[CAS NO. 1629052-78-3] KZR-504

Name: KZR-504
Brand: Arctom Scientific
SKU: AS380041

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PRODUCTS SPECIFICATIONS [1629052-78-3]

Fulfillment

Catalog

AS380041

Brand

Arctom Scientific

CAS

1629052-78-3

DESCRIPTION [1629052-78-3]

Overview

MDL	MFCD31746873
Molecular Weight	413.42
Molecular Formula	C21H23N3O6
SMILES	O=C(N[C@@H](CO)C(N[C@@H](CC1=CC=CC=C1)C([C@]2(CO2)C)=O)=O)C(N3)=CC=CC3=O

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

Summary

KZR-504 is a highly selective inhibitor of immunoproteasome low molecular mass polypeptide 2 (LMP2) , with IC ₅₀ s of 51 nM, 4.274 μM for LMP2 and LMP7, respectively. KZR-504 is of interest for the treatment of autoimmune disease ^[1] .

IC50 & Target

IC50: 51 nM (LMP2), 4.274 μM (LMP7) ^[1] .

In Vivo

Evaluating the inhibition of LMP2, and antitargets LMP7 and β5, in mouse tissues reveals that KZR-504 (compound 12) is both selective and potent in vivo with >50% target inhibition achieved at >1 mg/kg in all tissues tested except brain ^[1] .

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

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility

In Vitro:

DMSO : 170 mg/mL ( 411.20 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4188 mL	12.0942 mL	24.1885 mL
5 mM	0.4838 mL	2.4188 mL	4.8377 mL
10 mM	0.2419 mL	1.2094 mL	2.4188 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

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

Solubility: ≥ 4.25 mg/mL (10.28 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 4.25 mg/mL (10.28 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 4.25 mg/mL (10.28 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Johnson HWB, et al. Discovery of Highly Selective Inhibitors of the Immunoproteasome Low Molecular Mass Polypeptide 2 (LMP2) Subunit. ACS Med Chem Lett. 2017 Mar 9;8(4):413-417.