SB203580 - Moligand™, 10mM in DMSO , Inhibitor of cyclin G associated kinase;Inhibitor of mitogen-activated protein kinase 11;Inhibitor of mitogen-activated protein kinase 14, CAS No.152121-47-6, Inhibitor of cyclin G associated kinase;Inhibitor of mitogen-activated protein kinase 11;Inhibitor of mitogen-activated protein kinase 14

CAS: 152121-47-6 Cat. No.: S407781 분자식: C₂₁H₁₆FN₃OS 분자량: 377.43 EC 번호: 688-252-3 PubChem CID: 176155

등급 & 순도 Moligand™, 10mM in DMSO

Synonyms

RWJ 64809, PB 203580

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

개요

Information

In vitro

SB203580 inhibits the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC50 of 3–5 μm. SB203580 also inhibits IL-2-induced p70S6 kinase activation, although the concentration required is slightly higher with an IC50 above 10 μm. SB203580 also inhibits the activity of PDK1 in a dose-dependent manner with an IC50 in the 3–10 μm range. SB203580 inhibits p38-MAPK stimulation of MAPKAPK2 with an IC50 of approximately 0.07 μM, whereas inhibits total SAPK/JNK activity with an IC50 of 3–10 μM. SB203580 at higher concentrations activates the ERK pathway, which subsequently enhances NF-κB transcriptional activity. SB203580 induces autophagy in human hepatocellular carcinoma (HCC) cells.

In vivo

SB203580 protects pig myocardium against ischemic injury in an in vivo model. SB203580 is effective to prevent and treat the disease in MRL/lpr mice model of Systemic lupus erythematosus (SLE).
Cell Data

cell lines：

Concentrations：0–30 μM

Incubation Time：1 hour

Powder Purity:≥99%

사양

동의어

RWJ 64809, PB 203580

사양 및 순도

Moligand™, 10mM in DMSO

생화학 및 생리적 메커니즘

SB203580 (RWJ 64809, PB 203580) is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM in THP-1 cells, 10-fold less sensitive to SAPK3(106T) and SAPK4(106T) and blocks PKB phosphorylation with IC50 of 3-5 μM. SB203580 induces mitophagy and autophagy.

보관 조건

Store at -80°C

배송

Dry ice packs + Cold packs

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등급

Moligand™

작업 유형

INHIBITOR

작동 메커니즘

Inhibitor of cyclin G associated kinase;Inhibitor of mitogen-activated protein kinase 11;Inhibitor of mitogen-activated protein kinase 14

이름과 식별자

이성체 SMILES

CS(=O)C1=CC=C(C=C1)C2=NC(=C(N2)C3=CC=NC=C3)C4=CC=C(C=C4)F

WGK 독일

3

PubChem CID

176155

분자량

377.43

관련 대상(인간)

CYP1A2 Tchem Cytochrome P450 1A2 (1 Activities)

Discover Target: CYP1A2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CYP2C19 Tchem Cytochrome P450 2C19 (2 Activities)

Discover Target: CYP2C19

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CYP3A4 Tclin Cytochrome P450 3A4 (1 Activities)

Discover Target: CYP3A4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CYP2C9 Tchem Cytochrome P450 2C9 (1 Activities)

Discover Target: CYP2C9

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GAK Tchem Cyclin-G-associated kinase (3 Activities)

Discover Target: GAK

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

TBXAS1 Tchem Thromboxane-A synthase (1 Activities)

Discover Target: TBXAS1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

RIPK2 Tchem Receptor-interacting serine/threonine-protein kinase 2 (4 Activities)

Discover Target: RIPK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAPK10 Tchem Mitogen-activated protein kinase 10 (1 Activities)

Discover Target: MAPK10

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ALOX5 Tclin Arachidonate 5-lipoxygenase (1 Activities)

Discover Target: ALOX5

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GCGR Tclin Glucagon receptor (1 Activities)

Discover Target: GCGR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

P2RX7 Tchem P2X purinoceptor 7 (1 Activities)

Discover Target: P2RX7

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

NLK Tchem Serine/threonine-protein kinase NLK (2 Activities)

Discover Target: NLK

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAPK11 Tchem Mitogen-activated protein kinase 11 (2 Activities)

Discover Target: MAPK11

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAPK14 Tchem Mitogen-activated protein kinase 14 (18 Activities)

Discover Target: MAPK14

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

화학 및 물리적 특성

• 굴절률: 1.71
• 끓는점(°C): 615.6° C
• 녹는점(°C): 280.73°C