MarizoMib Property

Melting point:

168-170 °C

Boiling point:

547.0±50.0 °C(Predicted)

Density 

1.348±0.06 g/cm3(Predicted)

storage temp. 

-20°C

solubility 

Soluble in DMSO

form 

powder

pka

13.10±0.20(Predicted)

color 

white to beige

Safety

RTECS 

RN6803500

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H315Causes skin irritation

H361Suspected of damaging fertility or the unborn child

H372Causes damage to organs through prolonged or repeated exposure

Precautionary statements

P201Obtain special instructions before use.

P202Do not handle until all safety precautions have been read and understood.

P260Do not breathe dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P281Use personal protective equipment as required.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P308+P313IF exposed or concerned: Get medical advice/attention.

P314Get medical advice/attention if you feel unwell.

P321Specific treatment (see … on this label).

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

P405Store locked up.

P501Dispose of contents/container to..…

MarizoMib Chemical Properties,Usage,Production

Uses

Marizomib has been used as a proteasome inhibitor:

• to study its effects on glioblastoma cell lines
• to analyze its effects on the aging of killifish brain
• to test its effect on protein kinase B (PKB/AKT) levels in multiple myeloma cells

Definition

ChEBI: A salinosporamide in which the core (1R)-6-oxa-2-azabicyclo[3.2.0]heptane-3,7-dione skeleton is substituted at positions 1, 4, and 5 by (1S)-cyclohex-2-en-1-yl(hydroxy)methyl, 2-chloroethyl, and methyl groups, respectively (the 1R,4R,5S diastereoisomer). A potent proteasome inhibitor, it has attracted interest for potential use in the treatment of various cancers.

Biological Activity

salinosporamide a is a potent inhibitor of 20s proteasome with ic50 value of 1.3 nm [1].salinosporamide a was isolated from the crude extract of a salinospora strain cnb-392. it showed potent anti-tumor activity with an ic50 value of 11 ng/ml in hct-116 cells. it also exerted a mean gi50 value of less than 10 nm in the nci’s 60 cell line-panel. among these cell lines, salinosporamide a showed the greatest potent efficacies in nci-h226, sf-539, sk-mel-28 and mda-mb-435 cells. salinosporamide a inhibited the purified 20s proteasome with ic50 value of 1.3 nm. it was about 35-fold more potent than the first discovered specific proteasome inhibitor, omuralide [1].

Biochem/physiol Actions

Marizomib is a second generation proteasome inhibitor with anti-cancer activity. Marizomib binds irreversibly and potently inhibits all three 20S proteasome subunits.

target

CT-L (EC50）

References

[1] feling r h, buchanan g o, mincer t j, et al. salinosporamide a: a highly cytotoxic proteasome inhibitor from a novel microbial source, a marine bacterium of the new genus salinospora. angewandte chemie international edition, 2003, 42(3): 355-357.