GLPBio

UNC1999

Catalog No.: GC11375Purity:>99.50%
COASDSData Sheet
UNC1999 ist ein SAM-kompetitiver, potenter und selektiver Inhibitor von EZH2/1 mit IC50-Werten von <10 nM bzw. 45 nM.

Die Produkte sind ausschließlich für Forschungszwecke bestimmt. Nicht zur Anwendung am Menschen. Wir verkaufen nicht an Patienten.

UNC1999
Cas No.: 1431612-23-5
10mM (in 1mL DMSO)In Stock
$63.00
1
1mgIn Stock
$20.00
1
10mgIn Stock
$78.00
1
5mgIn Stock
$50.00
1
25mgIn Stock
$140.00
1
50mgIn Stock
$224.00
1
100mgIn Stock
$349.00
1
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    187(9):2288-2304 (2024)
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Beschreibung (Description)

UNC1999 is an orally active inhibitor of EZH2 (IC50=2nM) and EZH1 (IC50=45nM)[1-2]. UNC1999 can be used to investigate the mechanisms of EZH2 and EZH1 in gene expression regulation, cancer development, and stem cell maintenance[3-4].

In vitro, treatment of human colorectal cancer cells (HCT116, LoVo, HCT-15, DLD-1) with UNC1999 (2.5–5μM) for 24–72 hours induces autophagy by upregulating LC3B gene expression transcriptionally, activates endoplasmic reticulum (ER) stress and the PERK/eIF2α pathway of the unfolded protein response (UPR), ultimately promoting tumor cell death[5]. UNC1999 (0.1–100μM) treatment of human bladder cancer cell lines E-J and 5637 for 24–120 hours, UNC1999 significantly inhibits cell proliferation and migration while inducing apoptosis by suppressing EZH2 activity and blocking the JAK2/STAT3 signaling pathway[6].

In vivo, intraperitoneal injection of UNC1999 (15–25mg/kg) twice weekly for 3 weeks in NOG mice bearing MM.1S human multiple myeloma xenografts significantly inhibits tumor growth and prolongs survival[7]. Intraperitoneal injection of UNC1999 (25mg/kg) twice weekly for 4 weeks in BALB/c nude mice inoculated with Y79 human retinoblastoma cells significantly suppresses the growth of subcutaneous xenograft tumors[8].

References:
[1] Zhou C, He A, Kang Q, et al. Development of a UPLC-MS/MS method for determination of a dual EZH1/2 inhibitor UNC1999 in rat plasma. Bioanalysis. 2022 Jan;14(2):67-74.
[2] Xu B, On DM, Ma A, et al. Selective inhibition of EZH2 and EZH1 enzymatic activity by a small molecule suppresses MLL-rearranged leukemia. Blood. 2015 Jan 8;125(2):346-57.
[3] Shinno Y, Takenobu H, Sugino RP, et al. Polycomb EZH1 regulates cell cycle/5-fluorouracil sensitivity of neuroblastoma cells in concert with MYCN. Cancer Sci. 2022 Dec;113(12):4193-4206.
[4] Zhang Q, Deng X, Tang X, et al. MicroRNA-20a Suppresses Tumor Proliferation and Metastasis in Hepatocellular Carcinoma by Directly Targeting EZH1. Front Oncol. 2021 Dec 16;11:737986.
[5] Hsieh YY, Lo HL, Yang PM. EZH2 inhibitors transcriptionally upregulate cytotoxic autophagy and cytoprotective unfolded protein response in human colorectal cancer cells. Am J Cancer Res. 2016 Aug 1;6(8):1661-80.
[6] Chen Z, Du Y, Liu X, et al. EZH2 inhibition suppresses bladder cancer cell growth and metastasis via the JAK2/STAT3 signaling pathway. Oncol Lett. 2019 Jul;18(1):907-915.
[7] Rizq O, Mimura N, Oshima M, et al. Dual Inhibition of EZH2 and EZH1 Sensitizes PRC2-Dependent Tumors to Proteasome Inhibition. Clin Cancer Res. 2017 Aug 15;23(16):4817-4830. doi: 10.1158/1078-0432.CCR-16-2735.
[8] Zhao Y, Cheng Y, Qu Y. The role of EZH2 as a potential therapeutic target in retinoblastoma. Exp Eye Res. 2023 Feb;227:109389.

