AP-1 Inhibitors            
TS1989     c-JUN peptide          1mg
分子量:2743.55
分子式:C121H210N36O34S
Peptide comprising residues 33 - 57 of the JNK binding (δ) domain of human c-Jun. Disrupts JNK/c-Jun interaction leading to inhibition of serum-induced c-Jun phosphorylation, up-regulation of p21^cip/waf and modulation of inflammatory gene expression. Specifically induces apoptosis in HeLa tumor cells.
JNK/c-Jun interaction inhibitor
TS2476      SR 11302                 10mg
分子量:376.54
分子式:C26H32O2
Solubility:Soluble to 100 mM in DMSO and to 10 mM in ethanol
Purity:>98 %
CAS No:[160162-42-5]
Inhibitor of activator protein-1 (AP-1) transcription factor activity that displays antitumor effects in vivo. Does not activate transcription from the retinoic acid response element (RARE) and displays no activity at retinoic acid receptors (EC₅₀ > 1 μM for RARα, RARβ, RARγ and RXRα).
Inhibitor of AP-1 transcription factor; antitumor agent

Raf Kinase  Inhibitors   
TS1381     GW 5074             10mg ，50mg 
Chemical Name: 3-(3,5-Dibromo-4-hydroxy-benzylidene)-5-iodo-1,3-dihydro-indol-2-one
分子量: 520.94           分子式C15H8Br2INO2
Solubility:Soluble to 1 mM in ethanol and to 100 mM in DMSO
Purity:>98 %
CAS No:[220904-83-6]
Potent, selective and cell-permeable c-Raf1 kinase inhibitor (IC₅₀ = 9 nM). Displays ≥ 100-fold selectivity for raf kinase over CDK1, CDK2, c-src, ERK2, MEK, p38, Tie2, VEGFR2 and c-fm.

TS3185       L-779,450          10mg ，50mg 
Chemical Name: 2-Chloro-5-[2-Phenyl-5-(4-pyridinyl)-1H-imidazol-4-yl]phenol
分子量:347.8               分子式:C20H14ClN3O
Solubility:Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:>99 %        CAS No:[303727-31-3]
Potent, ATP-competitive Raf kinase inhibitor (IC₅₀ = 10 nM) that displays > 7, > 30 and > 70-fold selectivity over p38α, GSK3β and Lck respectively. Suppresses DNA synthesis and induces apoptosis in cells that proliferate in response to Raf-1 and A-Raf but not B-Raf.
TS1321     ZM 336372
Potent, selective c-Raf inhibito
MAPK
MAPKs (mitogen-activated protein kinases) are serine-threonine kinases that regulate a wide variety of cellular functions. Six groups of MAPK have so far been identified:
1. Extracellular signal-regulated kinases (ERK1, ERK2).   2. c-Jun N-terminal kinases (JNKs)   3. p38 isoforms (MAPK11, MAPK12, MAPK13, MAPK14)
4. ERK5 (MAPK7)   5. ERK3 (MAPK6) and ERK4 (MAPK4)   6. ERK7/8 (MAPK15)

p38 MAPK ：
TS2999      RWJ 67657
Potent, selective p38α and p38β inhibitor
TS1202     SB 203580
Selective inhibitor of p38 MAPK
抑制剂:
TS2186       CMPD-1
Non-ATP-competitive p38α inhibitor
TS2908     EO 1428
Selective inhibitor of p38α and p38β2
TS2657     JX 401
Potent, reversible p38α inhibitor
TS2999    RWJ 67657
Potent, selective p38α and p38β inhibitor
TS1264    SB 202190
Potent, selective inhibitor of p38 MAPK
TS1202    SB 203580
Selective inhibitor of p38 MAPK
TS1402     SB 203580 hydrochloride
Selective inhibitor of p38 MAPK; water-soluble
TS1962     SB 239063
Potent, selective p38 MAPK inhibitor; orally active
TS2938     SD 169
Selective, orally active p38α inhibitor
TS2008     SKF 86002 dihydrochloride
p38 MAPK inhibitor; anti-inflammatory agent
TS3639     SX 011
p38 MAPK inhibitor
TS3916     VX 702
Orally active p38α and p38β inhibitor

ERK        
TS3706       FR 180204
Selective ERK inhibitor

JNK/c-Jun
TS1496       SP 600125
Novel and selective JNK inhibitor
Inhibitors
TS2651     AEG 3482
Inhibitor of JNK signaling
TS3314     BI 78D3
Selective, competitive JNK inhibitor
TS1989     c-JUN peptide
Peptide inhibitor of JNK/c-Jun interaction
TS1565     JIP-1 (153-163)
JNK-selective inhibitor peptide
TS1496     SP 600125
Novel and selective JNK inhibitor
TS3607     SU 3327
Selective JNK inhibitor
TS2827     TCS JNK 5a
Selective inhibitor of JNK2 and JNK3 (pIC₅₀ values are 6.7, 6.5, <5.0 and <4.8 for JNK3, JNK2, JNK1 and p38α respectively). Displays no significant activity at a range of other protein kinases including EGFR, ErbB2, cdk2, PLK-1 and Src (pIC₅₀ < 5.0).
Purity: >99 %
 
