nur für Forschungszwecke

Salubrinal PERK Modulator

Kat.-Nr.S2923

Salubrinal ist ein selektiver Inhibitor der eIF2α-Dephosphorylierung und hemmt die ER-Stress-vermittelte Apoptosis mit einem EC50 von ~15 μM in einem zellfreien Assay.
Salubrinal PERK Modulator Chemical Structure

Chemische Struktur

Molekulargewicht: 479.81

Springe zu

Qualitätskontrolle

Charge: Reinheit: 99.94%
99.94

Zellkultur, Behandlung & Arbeitskonzentration

Zelllinien Assay-Typ Konzentration Inkubationszeit Formulierung Aktivitätsbeschreibung PMID
LP-1 Growth inhibition assay Inhibition of human LP-1 cell growth in a cell viability assay, IC50 = 3.37112 μM. SANGER
697 Growth inhibition assay Inhibition of human 697 cell growth in a cell viability assay, IC50 = 3.98788 μM. SANGER
ALL-PO Growth inhibition assay Inhibition of human ALL-PO cell growth in a cell viability assay, IC50 = 4.08655 μM. SANGER
ML-2 Growth inhibition assay Inhibition of human ML-2 cell growth in a cell viability assay, IC50 = 4.61833 μM. SANGER
LB2241-RCC Growth inhibition assay Inhibition of human LB2241-RCC cell growth in a cell viability assay, IC50 = 4.98572 μM. SANGER
Becker Growth inhibition assay Inhibition of human Becker cell growth in a cell viability assay, IC50 = 5.79401 μM. SANGER
NEC8 Growth inhibition assay Inhibition of human NEC8 cell growth in a cell viability assay, IC50 = 6.05331 μM. SANGER
Daudi Growth inhibition assay Inhibition of human Daudi cell growth in a cell viability assay, IC50 = 6.33699 μM. SANGER
MHH-PREB-1 Growth inhibition assay Inhibition of human MHH-PREB-1 cell growth in a cell viability assay, IC50 = 6.78817 μM. SANGER
NCI-H510A Growth inhibition assay Inhibition of human NCI-H510A cell growth in a cell viability assay, IC50 = 7.03535 μM. SANGER
NCI-H720 Growth inhibition assay Inhibition of human NCI-H720 cell growth in a cell viability assay, IC50 = 7.57268 μM. SANGER
MRK-nu-1 Growth inhibition assay Inhibition of human MRK-nu-1 cell growth in a cell viability assay, IC50 = 7.75171 μM. SANGER
LB2518-MEL Growth inhibition assay Inhibition of human LB2518-MEL cell growth in a cell viability assay, IC50 = 7.97326 μM. SANGER
BE-13 Growth inhibition assay Inhibition of human BE-13 cell growth in a cell viability assay, IC50 = 8.2684 μM. SANGER
A3-KAW Growth inhibition assay Inhibition of human A3-KAW cell growth in a cell viability assay, IC50 = 8.43289 μM. SANGER
ST486 Growth inhibition assay Inhibition of human ST486 cell growth in a cell viability assay, IC50 = 8.5368 μM. SANGER
ES8 Growth inhibition assay Inhibition of human ES8 cell growth in a cell viability assay, IC50 = 8.64339 μM. SANGER
HT Growth inhibition assay Inhibition of human HT cell growth in a cell viability assay, IC50 = 8.94185 μM. SANGER
HAL-01 Growth inhibition assay Inhibition of human HAL-01 cell growth in a cell viability assay, IC50 = 9.31505 μM. SANGER
EB-3 Growth inhibition assay Inhibition of human EB-3 cell growth in a cell viability assay, IC50 = 9.62572 μM. SANGER
EW-1 Growth inhibition assay Inhibition of human EW-1 cell growth in a cell viability assay, IC50 = 9.7124 μM. SANGER
BL-41 Growth inhibition assay Inhibition of human BL-41 cell growth in a cell viability assay, IC50 = 9.78049 μM. SANGER
Ramos-2G6-4C10 Growth inhibition assay Inhibition of human Ramos-2G6-4C10 cell growth in a cell viability assay, IC50 = 9.90315 μM. SANGER
