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HYPOTHEMYCIN

HYPOTHEMYCIN Struktur
76958-67-3
CAS-Nr.
76958-67-3
Englisch Name:
HYPOTHEMYCIN
Synonyma:
f 152 D2;Nsc354462;HYPOTHEMYCIN;Hypothemicin;Hypothemycin, MEK inhibitor;Hypothemycin - CAS 76958-67-3 - Calbiochem;(1aR,3S,4S,6Z,9S,15bR)-1a,8,9,15b-Tetrahydro-3,4,12-trihydroxy-14-methoxy-9-methyl-3H-oxireno[k][2]benzoxacyclotetradecin-5,11(2H,4H)-dione;(1aR,3S,4S,6Z,9S,15bR)-1a,8,9,15b-Tetrahydro-3,4,12-trihydroxy-9-methyl-14-methoxy-3H-oxireno[k][2]benzoxacyclotetradecin-5,11(2H,4H)-dione;(1aR,3S,4S,6Z,9S,15bR)-1a,2,4,5,11,8,9,15b-Octahydro-3,4,12-trihydroxy-9-methyl-14-methoxy-3H-oxireno[k][2]benzoxacyclotetradecin-5,11-dione;3H-Oxireno[k][2]benzoxacyclotetradecin-5,11(2H,4H)-dione,1a,8,9,15b-tetrahydro-3,4,12-trihydroxy-14-methoxy-9-methyl-,(1aR,3S,4S,6Z,9S,15bR)-
CBNumber:
CB3229169
Summenformel:
C19H22O8
Molgewicht:
378.37
MOL-Datei:
76958-67-3.mol

HYPOTHEMYCIN Eigenschaften

Schmelzpunkt:
170-172℃
storage temp. 
-20°C
L?slichkeit
DMSO: soluble
Aggregatzustand
Lyophilized solid
Farbe
White
Stabilit?t:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Sicherheit
  • Risiko- und Sicherheitserkl?rung
  • Gefahreninformationscode (GHS)
Kennzeichnung gef?hrlicher Xn
R-S?tze: 22
WGK Germany  3
HS Code  29419000
Bildanzeige (GHS) GHS hazard pictograms
Alarmwort Warnung
Gefahrenhinweise
Code Gefahrenhinweise Gefahrenklasse Abteilung Alarmwort Symbol P-Code
H302 Gesundheitssch?dlich bei Verschlucken. Akute Toxizit?t oral Kategorie 4 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P270, P301+P312, P330, P501
Sicherheit

HYPOTHEMYCIN Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden

Hypothemycin is a potent and selective inhibitor of threonine/tyrosine-specific kinase, MEK, and other protein kinases that contain a conserved cysteine residue in the ATP-binding site in in vitro studies.

Allgemeine Beschreibung

A cell-permeable cis-enone resorlic acid lactone (RAL) and (5Z)-7-Oxozeaenol (Cat. No. 499610) analog that inhibits several kinases via an initial affinity binding to the ATP pocket, followed by a covalent adduct formation with a conserved ATP site cysteine residue of the targeted enzymes, including, but not limited to, Flt1/VEGFR-1, Flt3, cKit(D816V), MAPK1, MAPK2, MEK1, MKK6, PKCμ, PKD2, PRAK, and Tak1 (≥90% inhibition at 2 μM). Hypothemycin is also reported to inhibit two non-RAL targets (99% and 82% inhibition of TrkA and TrkB, respectively, at 2 μM), while one of the 46 putative cis-enone RALs targets, namely GSK-3α, is shown not to be affected. Hypothemycin inhibits multiple kinases involved in MAP kinase pathways and is therefore particularly effective in inhibiting BRAF(V600E)-dependent tumor growth. (5Z)-Zeaenol (Cat. No. 499609) may serve as a negative control.

Biochem/physiol Actions

Hypothemycin, one of the highly oxygenated analogues in the group of 14-membered resorcylic acid lactones (RAL), has minor antifungal and cytotoxic activity and exhibits an in vitro anti-malarial activity with an IC50 of 2.2 μg/mL. Hypothemycin is also reported to selectively and irreversibly inhibit protein kinases that contain a conserved cysteine residue (Cys166) that is located within the ATP-binding domain. Though this group accounts for less then 10% of all identified kinases, there are several targets implicated in aberrant cellular proliferation such as ERKs, MEK, FMS-like tyrosine kinase protein (FLT), and platelet-derived growth factor receptors (PDGFR). In cell culture, hypothemycin displays potent cytotoxicity against cancer cell lines that are dependent on certain activating kinase mutations. Additionally, hypothemycin demonstrates significant tumor growth inhibition in at least three separate murine xenograft models. Hypothemycin also inhibits the production of several cytokines such as IL2, IL6, IFNγ, and TNFα.

HYPOTHEMYCIN Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


HYPOTHEMYCIN Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 32)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
TargetMol Chemicals Inc.
+1-781-999-5354 +1-00000000000
marketing@targetmol.com United States 32161 58
Aladdin Scientific
+1-+1(833)-552-7181
sales@aladdinsci.com United States 52924 58
Shanghai Tauto Biotech Co., Ltd. 021-51320588
tauto@tautobiotech.com China 3989 66
AdooQ BioScience, LLC +1 (866) 930-6790
info@adooq.com United States 2782 58
Sigma-Aldrich 021-61415566 800-8193336
orderCN@merckgroup.com China 51456 80
Shanghai EFE Biological Technology Co., Ltd. 021-65675885 18964387627
info@efebio.com China 9806 58
Lynnchem 86-(0)29-85992781 17792393971
info@lynnchem.com China 4587 58
Novachemistry 44-20819178-90 02081917890
info@novachemistry.com United Kingdom 4381 58
Shenzhen Regent Biochemical Technology Co., Ltd. 0755-0755-85201366 18938635012
sales@regentsciences.com China 9371 58
Shanghai Hongye Biotechnology Co. Ltd 400-9205774
sales@glpbio.cn China 6777 58

76958-67-3()Verwandte Suche:


  • HYPOTHEMYCIN
  • (1aR,3S,4S,6Z,9S,15bR)-1a,2,4,5,11,8,9,15b-Octahydro-3,4,12-trihydroxy-9-methyl-14-methoxy-3H-oxireno[k][2]benzoxacyclotetradecin-5,11-dione
  • (1aR,3S,4S,6Z,9S,15bR)-1a,8,9,15b-Tetrahydro-3,4,12-trihydroxy-9-methyl-14-methoxy-3H-oxireno[k][2]benzoxacyclotetradecin-5,11(2H,4H)-dione
  • Hypothemicin
  • Nsc354462
  • 3H-Oxireno[k][2]benzoxacyclotetradecin-5,11(2H,4H)-dione,1a,8,9,15b-tetrahydro-3,4,12-trihydroxy-14-methoxy-9-methyl-,(1aR,3S,4S,6Z,9S,15bR)-
  • (1aR,3S,4S,6Z,9S,15bR)-1a,8,9,15b-Tetrahydro-3,4,12-trihydroxy-14-methoxy-9-methyl-3H-oxireno[k][2]benzoxacyclotetradecin-5,11(2H,4H)-dione
  • f 152 D2
  • Hypothemycin - CAS 76958-67-3 - Calbiochem
  • Hypothemycin, MEK inhibitor
  • 76958-67-3
  • Antibiotic
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