MK-1775 sarms powder for muscle growth
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Product Name: MK-1775
Alias: MK1775, MK 1775
Appearance: yellow powder
Brand Nmae: HKYC
Storage: store at 0-5 ºC
Usage:MK-1775 is an inhibitor of the checkpoint kinase Wee1V
Payment terms: T/T, Western Union, Money Gram, Bitcoin
What is MK-1775?
MK-1775 is an inhibitor of the checkpoint kinase Wee1 (IC50 = 5.2 nM).1 It has been shown to inhibit the phosphorylation of Cdc2 at tryosine-15, which abrogates the G2 DNA damage checkpoint.1 In p53-deficient tumors that rely solely on the G2 checkpoint upon DNA damage, MK-1775, in combination with DNA-damaging chemotherapeutic agents, is reported to induce apoptosis in vitro and potentiate the inhibition of tumor growth in vivo.
MK-1775 treatment led to the inhibition of Wee1 kinase and reduced inhibitory phosphorylation of its substrate Cdc2. MK-1775, when dosed with gemcitabine, abrogated the checkpoint arrest to promote mitotic entry and facilitated tumor cell death as compared to control and gemcitabine treated tumors. MK-1775 monotherapy did not induce tumor regressions. However, the combination of gemcitabine with MK-1775 produced robust anti-tumor activity and remarkably enhanced tumor regression response (4.01 fold) compared to gemcitabine treatment in p53-deficient tumors. Tumor re-growth curves plotted after the drug treatment period suggest that the effect of the combination therapy is longer-lasting than that of gemcitabine. None of the agents produced tumor regressions in p53-wild type xenografts.
MK-1775 inhibits Wee1 kinase in an ATP-competitive manner. Compared to Wee1, MK-1775 displays 2- to 3-fold less potency against Yes with IC50 of 14 nM, 10-fold less potency against seven other kinases with >80% inhibition at 1 μM, and >100-fold selectivity over human Myt 1, another kinase that inhibits cyclin-dependent kinase 1 (CDC2) by phosphorylation at an alternative site (Thr14).
By abrogating the DNA damage checkpoint via blockade of Wee1 activity in WiDr cells bearing mutated p53, MK-1775 treatment inhibits the basal phosphorylation of CDC2 at Tyr15 (CDC2Y15) with EC50 of 49 nM, and suppresses gemcitabine-, carboplatin- or cisplatin-induced phosphorylation of CDC2 and cell cycle arrest in a dose-dependent manner, with EC50 of 82 nM and 81 nM, 180 nM and 163 nM, as well as 159 nM and 160 nM, respectively. MK-1775 treatment alone at 30-100 nM has no significant antiproliferative effect in WiDr and H1299 cells, whereas MK-1775 at 300 nM, sufficient to inhibit Wee1 by >80%, displays moderate but significant antiproliferative effects by 34.1% in WiDr cells and 28.4% in H1299 cells.
Packaging & Service:
1. Mass stock, to make sure delivery promptly every day when the payment is done.
2. Having been engaged in this field for years, we have sophisticated and professional logistics department, which can guarantee safe and speedy delivery.
3. Well-trained and disciplined packing team which is professional enough to provide you a safe package. It also avoid a lot of emergency happen during the delivery so that high customs pass is guaranteed. Unique ways to ship 10grams to 25 kilograms powders(or 100ml to 30 Liter liquids) at one time to your destination.
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5. Perfect after-sale service: Any questions or problems happened after receiving the product.
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