DOHH-2 Growth inhibition assay Inhibition of human DOHH-2 cell growth in a cell viability assay, IC50 = 10.2262 μM. SANGER
MONO-MAC-6 Growth inhibition assay Inhibition of human MONO-MAC-6 cell growth in a cell viability assay, IC50 = 10.5482 μM. SANGER
NKM-1 Growth inhibition assay Inhibition of human NKM-1 cell growth in a cell viability assay, IC50 = 10.6196 μM. SANGER
HEL Growth inhibition assay Inhibition of human HEL cell growth in a cell viability assay, IC50 = 10.6252 μM. SANGER
8-MG-BA Growth inhibition assay Inhibition of human 8-MG-BA cell growth in a cell viability assay, IC50 = 10.9999 μM. SANGER
K-562 Growth inhibition assay Inhibition of human K-562 cell growth in a cell viability assay, IC50 = 11.0191 μM. SANGER
HC-1 Growth inhibition assay Inhibition of human HC-1 cell growth in a cell viability assay, IC50 = 11.1547 μM. SANGER
LXF-289 Growth inhibition assay Inhibition of human LXF-289 cell growth in a cell viability assay, IC50 = 11.1547 μM. SANGER
MC116 Growth inhibition assay Inhibition of human MC116 cell growth in a cell viability assay, IC50 = 11.2073 μM. SANGER
TE-12 Growth inhibition assay Inhibition of human TE-12 cell growth in a cell viability assay, IC50 = 11.3357 μM. SANGER
BV-173 Growth inhibition assay Inhibition of human BV-173 cell growth in a cell viability assay, IC50 = 11.5021 μM. SANGER
NCCIT Growth inhibition assay Inhibition of human NCCIT cell growth in a cell viability assay, IC50 = 11.6039 μM. SANGER
CESS Growth inhibition assay Inhibition of human CESS cell growth in a cell viability assay, IC50 = 11.6662 μM. SANGER
HUTU-80 Growth inhibition assay Inhibition of human HUTU-80 cell growth in a cell viability assay, IC50 = 11.6704 μM. SANGER
IST-SL2 Growth inhibition assay Inhibition of human IST-SL2 cell growth in a cell viability assay, IC50 = 11.7704 μM. SANGER
ATN-1 Growth inhibition assay Inhibition of human ATN-1 cell growth in a cell viability assay, IC50 = 12.0227 μM. SANGER
HCC1599 Growth inhibition assay Inhibition of human HCC1599 cell growth in a cell viability assay, IC50 = 12.1094 μM. SANGER
NTERA-S-cl-D1 Growth inhibition assay Inhibition of human NTERA-S-cl-D1 cell growth in a cell viability assay, IC50 = 12.8888 μM. SANGER
EVSA-T Growth inhibition assay Inhibition of human EVSA-T cell growth in a cell viability assay, IC50 = 12.9204 μM. SANGER
NALM-6 Growth inhibition assay Inhibition of human NALM-6 cell growth in a cell viability assay, IC50 = 13.093 μM. SANGER
KMOE-2 Growth inhibition assay Inhibition of human KMOE-2 cell growth in a cell viability assay, IC50 = 13.1092 μM. SANGER
HL-60 Growth inhibition assay Inhibition of human HL-60 cell growth in a cell viability assay, IC50 = 13.3308 μM. SANGER
D-542MG Growth inhibition assay Inhibition of human D-542MG cell growth in a cell viability assay, IC50 = 13.4306 μM. SANGER
L-363 Growth inhibition assay Inhibition of human L-363 cell growth in a cell viability assay, IC50 = 13.5583 μM. SANGER
CMK Growth inhibition assay Inhibition of human CMK cell growth in a cell viability assay, IC50 = 13.7436 μM. SANGER
IMR-5 Growth inhibition assay Inhibition of human IMR-5 cell growth in a cell viability assay, IC50 = 13.7849 μM. SANGER
A101D Growth inhibition assay Inhibition of human A101D cell growth in a cell viability assay, IC50 = 13.8206 μM. SANGER
