrocyte differentiation and proliferation by activating the MAPK/STAT signaling pathway. FGFR-3 is a tumor marker. FGFR-3 Protein, Cynomolgus/Rhesus Macaque (HEK293, Fc) is the recombinant cynomolgus-derived FGFR-3 protein, expressed by HEK293 , with C-hFc labeled tag. The total length of FGFR-3 Protein, Cynomolgus/Rhesus Macaque (HEK293, Fc) is 375 a.a., with molecular weight of ~99.9 KDa.
The FGFR-3 protein is a tyrosine-protein kinase receptor for fibroblast growth factor that is critical for cellular processes, particularly in chondrocytes, osteoblasts, and inner ear development. Its effects span normal skeletal development and postnatal bone mineralization. FGFR-3 Protein, Human (HEK293, hFc) is the recombinant human-derived FGFR-3 protein, expressed by HEK293 , with C-hFc labeled tag. The total length of FGFR-3 Protein, Human (HEK293, hFc) is 353 a.a., with molecular weight of ~90 kDa.
The FGFR-3 protein is a tyrosine-protein kinase receptor for fibroblast growth factor that is critical for cellular processes, particularly in chondrocytes, osteoblasts, and inner ear development. Its effects span normal skeletal development and postnatal bone mineralization. FGFR-3 Protein, Human (His-B2M) is the recombinant human-derived FGFR-3 protein, expressed by E. coli , with N-6*His, N-B2M labeled tag. The total length of FGFR-3 Protein, Human (His-B2M) is 410 a.a., with molecular weight of ~59.4 kDa.
FGFR-1 alpha is a tyrosine-protein kinase receptor for fibroblast growth factor that is critical in embryonic development, cell proliferation, differentiation, and migration. GnRH is essential for mesodermal patterning, axial organization, skeletogenesis, and nervous system development. FGFR-1 beta (IIIc) Protein, Human (Biotinylated, HEK293, His-Avi) is the recombinant human-derived FGFR-1 beta, expressed by HEK293 , with C-Avi, C-His labeled tag. The total length of FGFR-1 beta (IIIc) Protein, Human (Biotinylated, HEK293, His-Avi) is 198 a.a., with molecular weight of 45-55 kDa.
FGFR-2 beta is a tyrosine protein kinase that serves as a cell surface receptor for fibroblast growth factor and is critical for cell regulation, proliferation, differentiation, migration, and apoptosis. It plays important roles in embryonic development, trophoblast function, limb buds, lungs, osteogenesis, and skin development. FGFR-2 beta (IIIb) Protein, Cynomolgus (HEK293, His) is the recombinant cynomolgus-derived FGFR-2 beta, expressed by HEK293 , with C-His labeled tag. The total length of FGFR-2 beta (IIIb) Protein, Cynomolgus (HEK293, His) is 215 a.a., with molecular weight of 50-68 kDa.
FGFR-2 beta is a tyrosine protein kinase that serves as a cell surface receptor for fibroblast growth factor and is critical for cell regulation, proliferation, differentiation, migration, and apoptosis. It plays important roles in embryonic development, trophoblast function, limb buds, lungs, osteogenesis, and skin development. FGFR-2 beta (IIIb) Protein, Mouse (HEK293, His) is the recombinant mouse-derived FGFR-2 beta, expressed by HEK293 , with C-His labeled tag. The total length of FGFR-2 beta (IIIb) Protein, Mouse (HEK293, His) is 225 a.a., with molecular weight of 50-70 kDa.
The FGFR-2 α IIIc protein is a tyrosine protein kinase receptor for fibroblast growth factor and is critical for embryonic development, regulating proliferation, differentiation, and apoptosis. Its importance is evident in embryonic patterning, trophoblast function, limb bud development, lung morphogenesis, osteogenesis, and skin development. FGFR-2 beta IIIb Protein, Human (HEK293, Avi) is the recombinant human-derived FGFR-2 beta IIIb protein, expressed by HEK293 , with C-Avi labeled tag. The total length of FGFR-2 beta IIIb Protein, Human (HEK293, Avi) is 126 a.a., with molecular weight of 35-50 kDa.
The FGFR-2 α IIIc protein is a tyrosine protein kinase receptor for fibroblast growth factor and is critical for embryonic development, regulating proliferation, differentiation, and apoptosis. Its importance is evident in embryonic patterning, trophoblast function, limb bud development, lung morphogenesis, osteogenesis, and skin development. FGFR-2 beta IIIb Protein, Human (Biotinylated, HEK293, His-Avi) is the recombinant human-derived FGFR-2 beta IIIb protein, expressed by HEK293 , with C-Avi, C-His labeled tag. The total length of FGFR-2 beta IIIb Protein, Human (Biotinylated, HEK293, His-Avi) is 227 a.a., with molecular weight of 48-60 kDa.
The FGFR-2 α IIIc protein is a tyrosine protein kinase receptor for fibroblast growth factor and is critical for embryonic development, regulating proliferation, differentiation, and apoptosis. Its importance is evident in embryonic patterning, trophoblast function, limb bud development, lung morphogenesis, osteogenesis, and skin development. FGFR-2 beta IIIc Protein, Human (Biotinylated, HEK293, His-Avi) is the recombinant human-derived FGFR-2 beta IIIc protein, expressed by HEK293 , with C-Avi, C-His labeled tag. The total length of FGFR-2 beta IIIc Protein, Human (Biotinylated, HEK293, His-Avi) is 226 a.a., with molecular weight of 48-60 kDa.
The FGFR-2 α IIIc protein is a tyrosine protein kinase receptor for fibroblast growth factor and is critical for embryonic development, regulating proliferation, differentiation, and apoptosis. Its importance is evident in embryonic patterning, trophoblast function, limb bud development, lung morphogenesis, osteogenesis, and skin development. FGFR-2 alpha IIIb Protein, Human (Biotinylated, HEK293, His-Avi) is the recombinant human-derived FGFR-2 alpha IIIb protein, expressed by HEK293 , with C-Avi, C-His labeled tag. The total length of FGFR-2 alpha IIIb Protein, Human (Biotinylated, HEK293, His-Avi) is 357 a.a., with molecular weight of 70-110 kDa.
The FGFR-2 α IIIc protein is a tyrosine protein kinase receptor for fibroblast growth factor and is critical for embryonic development, regulating proliferation, differentiation, and apoptosis. Its importance is evident in embryonic patterning, trophoblast function, limb bud development, lung morphogenesis, osteogenesis, and skin development. FGFR-2 alpha IIIc Protein, Human (Biotinylated, HEK293, His-Avi) is the recombinant human-derived FGFR-2 alpha IIIc protein, expressed by HEK293 , with C-His, C-Avi labeled tag. The total length of FGFR-2 alpha IIIc Protein, Human (Biotinylated, HEK293, His-Avi) is 356 a.a., with molecular weight of 70-80 kDa.
5'-Methylthioadenosine- 13C6 is the 13C-labeled 5'-Methylthioadenosine. 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis[1]. 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis[2].
5'-Methylthioadenosine-d3 is the deuterium labeled 5'-Methylthioadenosine[1]. 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis. 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis[2][3][4].
