UNC1999 - ≥98%, high purity , CAS No.1431612-23-5, Inhibitor of enhancer of zeste 2 polycomb repressive complex 2 subunit

Item Number
U125711
Grouped product items
SKUSizeAvailabilityPrice Qty
U125711-5mg
5mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$88.90
U125711-25mg
25mg
In stock
$400.90
U125711-100mg
100mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$835.90

Potent, selective cell-permeable EZH2 methyltransferase inhibitor

Basic Description

SynonymsMFCD26960958 | HMS3653O13 | SCHEMBL16767552 | CS-1658 | Q27089090 | UNC1999 | UNC-1999 | 1431612-23-5 | YSZC348 | DTXSID001099939 | N-[(6-methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-1-propan-2-yl-6-[6-(4-propan-2-ylpiperazin-1-yl)pyridin-3-yl]indazole-4
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsUNC1999 was the first orally bioavailable EZH2 inhibitor that has high in vitro potency for wild-type and mutant EZH2 as well as EZH1, UNC1999 was highly selective for EZH2 and EZH1 over a broad range of epigenetic and non-epigenetic targets, competitive
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of enhancer of zeste 2 polycomb repressive complex 2 subunit
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. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

UNC1999 is a potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM in cell-free assays, respectively, showing >1000-fold selectivity over a broad range of epigenetic and non-epigenetic targets.

Associated Targets(Human)

EZH1 Tchem Histone-lysine N-methyltransferase EZH1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
EZH2 Tclin Histone-lysine N-methyltransferase EZH2 (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name N-[(6-methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-1-propan-2-yl-6-[6-(4-propan-2-ylpiperazin-1-yl)pyridin-3-yl]indazole-4-carboxamide
INCHI InChI=1S/C33H43N7O2/c1-7-8-24-15-23(6)37-33(42)28(24)19-35-32(41)27-16-26(17-30-29(27)20-36-40(30)22(4)5)25-9-10-31(34-18-25)39-13-11-38(12-14-39)21(2)3/h9-10,15-18,20-22H,7-8,11-14,19H2,1-6H3,(H,35,41)(H,37,42)
InChi Key DPJNKUOXBZSZAI-UHFFFAOYSA-N
Canonical SMILES CCCC1=C(C(=O)NC(=C1)C)CNC(=O)C2=C3C=NN(C3=CC(=C2)C4=CN=C(C=C4)N5CCN(CC5)C(C)C)C(C)C
Isomeric SMILES CCCC1=C(C(=O)NC(=C1)C)CNC(=O)C2=C3C=NN(C3=CC(=C2)C4=CN=C(C=C4)N5CCN(CC5)C(C)C)C(C)C
WGK Germany 3
PubChem CID 72551585
Molecular Weight 569.74

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.

2 results found

Lot NumberCertificate TypeDateItem
H1618058Certificate of AnalysisFeb 26, 2024 U125711
L2014248Certificate of AnalysisOct 14, 2022 U125711

Chemical and Physical Properties

SolubilityDMSO

Safety and Hazards(GHS)

Pictogram(s) GHS07
Signal Warning
Hazard Statements

H302:Harmful if swallowed

Precautionary Statements

P501:Dispose of contents/container to ...

P264:Wash hands [and …] thoroughly after handling.

P270:Do not eat, drink or smoke when using this product.

P330:Rinse mouth.

P301+P317:IF SWALLOWED: Get medical help.

WGK Germany 3

Related Documents

References

1. Konze KD, Ma A, Li F, Barsyte-Lovejoy D, Parton T, Macnevin CJ, Liu F, Gao C, Huang XP, Kuznetsova E et al..  (2013)  An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1..  ACS Chem Biol,  (6): (1324-34).  [PMID:23614352]
2. Marsolier J et al..  (2022)  H3K27me3 conditions chemotolerance in triple-negative breast cancer..  Nat Genet,  54  (4): (459-468).  [PMID:35410383]
3. Zijlmans DW et al..  (2022)  Integrated multi-omics reveal polycomb repressive complex 2 restricts human trophoblast induction..  Nat Cell Biol,  24  (6): (858-871).  [PMID:35697783]

Solution Calculators