MOLT-16 Growth inhibition assay Inhibition of human MOLT-16 cell growth in a cell viability assay, IC50 = 13.9665 μM. SANGER
LU-139 Growth inhibition assay Inhibition of human LU-139 cell growth in a cell viability assay, IC50 = 14.0444 μM. SANGER
A4-Fuk Growth inhibition assay Inhibition of human A4-Fuk cell growth in a cell viability assay, IC50 = 14.1299 μM. SANGER
J-RT3-T3-5 Growth inhibition assay Inhibition of human J-RT3-T3-5 cell growth in a cell viability assay, IC50 = 14.6941 μM. SANGER
OVCAR-4 Growth inhibition assay Inhibition of human OVCAR-4 cell growth in a cell viability assay, IC50 = 14.7604 μM. SANGER
BC-3 Growth inhibition assay Inhibition of human BC-3 cell growth in a cell viability assay, IC50 = 14.7982 μM. SANGER
D-336MG Growth inhibition assay Inhibition of human D-336MG cell growth in a cell viability assay, IC50 = 15.1134 μM. SANGER
BC-1 Growth inhibition assay Inhibition of human BC-1 cell growth in a cell viability assay, IC50 = 15.198 μM. SANGER
KE-37 Growth inhibition assay Inhibition of human KE-37 cell growth in a cell viability assay, IC50 = 15.2825 μM. SANGER
LAMA-84 Growth inhibition assay Inhibition of human LAMA-84 cell growth in a cell viability assay, IC50 = 15.7455 μM. SANGER
OCI-AML2 Growth inhibition assay Inhibition of human OCI-AML2 cell growth in a cell viability assay, IC50 = 15.9159 μM. SANGER
L-540 Growth inhibition assay Inhibition of human L-540 cell growth in a cell viability assay, IC50 = 15.9712 μM. SANGER
JiyoyeP-2003 Growth inhibition assay Inhibition of human JiyoyeP-2003 cell growth in a cell viability assay, IC50 = 16.0011 μM. SANGER
MEG-01 Growth inhibition assay Inhibition of human MEG-01 cell growth in a cell viability assay, IC50 = 16.057 μM. SANGER
NOS-1 Growth inhibition assay Inhibition of human NOS-1 cell growth in a cell viability assay, IC50 = 16.0998 μM. SANGER
GI-ME-N Growth inhibition assay Inhibition of human GI-ME-N cell growth in a cell viability assay, IC50 = 17.1098 μM. SANGER
NB1 Growth inhibition assay Inhibition of human NB1 cell growth in a cell viability assay, IC50 = 17.2295 μM. SANGER
KU812 Growth inhibition assay Inhibition of human KU812 cell growth in a cell viability assay, IC50 = 17.2534 μM. SANGER
NCI-H1355 Growth inhibition assay Inhibition of human NCI-H1355 cell growth in a cell viability assay, IC50 = 17.3491 μM. SANGER
JAR Growth inhibition assay Inhibition of human JAR cell growth in a cell viability assay, IC50 = 17.4931 μM. SANGER
RPMI-8226 Growth inhibition assay Inhibition of human RPMI-8226 cell growth in a cell viability assay, IC50 = 18.1636 μM. SANGER
CCRF-CEM Growth inhibition assay Inhibition of human CCRF-CEM cell growth in a cell viability assay, IC50 = 18.6377 μM. SANGER
RS4-11 Growth inhibition assay Inhibition of human RS4-11 cell growth in a cell viability assay, IC50 = 18.9889 μM. SANGER
SIG-M5 Growth inhibition assay Inhibition of human SIG-M5 cell growth in a cell viability assay, IC50 = 19.1579 μM. SANGER
Calu-6 Growth inhibition assay Inhibition of human Calu-6 cell growth in a cell viability assay, IC50 = 19.4402 μM. SANGER
NMC-G1 Growth inhibition assay Inhibition of human NMC-G1 cell growth in a cell viability assay, IC50 = 19.64 μM. SANGER
HD-MY-Z Growth inhibition assay Inhibition of human HD-MY-Z cell growth in a cell viability assay, IC50 = 19.9247 μM. SANGER
