Z-IETD-FMK

Biological Activity

Z-IETD-FMK is a specific Caspase-8 inhibitor.

Customer Product Validations & Biological Datas

	Source	Mar Drugs (2018). Figure 6. Z-IETD-FMK
	Method	MTT assay
	Cell Lines	MG63 cells
	Concentrations	10 μM
	Incubation Time	24 h
	Results	These data indicated that MSP-4 induced cytotoxicity and caspase-dependent apoptosis, but pretreatment with Z-IETD-FMK (caspase-8 inhibitor) or Z-LEHD-FMK (caspase-9 inhibitor) sharply suppressed the cells’ cytotoxicity and caspase expression in Western blots.

Chemical Information

Molecular Weight	654.68
Formula	C30H43FN4O11
CAS Number	210344-98-2
Solubility (25°C)	DMSO ≥ 66 mg/mL
Storage	Powder          -20°C   3 years ;  4°C   2 years In solvent       -80°C   6 months ;  -20°C   1 month

Conversion of different model animals based on BSA (PMID: 27057123)

Species	Mouse	Rat	Rabbit	Guinea pig	Hamster	Dog
Weight (kg)	0.02	0.15	1.8	0.4	0.08	10
Body Surface Area (m2)	0.007	0.025	0.15	0.05	0.02	0.5
Km factor	3	6	12	8	5	20

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Y Niu, et al. The application of apoptotic inhibitor in apoptotic pathways of MII stage porcine oocytes after vitrification

[2] Wei Chi, et al. HMGB1 promotes the activation of NLRP3 and caspase-8 inflammasomes via NF-κB pathway in acute glaucoma

[3] C P Lawrence, et al. Suppression of human T cell proliferation by the caspase inhibitors, z-VAD-FMK and z-IETD-FMK is independent of their caspase inhibition properties

[4] Andrew S Cowburn, et al. z-VAD-fmk augmentation of TNF alpha-stimulated neutrophil apoptosis is compound specific and does not involve the generation of reactive oxygen species

[5] N Ozoren, et al. The caspase 9 inhibitor Z-LEHD-FMK protects human liver cells while permitting death of cancer cells exposed to tumor necrosis factor-related apoptosis-inducing ligand