MEK   抑制剂
TS1777     Arctigenin            10mg  , 50mg  
Alternative Name: (-)-Arctigenin
Chemical Name: (3R,4R)-4-[(3,4-Dimethoxyphenyl)methyl]dihydro-3-[(4-hydroxy-3-methoxyphenyl)methyl]-2(3H)-furanone
分子量:372.42          分子式:C21H24O6
Solubility:Soluble to 25 mM in ethanol and to 100 mM in DMSO
Purity:>99 %            CAS No:[7770-78-7]
Antioxidant, anti-inflammatory, antiproliferative and antiviral agent. Inhibits LPS-induced iNOS expression via inhibition of IκBα phosphorylation and p65 nuclear translocation (IC50 = 10 nM). Inhibits HIV-1 replication in vitro. Also potently inhibits MKK1 (IC50 = 0.5 nM) and provides neuroprotection by binding to kainate receptors.
Potent MKK1 inhibitor. Also inhibits IκBα phosphorylation

TS2605     PD 198306      10mg         Purity:>98 %
分子式：C18H16F3IN2O2    分子量：476.23
Solubility:Soluble to 100 mM in DMSO and to 100 mM in ethanol
CAS No:[212631-61-3]
Chemical Name: N-(Cyclopropylmethoxy)-3,4,5-trifluoro-2-[(4-iodo-2-methylphenyl)amino]-benzamide

Potent inhibitor of MEK1/2. Inhibits isolated enzyme at a concentration of 8 nM and inhibits MEK activity in synovial fibroblasts at concentrations of 30 - 100 nM. Highly selective for MEK; IC50 values are > 1, > 4, > 4 and > 10μM for ERK, c-Src, cdks and PI 3-kinaseγrespectively. Antihyperalgesic; blocks static allodynia in the streptozocin model of neuropathic pain following i.t. administration.

 MEK1GST, activeMitogen-activated kinase kinase 1, MAPKK1 human, recombinant, E. coli    PR-161    10 μg  
MKK6GST, activeMitogen-activated protein kinase kinase 6   human, recombinant, E. coli       PR-321    20 μg    

TS1213     PD 98059
Specific inhibitor of mitogen-activated protein kinase kinase (MAPKK / MEK). Acts by binding to the inactivated form of MEK, thereby preventing its phosphorylation by cRAF or MEK kinase (IC₅₀ = 2-7 μM). Inhibits cell growth and proliferation in acute myelogenous leukemia (AML) cell lines; causes G₁ arrest by blocking p53-dependent p21 induction. Also available as part of the MAPK Cascade Inhibitor Tocriset™ and MAPK Inhibitor Tocriset™.
Purity: >99 %

TS1969     SL 327       Purity:>99 %  
Chemical Name: α-[Amino[(4-aminophenyl)thio]methylene]-2-(trifluoromethyl)benzeneacetonitrile
分子式:C16H12F3O3S   分子量:335.35        CAS No:[305350-87-2]
Selective inhibitor of MEK1 and MEK2 (IC50 values are 0.18 and 0.22 μM respectively); blocks hippocampal LTP in vitro. Brain penetrant in vivo, blocking fear conditioning and learning in rats, and producing neuroprotection in mice, following systemic administration.

 

TS1868     U0124       10mg  

Chemical Name: Bis[amino(methylthio)methylene]butanedinitrile
Inactive analog of U0126 . Used as a negative control. Does not inhibit MEK at concentrations up to 100 μM.
Formula:C8H10N4S2     分子量:226.31  
CAS No:[108923-79-1]

TS1144     U0126         5mg ， 25mg
分子量:380.48      分子式:C18H16N6S2      CAS No:[109511-58-2] 
Chemical Name: 1,4-Diamino-2,3-dicyano-1,4-bis[2-aminophenylthio]butadiene
Solubility:Soluble to 100 mM in DMSO
Potent and selective non-competitive inhibitor of MAP kinase kinase. Inhibits MEK-1 and MEK-2 (IC50 values of 0.07 and 0.06 μM respectively) with little or no effect on the activities of PKC, Abl, Raf, MEKK, ERK, JNK, MKK-3, MKK-4/SEK, MKK-6, Cdk2 or Cdk4. Centrally active following systemic administration in vivo