KS-1 Growth inhibition assay Inhibition of human KS-1 cell growth in a cell viability assay, IC50 = 19.9385 μM. SANGER
IST-SL1 Growth inhibition assay Inhibition of human IST-SL1 cell growth in a cell viability assay, IC50 = 20.4273 μM. SANGER
EM-2 Growth inhibition assay Inhibition of human EM-2 cell growth in a cell viability assay, IC50 = 20.4831 μM. SANGER
NCI-SNU-16 Growth inhibition assay Inhibition of human NCI-SNU-16 cell growth in a cell viability assay, IC50 = 21.0539 μM. SANGER
CTV-1 Growth inhibition assay Inhibition of human CTV-1 cell growth in a cell viability assay, IC50 = 21.5621 μM. SANGER
CTB-1 Growth inhibition assay Inhibition of human CTB-1 cell growth in a cell viability assay, IC50 = 21.604 μM. SANGER
BL-70 Growth inhibition assay Inhibition of human BL-70 cell growth in a cell viability assay, IC50 = 21.6293 μM. SANGER
ONS-76 Growth inhibition assay Inhibition of human ONS-76 cell growth in a cell viability assay, IC50 = 22.3043 μM. SANGER
MOLT-4 Growth inhibition assay Inhibition of human MOLT-4 cell growth in a cell viability assay, IC50 = 22.3794 μM. SANGER
SCC-3 Growth inhibition assay Inhibition of human SCC-3 cell growth in a cell viability assay, IC50 = 22.5454 μM. SANGER
RCC10RGB Growth inhibition assay Inhibition of human RCC10RGB cell growth in a cell viability assay, IC50 = 22.6146 μM. SANGER
HCC2998 Growth inhibition assay Inhibition of human HCC2998 cell growth in a cell viability assay, IC50 = 23.1268 μM. SANGER
NCI-H82 Growth inhibition assay Inhibition of human NCI-H82 cell growth in a cell viability assay, IC50 = 23.2329 μM. SANGER
MV-4-11 Growth inhibition assay Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50 = 23.3519 μM. SANGER
D-247MG Growth inhibition assay Inhibition of human D-247MG cell growth in a cell viability assay, IC50 = 23.554 μM. SANGER
LB771-HNC Growth inhibition assay Inhibition of human LB771-HNC cell growth in a cell viability assay, IC50 = 23.627 μM. SANGER
COR-L279 Growth inhibition assay Inhibition of human COR-L279 cell growth in a cell viability assay, IC50 = 23.8825 μM. SANGER
NOMO-1 Growth inhibition assay Inhibition of human NOMO-1 cell growth in a cell viability assay, IC50 = 23.8983 μM. SANGER
HCC2218 Growth inhibition assay Inhibition of human HCC2218 cell growth in a cell viability assay, IC50 = 24.5033 μM. SANGER
GT3TKB Growth inhibition assay Inhibition of human GT3TKB cell growth in a cell viability assay, IC50 = 24.545 μM. SANGER
NCI-H1581 Growth inhibition assay Inhibition of human NCI-H1581 cell growth in a cell viability assay, IC50 = 24.5661 μM. SANGER
NCI-H69 Growth inhibition assay Inhibition of human NCI-H69 cell growth in a cell viability assay, IC50 = 24.7802 μM. SANGER
OCUB-M Growth inhibition assay Inhibition of human OCUB-M cell growth in a cell viability assay, IC50 = 24.9094 μM. SANGER
DG-75 Growth inhibition assay Inhibition of human DG-75 cell growth in a cell viability assay, IC50 = 25.8203 μM. SANGER
CA46 Growth inhibition assay Inhibition of human CA46 cell growth in a cell viability assay, IC50 = 25.8561 μM. SANGER
TE-9 Growth inhibition assay Inhibition of human TE-9 cell growth in a cell viability assay, IC50 = 26.298 μM. SANGER
MZ2-MEL Growth inhibition assay Inhibition of human MZ2-MEL cell growth in a cell viability assay, IC50 = 26.6189 μM. SANGER
