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DS-437 - 98%, high purity , CAS No.1674364-87-4

    Grade & Purity:
  • ≥98%
In stock
Item Number
D646188
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D646188-5mg
5mg
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$67.90
D646188-10mg
10mg
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$109.90
D646188-25mg
25mg
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$234.90
D646188-50mg
50mg
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$376.90
D646188-100mg
100mg
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$586.90

Basic Description

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
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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

Taxonomic Classification

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

Associated Targets(Human)

DNMT3A Tclin DNA (cytosine-5)-methyltransferase 3A (310 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MDA-MB-231 (73002 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRMT1 Tchem Protein-arginine N-methyltransferase 1 (867 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRMT3 Tchem Protein arginine N-methyltransferase 3 (219 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
DNMT3B Tchem DNA (cytosine-5)-methyltransferase 3B (150 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRMT6 Tchem Protein arginine N-methyltransferase 6 (321 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRMT5 Tchem Protein arginine N-methyltransferase 5 (1273 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRMT8 Tchem Protein arginine N-methyltransferase 8 (122 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRMT5 Tchem PRMT5/MEP50 complex (963 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

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

Certificates(CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Chemical and Physical Properties

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

Solution Calculators

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