2. PROTAC Epigenetics
  3. PROTACs Histone Methyltransferase
  4. NUCC-0226272

NUCC-0226272 is a potent PROTAC that targets EZH2 for degradation. NUCC-0226272 has anti-proliferative effect. NUCC-0226272 has the potential for cancer research.

For research use only. We do not sell to patients.

NUCC-0226272 Chemical Structure

NUCC-0226272 Chemical Structure

CAS No. : 3004503-12-9

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5 mg USD 437 In-stock
10 mg USD 700 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

NUCC-0226272 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

NUCC-0226272 is a potent PROTAC that targets EZH2 for degradation. NUCC-0226272 has anti-proliferative effect. NUCC-0226272 has the potential for cancer research[1].

IC50 & Target[1]

EZH2

 

In Vitro

NUCC-0226272 (0.01-10 μM; 5 days) shows anti-proliferative effect in LNCaP and 22Rv1 cells[1].
NUCC-0226272 (10 μM; 6 days) shows strong degradation of EZH2, as well as reduction of PRC2 component SUZ12, and reduced H3K27me3 levels in C4-2B cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

NUCC-0226272 Related Antibodies
In Vivo

Pharmacokinetic Parameters of NUCC-0226272 in C57Bl/6 mouse[1].

IP (4 mg/kg)
Tmax (h) 0.83
Cmax (ng/mL) 3650
AUClast (min·ng/mL) 12777389
t1/2 (h) 3.46
CL (mL/min/kg) 3.11
Vss (L/kg) 3.11

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

1182.56

Formula

C67H91N9O8S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CCN(C1CCOCC1)C2=CC(C3=CC=C(C=C3)CN4CCN(CC4)C(CCCCCCCCCC(N[C@@H](C(C)(C)C)C(N5[C@@H](C[C@H](C5)O)C(NCC6=CC=C(C7=C(N=CS7)C)C=C6)=O)=O)=O)=O)=CC(C(NCC8=C(C=C(NC8=O)C)C)=O)=C2C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (84.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.8456 mL 4.2281 mL 8.4562 mL
5 mM 0.1691 mL 0.8456 mL 1.6912 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 3.5 mg/mL (2.96 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 3.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.68%

SDS (251 KB)

COA (247 KB) HNMR (420 KB) RP-HPLC (263 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.8456 mL 4.2281 mL 8.4562 mL 21.1406 mL
5 mM 0.1691 mL 0.8456 mL 1.6912 mL 4.2281 mL
10 mM 0.0846 mL 0.4228 mL 0.8456 mL 2.1141 mL
15 mM 0.0564 mL 0.2819 mL 0.5637 mL 1.4094 mL
20 mM 0.0423 mL 0.2114 mL 0.4228 mL 1.0570 mL
25 mM 0.0338 mL 0.1691 mL 0.3382 mL 0.8456 mL
30 mM 0.0282 mL 0.1409 mL 0.2819 mL 0.7047 mL
40 mM 0.0211 mL 0.1057 mL 0.2114 mL 0.5285 mL
50 mM 0.0169 mL 0.0846 mL 0.1691 mL 0.4228 mL
60 mM 0.0141 mL 0.0705 mL 0.1409 mL 0.3523 mL
80 mM 0.0106 mL 0.0529 mL 0.1057 mL 0.2643 mL
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NUCC-0226272 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NUCC-02262723004503-12-9NUCC0226272NUCC 0226272PROTACsHistone MethyltransferaseInhibitorinhibitorinhibit

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