KARPAS-45 Growth inhibition assay Inhibition of human KARPAS-45 cell growth in a cell viability assay, IC50 = 27.3193 μM. SANGER
UACC-257 Growth inhibition assay Inhibition of human UACC-257 cell growth in a cell viability assay, IC50 = 27.5003 μM. SANGER
ES6 Growth inhibition assay Inhibition of human ES6 cell growth in a cell viability assay, IC50 = 28.2266 μM. SANGER
TGW Growth inhibition assay Inhibition of human TGW cell growth in a cell viability assay, IC50 = 28.5191 μM. SANGER
L-428 Growth inhibition assay Inhibition of human L-428 cell growth in a cell viability assay, IC50 = 28.7156 μM. SANGER
COLO-320-HSR Growth inhibition assay Inhibition of human COLO-320-HSR cell growth in a cell viability assay, IC50 = 28.9891 μM. SANGER
TE-10 Growth inhibition assay Inhibition of human TE-10 cell growth in a cell viability assay, IC50 = 29.223 μM. SANGER
COR-L88 Growth inhibition assay Inhibition of human COR-L88 cell growth in a cell viability assay, IC50 = 29.9805 μM. SANGER
LB996-RCC Growth inhibition assay Inhibition of human LB996-RCC cell growth in a cell viability assay, IC50 = 30.0438 μM. SANGER
HCC2157 Growth inhibition assay Inhibition of human HCC2157 cell growth in a cell viability assay, IC50 = 30.1625 μM. SANGER
HT-144 Growth inhibition assay Inhibition of human HT-144 cell growth in a cell viability assay, IC50 = 30.273 μM. SANGER
COLO-684 Growth inhibition assay Inhibition of human COLO-684 cell growth in a cell viability assay, IC50 = 30.4113 μM. SANGER
CP66-MEL Growth inhibition assay Inhibition of human CP66-MEL cell growth in a cell viability assay, IC50 = 30.4775 μM. SANGER
COLO-824 Growth inhibition assay Inhibition of human COLO-824 cell growth in a cell viability assay, IC50 = 30.9352 μM. SANGER
NCI-H209 Growth inhibition assay Inhibition of human NCI-H209 cell growth in a cell viability assay, IC50 = 31.7266 μM. SANGER
RPMI-6666 Growth inhibition assay Inhibition of human RPMI-6666 cell growth in a cell viability assay, IC50 = 32.0896 μM. SANGER
NCI-SNU-5 Growth inhibition assay Inhibition of human NCI-SNU-5 cell growth in a cell viability assay, IC50 = 32.1346 μM. SANGER
NCI-H1963 Growth inhibition assay Inhibition of human NCI-H1963 cell growth in a cell viability assay, IC50 = 32.1673 μM. SANGER
ES1 Growth inhibition assay Inhibition of human ES1 cell growth in a cell viability assay, IC50 = 32.6132 μM. SANGER
SIMA Growth inhibition assay Inhibition of human SIMA cell growth in a cell viability assay, IC50 = 32.64 μM. SANGER
K052 Growth inhibition assay Inhibition of human K052 cell growth in a cell viability assay, IC50 = 32.6965 μM. SANGER
DB Growth inhibition assay Inhibition of human DB cell growth in a cell viability assay, IC50 = 33.1128 μM. SANGER
LAN-6 Growth inhibition assay Inhibition of human LAN-6 cell growth in a cell viability assay, IC50 = 33.1613 μM. SANGER
TE-1 Growth inhibition assay Inhibition of human TE-1 cell growth in a cell viability assay, IC50 = 33.2542 μM. SANGER
PF-382 Growth inhibition assay Inhibition of human PF-382 cell growth in a cell viability assay, IC50 = 34.3366 μM. SANGER
LS-411N Growth inhibition assay Inhibition of human LS-411N cell growth in a cell viability assay, IC50 = 34.6261 μM. SANGER
KNS-81-FD Growth inhibition assay Inhibition of human KNS-81-FD cell growth in a cell viability assay, IC50 = 34.8848 μM. SANGER
DJM-1 Growth inhibition assay Inhibition of human DJM-1 cell growth in a cell viability assay, IC50 = 35.3674 μM. SANGER
