RG108 - ≥98%, high purity , CAS No.48208-26-0

  • ≥98%
Item Number
R126814
Grouped product items
SKUSizeAvailabilityPrice Qty
R126814-10mg
10mg
In stock
$77.90
R126814-50mg
50mg
In stock
$260.90
R126814-250mg
250mg
In stock
$1,174.90
R126814-1g
1g
In stock
$4,228.90

Novel, non-nucleoside DNA methyltransferase inhibitor (DNMT)

Basic Description

SynonymsHY-13642 | N-Phthalyl-L-tryptophan | AC-32704 | CHEBI:95041 | NCGC00097992-01 | P2023 | (S)-2-(1,3-dioxoisoindolin-2-yl)-3-(1H-indol-3-yl)propanoic acid | DTXSID801017660 | s2821 | RG108 | RG-108 | SCHEMBL164192 | EN300-7363574 | NSC-401077 | (2S)-2-(1,3-
Specifications & Purity≥98%
Biochemical and Physiological MechanismsRG108 is a non-nucleoside DNA methyltransferase (Dnmt) inhibitor that blocks the enzyme active site. RG108 inhibits DNA methylation in human cancer cell lines without detectable toxicity in vitro. The compound demethylates and reactivates epigenetically s
Storage TempProtected from light,Store at -20°C,Argon charged
Shipped InIce chest + Ice pads
NoteWherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Refer to SDS for further information. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

RG108 is an inhibitor of DNA methyltransferase with IC50 of 115 nM, does not cause trapping of covalent enzymes.
A Dnmt inhibitor that silences tumor suppressor genes.

Associated Targets(Human)

DNMT3B Tchem DNA (cytosine-5)-methyltransferase 3B (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
DNMT1 Tclin DNA (cytosine-5)-methyltransferase 1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
DNMT1 Tclin DNA (cytosine-5)-methyltransferase 1 (978 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
DNMT3A Tclin DNA (cytosine-5)-methyltransferase 3A (310 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2D6 Tclin Cytochrome P450 2D6 (33882 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP1A2 Tchem Cytochrome P450 1A2 (26471 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2C9 Tchem Cytochrome P450 2C9 (32119 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2C19 Tchem Cytochrome P450 2C19 (29246 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
DU-145 (51482 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HCT-8 (3484 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MCF7 (126967 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SF-295 (48000 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MDA-MB-435 (38290 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
DNMT3B Tchem DNA (cytosine-5)-methyltransferase 3B (150 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
DNMT3A Tclin DNMT3A2/3L complex (48 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAP2K3 Tchem MAP2K3/Myc proto-oncogene protein (25 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Mus musculus (284745 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Splenocyte (1641 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
sssIM CpG DNA methylase (38 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SARS-CoV-2 (38078 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Names and Identifiers

IUPAC Name (2S)-2-(1,3-dioxoisoindol-2-yl)-3-(1H-indol-3-yl)propanoic acid
INCHI InChI=1S/C19H14N2O4/c22-17-13-6-1-2-7-14(13)18(23)21(17)16(19(24)25)9-11-10-20-15-8-4-3-5-12(11)15/h1-8,10,16,20H,9H2,(H,24,25)/t16-/m0/s1
InChi Key HPTXLHAHLXOAKV-INIZCTEOSA-N
Canonical SMILES C1=CC=C2C(=C1)C(=O)N(C2=O)C(CC3=CNC4=CC=CC=C43)C(=O)O
Isomeric SMILES C1=CC=C2C(=C1)C(=O)N(C2=O)[C@@H](CC3=CNC4=CC=CC=C43)C(=O)O
WGK Germany 3
PubChem CID 702558
Molecular Weight 334.33
Reaxy-Rn 4552782

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

Find and download the COA for your product by matching the lot number on the packaging.

12 results found

Lot NumberCertificate TypeDateItem
H2222097Certificate of AnalysisJun 20, 2024 R126814
H2222100Certificate of AnalysisJun 20, 2024 R126814
G2312550Certificate of AnalysisJun 16, 2023 R126814
G2312554Certificate of AnalysisJun 16, 2023 R126814
G2312556Certificate of AnalysisJun 16, 2023 R126814
G2312621Certificate of AnalysisJun 16, 2023 R126814
G2312627Certificate of AnalysisJun 16, 2023 R126814
G2312639Certificate of AnalysisJun 16, 2023 R126814
G2312640Certificate of AnalysisJun 16, 2023 R126814
G2312682Certificate of AnalysisJun 16, 2023 R126814
F1503110Certificate of AnalysisJan 25, 2023 R126814
H2222105Certificate of AnalysisJun 20, 2022 R126814

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Chemical and Physical Properties

SolubilitySoluble in DMSO (100 mM), water (<1 mg/ml at 25 °C), ethanol (67 mg/ml at 25 °C), and DMF (~30 mg/ml).
Sensitivityheat sensitive;light sensitive
Specific Rotation[α]-271° (C=1,EtOH)
Melt Point(°C)181 °C

Safety and Hazards(GHS)

WGK Germany 3
Reaxy-Rn 4552782

Related Documents

References

1. Liu K et al..  (2020)  DNA Methylation May be Involved in the Analgesic Effect of Hyperbaric Oxygen via Regulating FUNDC1..  Pain Res Manag,  2020  (1528362).  [PMID:32148597]
2. Bialesova L et al..  (2017)  Epigenetic Regulation of PLIN 1 in Obese Women and its Relation to Lipolysis..  Sci Rep,  (10152).  [PMID:28860604]
3. Saunders J et al..  (2018)  Negative Evidence for a Functional Role of Neuronal DNMT3a in Persistent Pain..  Front Mol Neurosci,  11  (332).  [PMID:30258352]
4. Zanconato F et al..  (2018)  Transcriptional addiction in cancer cells is mediated by YAP/TAZ through BRD4..  Nat Med,  24  (10): (1599-1610).  [PMID:30224758]

Solution Calculators