Protokoll (Protocol)

Cell experiment [1]:

Cell lines

E-J and 5637 cells (human bladder cancer cell lines)

Preparation Method

E-J and 5637 cells were maintained in RPMI 1640 medium supplemented with 10% fetal bovine serum (FBS) at 37°C, 5% CO₂. Cells were treated with the EZH2 inhibitor UNC1999 at concentrations of 0.1, 1, 10, and 100µM for 24, 72, and 120 hours.

Reaction Conditions

0.1-100µM; 24-120h

Applications

UNC1999 significantly inhibited the proliferation of bladder cancer cells in a dose- and time-dependent manner. UNC1999 induced significant apoptosis and suppressed cell migration and invasion. Mechanistically, UNC1999 reduced the phosphorylation levels of JAK2 and STAT3, indicating inhibition of the JAK2/STAT3 signaling pathway.

Animal experiment [2]:

Animal models

BALB/c nude mice

Preparation Method

Y79 retinoblastoma cells were subcutaneously injected into the posterior flank of female BALB/c nude mice. After one week of tumor growth, mice were randomly divided into two groups. One group was treated with UNC1999 (25mg/kg, i.p.) twice a week for 3 weeks. The control group received intraperitoneal injections of vehicle (5% DMSO in corn oil). Tumor volume was measured three times per week. Mice were sacrificed after 4 weeks, and tumors were collected for further analysis.

Dosage form

25mg/kg; i.p.; Twice per week for 3 weeks

Applications

UNC1999 administration significantly inhibited the growth of retinoblastoma xenograft tumors in vivo compared to the vehicle control. UNC1999 treatment reduced the protein levels of EZH2 and phosphorylated STAT3 (pY-STAT3) while increasing the expression of FoxO1 in the excised tumors.

References:
[1] Chen Z, Du Y, Liu X, et al. EZH2 inhibition suppresses bladder cancer cell growth and metastasis via the JAK2/STAT3 signaling pathway. Oncol Lett. 2019 Jul;18(1):907-915.
[2] Zhao Y, Cheng Y, Qu Y. The role of EZH2 as a potential therapeutic target in retinoblastoma. Exp Eye Res. 2023 Feb;227:109389.

Produktdokumente (Product Documents)

Purity:>99.50%Appearance:A solid
COASDSData Sheet

Chemische Eigenschaften (Chemical Properties)

CAS-Nr.
1431612-23-5
Chemischer 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
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
Summenformel
C33H43N7O2
Molekulargewicht
569.74
Löslichkeit
≥ 28.5mg/mL in DMSO
Lagerung
Store at -20° C
Allgemeine Hinweise
Wählen Sie anhand der Löslichkeitsdaten des Produkts ein geeignetes Lösungsmittel. Aliquotieren Sie die Stammlösung nach der Herstellung, um wiederholte Gefrier-Auftau-Zyklen zu vermeiden.
Verwenden Sie Stammlösungen bei Lagerung bei -80°C innerhalb von 6 Monaten bzw. bei -20°C innerhalb von 1 Monat.
Zur Verbesserung der Löslichkeit das Röhrchen auf 37°C erwärmen und für eine angemessene Dauer beschallen.
Versandbedingungen
Evaluierungsmuster werden mit Kühlakkus versandt. Andere verfügbare Größen werden bei Raumtemperatur oder auf Anfrage mit Kühlakkus versandt.

Rechner (Calculators)Molarität / Verdünnung / Molekulargewicht / Einheitenumrechnung / In-vivo-Formulierung / Löslichkeit

g/mol

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