MC-CAR Growth inhibition assay Inhibition of human MC-CAR cell growth in a cell viability assay, IC50 = 35.5256 μM. SANGER
GI-1 Growth inhibition assay Inhibition of human GI-1 cell growth in a cell viability assay, IC50 = 35.5327 μM. SANGER
MOLT-13 Growth inhibition assay Inhibition of human MOLT-13 cell growth in a cell viability assay, IC50 = 35.6624 μM. SANGER
KM12 Growth inhibition assay Inhibition of human KM12 cell growth in a cell viability assay, IC50 = 35.7371 μM. SANGER
NCI-H64 Growth inhibition assay Inhibition of human NCI-H64 cell growth in a cell viability assay, IC50 = 35.7738 μM. SANGER
MPP-89 Growth inhibition assay Inhibition of human MPP-89 cell growth in a cell viability assay, IC50 = 36.9055 μM. SANGER
PSN1 Growth inhibition assay Inhibition of human PSN1 cell growth in a cell viability assay, IC50 = 37.1904 μM. SANGER
NCI-H2126 Growth inhibition assay Inhibition of human NCI-H2126 cell growth in a cell viability assay, IC50 = 37.6544 μM. SANGER
EKVX Growth inhibition assay Inhibition of human EKVX cell growth in a cell viability assay, IC50 = 38.3242 μM. SANGER
SHP-77 Growth inhibition assay Inhibition of human SHP-77 cell growth in a cell viability assay, IC50 = 39.3648 μM. SANGER
KMS-12-PE Growth inhibition assay Inhibition of human KMS-12-PE cell growth in a cell viability assay, IC50 = 39.5152 μM. SANGER
RKO Growth inhibition assay Inhibition of human RKO cell growth in a cell viability assay, IC50 = 39.6481 μM. SANGER
SK-LMS-1 Growth inhibition assay Inhibition of human SK-LMS-1 cell growth in a cell viability assay, IC50 = 40.7279 μM. SANGER
DMS-153 Growth inhibition assay Inhibition of human DMS-153 cell growth in a cell viability assay, IC50 = 42.3528 μM. SANGER
GCIY Growth inhibition assay Inhibition of human GCIY cell growth in a cell viability assay, IC50 = 43.1088 μM. SANGER
MFH-ino Growth inhibition assay Inhibition of human MFH-ino cell growth in a cell viability assay, IC50 = 43.6888 μM. SANGER
RXF393 Growth inhibition assay Inhibition of human RXF393 cell growth in a cell viability assay, IC50 = 44.458 μM. SANGER
NB13 Growth inhibition assay Inhibition of human NB13 cell growth in a cell viability assay, IC50 = 44.8691 μM. SANGER
D-392MG Growth inhibition assay Inhibition of human D-392MG cell growth in a cell viability assay, IC50 = 45.4383 μM. SANGER
KNS-42 Growth inhibition assay Inhibition of human KNS-42 cell growth in a cell viability assay, IC50 = 45.5753 μM. SANGER
HOP-62 Growth inhibition assay Inhibition of human HOP-62 cell growth in a cell viability assay, IC50 = 47.6626 μM. SANGER
HCE-T Growth inhibition assay Inhibition of human HCE-T cell growth in a cell viability assay, IC50 = 47.9693 μM. SANGER
MLMA Growth inhibition assay Inhibition of human MLMA cell growth in a cell viability assay, IC50 = 48.8336 μM. SANGER
ECC12 Growth inhibition assay Inhibition of human ECC12 cell growth in a cell viability assay, IC50 = 48.9803 μM. SANGER
no-11 Growth inhibition assay Inhibition of human no-11 cell growth in a cell viability assay, IC50 = 48.9923 μM. SANGER
NCI-H1648 Growth inhibition assay Inhibition of human NCI-H1648 cell growth in a cell viability assay, IC50 = 49.2167 μM. SANGER
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Chemische Informationen, Lagerung & Stabilität

