UNC1999

Alias: UNC1999; UNC 1999; UNC-1999;
Cat No.:V0385 Purity: ≥98%
UNC1999 (UNC-1999) is an orally bioavailable, cell-permeable, selective, SAM-competitive and dual inhibitor of EZH2/EZH1 (Enhancer of zeste homolog) with antineoplastic activity.
UNC1999 Chemical Structure CAS No.: 1431612-23-5
Product category: Histone Methyltransferase
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
250mg
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

UNC1999 (UNC-1999) is an orally bioavailable, cell-permeable, selective, SAM-competitive and dual inhibitor of EZH2/EZH1 (Enhancer of zeste homolog) with antineoplastic activity. It inhibits EZH2/EZH1 with IC50s of 2 nM and 45 nM in cell-free assays, respectively, and shows >1000-fold selectivity for EZH2/EZH1 over a variety of epigenetic and non-epigenetic targets.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
UNC1999 is a novel oral bioavailable inhibitor that exhibits strong in vitro potency against both wild-type and mutant EZH2. Additionally, it exhibits great potency against EZH1, a closely related H3K27 methyltransferase that shares 96% sequence identity with EZH2 in their respective catalytic domains. Over a wide spectrum of epigenetic and non-epigenetic targets, UNC1999 exhibits great selectivity for EZH2 and EZH1. It competes with the cofactor SAM but does not bind with peptide substrates. For sigma1, sigma2, histamine H3, and NET, the Ki values of UNC1999 are 4,700 nM, 65 nM, 300 nM, and 1,500 nM, in that order. DB cells, a DLBCL cell line carrying the EZH2 Y641N mutation, are specifically eliminated by NC1999. UNC1999 inhibits DB cell growth in a concentration- and time-dependent manner (EC50=633±101 nM (n=3))[1].
ln Vivo
In male Swiss albino mice, a single intraperitoneal (IP) injection of UNC1999 at 15, 50, or 150 mg/kg produced a high Cmax (9,700-11,800 nM) and demonstrated dosage linearity. While the 15 mg/kg IP dose caused the plasma concentrations of UNC1999 to be above their cellular IC50 for about 12 hours, the 150 and 50 mg/kg IP doses caused the plasma concentrations of UNC1999 to be above their cellular IC50 for the full 24 hours. The oral bioavailability of UNC1999 was next investigated, and we are happy to report that in male Swiss albino mice, a single oral dosage of 50 mg/kg of UNC1999 produced a high Cmax (4,700 nM) and good exposure levels. After this single oral dose, UNC1999 plasma concentrations are sustained above its cellular IC50 for about 20 hours. It is noteworthy that the test animals exhibit good tolerance to all dosages, including the 150 mg/kg IP dose, and no side effects are noted [1].
Animal Protocol
Dissolved in DMSO; ~150 mg/kg (i.p.), ~50 mg/kg (oral); i.p.injection or oral administration
Male Swiss albino mice
References
[1]. Konze KD, et al. An Orally Bioavailable Chemical Probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem Biol. 2013;8(6):1324-34
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C33H43N7O2
Molecular Weight
569.74
CAS #
1431612-23-5
SMILES
O=C(C1C([H])=C(C([H])=C2C=1C([H])=NN2C([H])(C([H])([H])[H])C([H])([H])[H])C1=C([H])N=C(C([H])=C1[H])N1C([H])([H])C([H])([H])N(C([H])(C([H])([H])[H])C([H])([H])[H])C([H])([H])C1([H])[H])N([H])C([H])([H])C1C(N([H])C(C([H])([H])[H])=C([H])C=1C([H])([H])C([H])([H])C([H])([H])[H])=O
InChi Key
DPJNKUOXBZSZAI-UHFFFAOYSA-N
InChi Code
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)
Chemical Name
1-isopropyl-6-(6-(4-isopropylpiperazin-1-yl)pyridin-3-yl)-N-((6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl)-1H-indazole-4-carboxamide
Synonyms
UNC1999; UNC 1999; UNC-1999;
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 100 mg/mL (175.5 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.7552 mL 8.7759 mL 17.5519 mL
5 mM 0.3510 mL 1.7552 mL 3.5104 mL
10 mM 0.1755 mL 0.8776 mL 1.7552 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

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Biological Data
  • UNC1999
    Biotinylated UNC1999 (UNC2399) enriches EZH2 from HEK293T cell lysates. ACS Chem Biol. 2013 Jun 21; 8(6): 1324–1334.
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