Product Catalog / Myostatin Inhibitors

ACE-031 (ACVR2B)

The TGFβ (transforming growth factor β) superfamily proteins are pleiotropic cytokines that regulate a diverse range of cellular processes, including proliferation, differentiation, migration, adhesion and death. The TGFβ superfamily elicits 4 signaling pathways: TGFβ, Bone Morphogenic Protein (BMP), Activin, and Nodal. Each pathway signals through a heteromeric receptor complex composed of at least two type-I and two type-II transmembrane receptors containing cytoplasmic serine/threonine kinase domains. These receptors are distinguished by the presence of a glycine/serine-rich juxta-membrane domain found only in the type I receptors. Either type receptor may initially bind ligand, followed by the recruitment of an alternate-type receptor counterpart to form a signal-activating complex. ACVR2B (Activin receptor type-2B), also known as ACTR-IIB, is a type-II receptors for Activin and Myostatin. Ligands such as Activin and Myostatin bind to ACVR2B, which then associates with a type I receptor to initiate signal transduction. Human, mouse and rat ACVRIIB share greater than 98% amino acid sequence homology. Recombinant soluble ACVRIIB bind Activin with high affinity, and are potent Activin antagonists. Myostatin, a negative regulator of skeletal muscle growth, binds to ACVR2B effectively, and to a lesser extent, to ACVR2A. Haplotype structure at the ACVR2B gene locus may contribute to interindividual variation in skeletal muscle mass and strength. A heterozygous mutation in ACVR2B is a cause of left-right axis malformation, visceral heterotaxy-4 (HTX4).

AA Sequence: SGRGEAETRECIYYNANWELERTNQSGLERCEGEQDKRLHCYASWRN SSGTIELVKKGCWLDDFNCYDRQECVATEENPQVYFCCCEGNFCNER FTHLPEAGGPEVTYEPPPTAPTSTGTHTCPPCPAPELLGGPSVFLFP PKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKP REEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISK AKGQPREPQVYTLPPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNG QPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEAL HNHYTQKSLSLSPGK
Molecular Formula: C10H17N3O6S
Molecular Weight: 38.9 kDa
PubChem SID: 160778379
Synonyms: ACVR2B; ACTRIIB; ActR-IIB; HTX4; activin A receptor type 2B

Follistatin-344

Follistatin is an autocrine, activin-binding protein that is ubiquitously expressed with highest expression levels being in the ovary and skin. Follistatin negatively regulates the signaling of transforming growth factor beta (TGF-β) family members, such as activin, bone morphogenetic proteins (BMPs), myostatin, growth differentiation factor 11 (GDF-11), and TGF-β1. Follistatin functions as an antagonist by binding TGF-β family members to block interaction with their signaling receptors. Recombinant human Follistatin cDNA encodes a 344 amino acid protein with a 29 amino acid signal sequence, an N­terminal atypical TGF binding domain, three Follistatin domains that contain EGF­like and kazal­like motifs, and a highly acidic C­terminal tail.

AA Sequence: MGNCWLRQAK NGRCQVLYKT ELSKEECCST GRLSTSWTEE DVNDNTLFKW MIFNGGAPNC IPCKETCENV DCGPGKKCRMNKKNKPRCVC APDCSNITWK GPVCGLDGKT YRNECALLKA RCKEQPELEV QYQGRCKKTC RDVFCPGSST CVVDQTNNAY CVTCNRICPEPASSEQYLCG NDGVTYSSAC HLRKATCLLG RSIGLAYEGK CIKAKSCEDI QCTGGKKCLW DFKVGRGRCS LCDELCPDSK SDEPVCASDNATYASECAMK EAACSSGVLL EVKHSGSCN
Molecular Formula: C121H199N40O40
Molecular Weight: 2868.2 g/mol
PubChem SID: 160728500
Synonyms: FST; FS; Activin-Binding Protein; Follistatin

YK11

YK-11 is a synthetic, steroidal selective androgen receptor modulator (SARM). It is a gene-selective partial agonist of the androgen receptor (AR) and does not induce the physical interaction between the NTD/AF1 and LBD/AF2 (known as the N/C interaction), which is required for full transactivation of the AR. The drug has anabolic activity in vitro in C2C12 myoblasts and shows greater potency than dihydrotestosterone (DHT) in this regard.

IUPAC Name: methyl (2E)-2-[(8R,9S,10R,13S,14S,17S)-2'-methoxy-2',13-dimethyl-3-oxospiro[1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthrene-17,5'-1,3-dioxolane]-4'-ylidene]acetate
Molecular Formula: C25H34O6
Molecular Weight: 430.541 g/mol
PubChem SID: 313371232
Synonyms: (17alpha,20E)-17,20-((1-Methoxyethylidene)bis(oxy))-3-oxo-19-norpregna-4,20-diene-21-carboxylic acid methyl ester; 19-Norpregna-4,20-diene-21-carboxylic acid, 17,20-((1-methoxyethylidene)bis(oxy))-3-oxo-, methyl ester, (17alpha,20E)-; Z9748J6B0R

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