Molekulargewicht 479.81 Formel

C21H17Cl3N4OS

Lagerung (Ab dem Eingangsdatum)
CAS-Nr. 405060-95-9 SDF herunterladen Lagerung von Stammlösungen

Synonyme N/A Smiles C1=CC=C(C=C1)C=CC(=O)NC(C(Cl)(Cl)Cl)NC(=S)NC2=CC=CC3=C2N=CC=C3

Löslichkeit

In vitro
Charge:

DMSO : 96 mg/mL (200.07 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

Molaritätsrechner

Masse Konzentration Volumen Molekulargewicht
Verdünnungsrechner Molekulargewichtsrechner

In vivo
Charge:

In-vivo-Formulierungsrechner (Klare Lösung)

Schritt 1: Geben Sie die untenstehenden Informationen ein (Empfohlen: Ein zusätzliches Tier zur Berücksichtigung von Verlusten während des Experiments)

mg/kg g μL

Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, keine Formulierung. Bitte kontaktieren Sie uns zuerst, wenn es im Abschnitt "Löslichkeit" keine In-vivo-Formulierung gibt.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Berechnungsergebnisse:

Arbeitskonzentration: mg/ml;

Methode zur Herstellung der DMSO-Stammlösung: mg Wirkstoff vorgelöst in μL DMSO ( Konzentration der Stammlösung mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der Wirkstoffcharge überschreitet. )

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügenμL PEG300, mischen und klären, dann hinzufügenμL Tween 80, mischen und klären, dann hinzufügen μL ddH2O, mischen und klären.

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügen μL Maisöl, mischen und klären.

Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, das/die Lösungsmittel der Reihe nach hinzuzufügen. Sie müssen sicherstellen, dass die bei der vorherigen Zugabe erhaltene Lösung eine klare Lösung ist, bevor Sie mit der Zugabe des nächsten Lösungsmittels fortfahren. Physikalische Methoden wie Vortex, Ultraschall oder ein heißes Wasserbad können zur Unterstützung des Lösens verwendet werden.

Wirkmechanismus

Targets/IC50/Ki
eIF2α
(Cell-free assay)
In vitro

Salubrinal ist ein selektiver Inhibitor zellulärer Komplexe, die den eukaryotischen Translationsinitiationsfaktor 2 Untereinheit α (eIF2α) dephosphorylieren. Diese Verbindung hemmte die durch den Proteinglykosylierungsinhibitor Tunicamycin (Tm) induzierte ER-Stress-vermittelte Apoptosis dosisabhängig mit einer medianen effektiven Konzentration (EC50) von ∼ 15 μM. Es unterdrückte auch die Tm-induzierte DNA-Fragmentierung und die Verarbeitung von Caspase-7, einer durch ER-Stress aktivierten Caspase. Diese Chemikalie ist jedoch kein allgemeiner Apoptosis-Inhibitor. Sie induzierte eine schnelle und robuste eIF2α-Phosphorylierung und ihre nachgeschalteten Effekte in PC12-Zellen, einschließlich der Herunterregulierung von Cyclin D1 und der Hochregulierung von GADD34 und CHOP, zwei Proteinen, deren Expression durch eIF2α-Phosphorylierung induziert wird. Dieser Inhibitor hemmt die eIF2α-Dephosphorylierung durch Hemmung des PP1/GADD34-Komplexes. Er hemmt die HSV-Replikation mit einem IC50 von ~ 3μM durch Hemmung der eIF2α-Dephosphorylierung. Diese Verbindung erhöhte den Non-REM-Schlaf (NREM).

In vivo

Salubrinal hemmt die HSV-Replikation in einem Maus-Hornhautinfektionsmodell. Im Vergleich zur Vehikelkontrolle reduzierte die topische Behandlung mit dieser Verbindung den aus Augenabstrichen infizierter Tiere gewonnenen Virustiter signifikant. Die I.C.V.-Verabreichung dieser Chemikalie modifizierte die homöostatische Schlafantwort signifikant.

Literatur

Anwendungen

Methoden Biomarker Bilder PMID
Western blot ATF4 HSF1 / p-HSF1 / ATF3 / c-fos / NFATc1 / RelA GRP78 / p-eIF2α / CHOP
S2923-WB2
27729194

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