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| SKU | Size | Availability |
Price | Qty |
|---|---|---|---|---|
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D646188-5mg
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5mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
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$67.90
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D646188-10mg
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10mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
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$109.90
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D646188-25mg
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25mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
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$234.90
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D646188-50mg
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50mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
|
$376.90
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D646188-100mg
|
100mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
|
$586.90
|
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| Specifications & Purity | ≥98% |
|---|---|
| Biochemical and Physiological Mechanisms | DS-437 is a dual PRMT5/7 inhibitor ( IC 50 s 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 inhi |
| Storage Temp | Store at -20°C |
| Shipped In |
Ice chest + Ice pads This product requires cold chain shipping. Ground and other economy services are not available. |
| Product Description |
DS-437 is a dual PRMT5/7 inhibitor ( IC 50 s 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 IC 50 s of 52 and 62 μM, respectively. DS-437 inhibits the methylation of FOXP3 In Vitro DS-437 was able to inhibit methylation of an H4[1–24] peptide by the PRMT5–MEP50 complex under balanced conditions (cofactor and substrate concentrations set at their respective?Km?values) in a dose-dependent manner with an IC 50 ?of 5.9 ± 1.4 μM. ?\nDS-437 increased total CD8 + ?and CD8 + PD-1 + T cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo DS-437 (10 mg/kg; i.p.; 5 times a week) has some beneficial effects on inhibiting tumor growth. The combination of DS-437 and the anti-p185 erbB2/neu ?antibody 4D5 had even more dramatic effects . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Six to Ten weeks old female Balb/c mice (bearing CT26Her2 tumor cells) Dosage: 10 mg/kg Administration: i.p.; 5 times a week Result: Had some beneficial effects on inhibiting tumor growth. Form:Solid IC50& Target:PRMT5 PRMT7 |
Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Nucleosides, nucleotides, and analogues |
| Class | 5'-deoxyribonucleosides |
| Subclass | 5'-deoxy-5'-thionucleosides |
| Intermediate Tree Nodes | Not available |
| Direct Parent | 5'-deoxy-5'-thionucleosides |
| Alternative Parents | Glycosylamines 6-aminopurines Pentoses Aminopyrimidines and derivatives N-substituted imidazoles Imidolactams Tetrahydrofurans Heteroaromatic compounds Ureas 1,2-diols Secondary alcohols Sulfenyl compounds Oxacyclic compounds Azacyclic compounds Dialkylthioethers Carbonyl compounds Primary amines Organopnictogen compounds Organic oxides Hydrocarbon derivatives |
| Molecular Framework | Aromatic heteropolycyclic compounds |
| Substituents | 5'-deoxy-5'-thionucleoside - Glycosyl compound - N-glycosyl compound - 6-aminopurine - Pentose monosaccharide - Imidazopyrimidine - Purine - Aminopyrimidine - Monosaccharide - N-substituted imidazole - Pyrimidine - Imidolactam - Tetrahydrofuran - Heteroaromatic compound - Azole - Imidazole - Urea - Secondary alcohol - Carbonic acid derivative - 1,2-diol - Sulfenyl compound - Thioether - Azacycle - Oxacycle - Organoheterocyclic compound - Dialkylthioether - Alcohol - Organic nitrogen compound - Hydrocarbon derivative - Organonitrogen compound - Organic oxide - Organopnictogen compound - Carbonyl group - Organooxygen compound - Organic oxygen compound - Organosulfur compound - Amine - Primary amine - Aromatic heteropolycyclic compound |
| Description | This compound belongs to the class of organic compounds known as 5'-deoxy-5'-thionucleosides. These are 5'-deoxyribonucleosides in which the ribose is thio-substituted at the 5'position by a S-alkyl group. |
| External Descriptors | Not available |
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| IUPAC Name | 1-[2-[[(2S,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]ethyl]-3-ethylurea |
|---|---|
| INCHI | InChI=1S/C15H23N7O4S/c1-2-17-15(25)18-3-4-27-5-8-10(23)11(24)14(26-8)22-7-21-9-12(16)19-6-20-13(9)22/h6-8,10-11,14,23-24H,2-5H2,1H3,(H2,16,19,20)(H2,17,18,25)/t8-,10-,11-,14-/m1/s1 |
| InChIKey | CACMCLIHCDTJHL-IDTAVKCVSA-N |
| Smiles | CCNC(=O)NCCSCC1C(C(C(O1)N2C=NC3=C(N=CN=C32)N)O)O |
| Isomeric SMILES | CCNC(=O)NCCSC[C@@H]1[C@H]([C@H]([C@@H](O1)N2C=NC3=C(N=CN=C32)N)O)O |
| PubChem CID | 122178085 |
| Molecular Weight | 397.45 |
| Solubility | DMSO : 125 mg/mL (314.50 mM; Need ultrasonic) |
|---|---|
| Molecular Weight | 397.500 g/mol |
| XLogP3 | -0.800 |
| Hydrogen Bond Donor Count | 5 |
| Hydrogen Bond Acceptor Count | 9 |
| Rotatable Bond Count | 7 |
| Exact Mass | 397.153 Da |
| Monoisotopic Mass | 397.153 Da |
| Topological Polar Surface Area | 186.000 Ų |
| Heavy Atom Count | 27 |
| Formal Charge | 0 |
| Complexity | 505.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 4 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 0 |
| Covalently-Bonded Unit Count | 1 |