1. PROTAC MAPK/ERK Pathway
  2. PROTACs p38 MAPK
  3. NR-11c

NR-11c is a selective and potent p38α PROTAC degrader. NR-11c effectively degrades p38α in a variety of tumor cells. When administered intraperitoneally or intravenously to mice, NR-11c primarily acts in the liver. NR-11c can be used in cancer research. (Pink: p38α inhibitor 5 (HY-159799); Black: linker (HY-159800); Blue: VHL E3 ligase ligand (HY-112078)).

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

NR-11c Chemical Structure

NR-11c Chemical Structure

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Based on 1 publication(s) in Google Scholar

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Description

NR-11c is a selective and potent p38α PROTAC degrader. NR-11c effectively degrades p38α in a variety of tumor cells. When administered intraperitoneally or intravenously to mice, NR-11c primarily acts in the liver. NR-11c can be used in cancer research. (Pink: p38α inhibitor 5 (HY-159799); Black: linker (HY-159800); Blue: VHL E3 ligase ligand (HY-112078))[1].

IC50 & Target[1]

p38α

 

In Vitro

NR-11c (1-1000 nM; 24 h) effectively degrades p38α in a variety of tumor cell lines, among which in MDA-MB-231 cells, DC50 is 11.55 nM[1].

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

Western Blot Analysis[1]

Cell Line: U2OS, MG63, SAOS-2, BBL358, MDA-MB-231 and T47D cells
Concentration: 1 μM
Incubation Time: 24 h
Result: Significantly reduced the level of p38α.
In Vivo

NR-11c (15 mg/kg; intra/peritumoral injection; single dose) down-regulates p38α level in tumor for both administration modes in mouse breast cancer models[1].

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

Molecular Weight

1198.22

Formula

C59H71BrF2N10O8S

Appearance

Solid

SMILES

O=C([C@H]1N(C([C@@H](NC(CCCCCNC(CCCN2N=NC(CCCNC(C3=CC=C(C)C(N4C(C)=CC(OCC5=CC=C(F)C=C5F)=C(Br)C4=O)=C3)=O)=C2)=O)=O)C(C)(C)C)=O)C[C@@H](O)C1)N[C@H](C6=CC=C(C7=C(C)N=CS7)C=C6)C

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 (83.46 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.8346 mL 4.1729 mL 8.3457 mL
5 mM 0.1669 mL 0.8346 mL 1.6691 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 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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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 0.8346 mL 4.1729 mL 8.3457 mL 20.8643 mL
5 mM 0.1669 mL 0.8346 mL 1.6691 mL 4.1729 mL
10 mM 0.0835 mL 0.4173 mL 0.8346 mL 2.0864 mL
15 mM 0.0556 mL 0.2782 mL 0.5564 mL 1.3910 mL
20 mM 0.0417 mL 0.2086 mL 0.4173 mL 1.0432 mL
25 mM 0.0334 mL 0.1669 mL 0.3338 mL 0.8346 mL
30 mM 0.0278 mL 0.1391 mL 0.2782 mL 0.6955 mL
40 mM 0.0209 mL 0.1043 mL 0.2086 mL 0.5216 mL
50 mM 0.0167 mL 0.0835 mL 0.1669 mL 0.4173 mL
60 mM 0.0139 mL 0.0695 mL 0.1391 mL 0.3477 mL
80 mM 0.0104 mL 0.0522 mL 0.1043 mL 0.2608 mL
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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.

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Product Name:
NR-11c
Cat. No.:
HY-159798
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