There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
Maritoclax is a selective Mcl-1 inhibitor with IC50 value of 10.1μM against the binding of a biotinylated Bim BH3 peptide to Mcl-1 protein, but with IC50 value>80μM for Bcl-XL. Maritoclax induced cell death with EC50 value of 1.6μM in K562 cells retrovirally transduced Mcl-1-IRES-BimEL and also exhibited anti-proliferation against primary large-granular lymphocyte leukemia (LGLL) cells with EC50 values ranging in 4.64-40μM correlated to the Mcl-1 level. Maritoclax at dose ranging in 1.5-2.5μM induced proteasome-mediated Mcl-1 degradation in Mcl-1-IRES-BimEL K562 cells at 12h post treatment, without induction of Mcl-1 phosphorylation and Noxa expression. Maritoclax, at concentration of 2 or 2.5μM, synergistically sensitized lymphoma/leukemia K562 cells and Raji cells to ABT-737, respectively, at 24h post treatment[1]. Also Maritoclax could exhibited cytotoxicity in Mcl-1-independent manner in cells such as RS4;11 human leukemia cell line which have previously been shown to be dependent on Bcl-2 for survival[2].
作用机制
Maritoclax blocks the binding of Bim BH3 α-helix to Mcl-1 and induces Mcl-1 degradation, thereby leading to Mcl-1-dependent apoptosis.[1]
Maritoclax 细胞实验
Cell Line
Concentration
Treated Time
Description
References
A549 breast cancer cells
500 nM
To study the activity of marinopyrrole A in A549 breast cancer cells
J Am Chem Soc. 2009 Sep 2;131(34):12094-6.
HCT-116 cells
10 μM
12 h
To study the activity of marinopyrrole A in HCT-116 cells and its binding to actin
J Am Chem Soc. 2009 Sep 2;131(34):12094-6.
SK-Hep1 cells
2 μM
24 h
Maritoclax enhanced TRAIL-induced apoptosis, as evidenced by the accumulation of sub-G1 population and PARP cleavage.
Molecules. 2018 Nov 20;23(11):3030.
A549 cells
2 μM
24 h
Maritoclax enhanced TRAIL-induced apoptosis, as evidenced by the accumulation of sub-G1 population and PARP cleavage.
Molecules. 2018 Nov 20;23(11):3030.
A498 cells
2 μM
24 h
Maritoclax enhanced TRAIL-induced apoptosis, as evidenced by the accumulation of sub-G1 population and PARP cleavage.
Molecules. 2018 Nov 20;23(11):3030.
ACHN cells
2 μM
24 h
Maritoclax enhanced TRAIL-induced apoptosis, as evidenced by the accumulation of sub-G1 population and PARP cleavage.
Molecules. 2018 Nov 20;23(11):3030.
Caki cells
1, 2 μM
24 h
Maritoclax enhanced TRAIL-induced apoptosis, as evidenced by the accumulation of sub-G1 population and PARP cleavage.
Molecules. 2018 Nov 20;23(11):3030.
MRSA
320 nM
Evaluate the inhibitory effect of MA-D1 on GlmS enzymatic activity, results showed that MA-D1 can effectively inhibit GlmS activity with an IC50 value of 320 nM.
ACS Cent Sci. 2024 Oct 25;10(11):2090-2098.
MDA-MB-468 breast cancer cells
3 μM
To evaluate the ability of marinopyrrole derivatives to decrease Mcl-1 levels and induce apoptosis. Results showed that several marinopyrrole derivatives significantly decreased Mcl-1 levels and induced caspase 3 activation.
Eur J Med Chem. 2015 Jan 27;90:315-331.
HL60/VCR cells
1 μM
48 h
maritoclax markedly enhances the efficacy of ABT-737 against HL60/VCR cells by 600-fold at 1 μM
J Biol Chem. 2012 Mar 23;287(13):10224-10235.
Raji cells
2.5 μM
24 h
maritoclax markedly enhances the efficacy of ABT-737 against Raji cells by 2000-fold at 2.5 μM
J Biol Chem. 2012 Mar 23;287(13):10224-10235.
K562 cells
1–2 μM
24 h
maritoclax markedly enhances the efficacy of ABT-737 against K562 cells by 60-fold at 1–2 μM
J Biol Chem. 2012 Mar 23;287(13):10224-10235.
Maritoclax 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
MRSA infection model
Intraperitoneal injection
0.5 and 1 mg/kg
Evaluate the antibacterial efficacy of MA-D1 in MRSA-infected mouse models, results showed that MA-D1 significantly reduced bacterial load and rescued infected mice.
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