Bz 423 is a pro-apoptotic 1,4-benzodiazepine compound that can activate Bax and Bak and may be utilized in study/research of autoimmune diseases like lupus erythematosus.

Physicochemical Properties

Molecular Formula	C27H21CLN2O2
Molecular Weight	440.92
Exact Mass	440.129
CAS #	216691-95-1
PubChem CID	644335
Appearance	Light yellow to yellow solid powder
Density	1.318g/cm3
Boiling Point	737.5ºC at 760 mmHg
Flash Point	399.8ºC
Vapour Pressure	1.29E-21mmHg at 25°C
Index of Refraction	1.682
LogP	5.47
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	3
Rotatable Bond Count	3
Heavy Atom Count	32
Complexity	704
Defined Atom Stereocenter Count	0
InChi Key	HIJCSNHREFFOML-UHFFFAOYSA-N
InChi Code	InChI=1S/C27H21ClN2O2/c1-30-25-13-10-21(28)16-23(25)26(19-8-11-22(31)12-9-19)29-24(27(30)32)15-17-6-7-18-4-2-3-5-20(18)14-17/h2-14,16,24,31H,15H2,1H3
Chemical Name	7-chloro-5-(4-hydroxyphenyl)-1-methyl-3-(naphthalen-2-ylmethyl)-3H-1,4-benzodiazepin-2-one
Synonyms	Bz423; Bz 423; Bz-423
HS Tariff Code	2934.99.9001
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)

Biological Activity

ln Vitro

Ramos B cells are rapidly killed by Bz-423, which also increases the superoxide response in Ramos cells. In Ramos cells, Bz-423 activates Bak and Bax but not ASK1/JNK. By altering Mcl-1 expression and functionally activating BH3-only proteins, Bz-423-induced superoxide in Ramos cells activates Bax and Bak [1]. Superoxide levels in MEFs are quickly raised by Bz-423 within an hour, and the extent of the increase depends on the concentration. The apoptosis caused by Bz-423 is dependent on superoxide [2].

References

[1]. Bz-423 superoxide signals B cell apoptosis via Mcl-1, Bak, and Bax. Biochem Pharmacol. 2009 Oct 15;78(8):966-73. [2]. Bz-423 superoxide signals apoptosis via selective activation of JNK, Bak, and Bax. Free Radic Biol Med. 2008 Nov 1;45(9):1232-42.

Solubility Data

Solubility (In Vitro)

DMSO : ≥ 125 mg/mL (~283.50 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.08 mg/mL (4.72 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.72 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.2680 mL	11.3399 mL	22.6799 mL
	5 mM	0.4536 mL	2.2680 mL	4.5360 mL
	10 mM	0.2268 mL	1.1340 mL	2.2680 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.