ChemicalBook > CAS DataBase List > A-83-01

A-83-01

Product Name
A-83-01
CAS No.
909910-43-6
Chemical Name
A-83-01
Synonyms
CS-578;A 83-01, >=98%;A 83-01;A83-01;A-83-01AB142092);ALK5 Inhibitor IV;TGF inhibitor A-83-01;A 83-01 (DMSO solution;TGF-β RI Kinase Inhibitor IV;A83-01; A-83-01;A8301;A-8301;A 8301;A 83-01, ALK4, 5 and 7 kinase inhibitor
CBNumber
CB9972670
Molecular Formula
C25H19N5S
Formula Weight
421.52
MOL File
909910-43-6.mol
More
Less

A-83-01 Property

Melting point:
111℃
Boiling point:
590.0±60.0 °C(Predicted)
Density 
1.27±0.1 g/cm3(Predicted)
storage temp. 
-20°C
solubility 
DMSO: soluble5mg/mL, clear (warmed)
form 
powder
pka
8.77±0.70(Predicted)
color 
white to beige
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 2 months.
More
Less

Safety

Hazard Codes 
Xn
Risk Statements 
22-36/37/38
Safety Statements 
26-36
WGK Germany 
3
More
Less

Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P337+P313IF eye irritation persists: Get medical advice/attention.

More
Less

N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML0788
Product name
A 83-01
Purity
≥98% (HPLC)
Packaging
5mg
Price
$93.5
Updated
2024/03/01
Sigma-Aldrich
Product number
SML0788
Product name
A 83-01
Purity
≥98% (HPLC)
Packaging
25mg
Price
$377
Updated
2024/03/01
Cayman Chemical
Product number
9001799
Product name
A 83-01
Purity
≥95%
Packaging
1mg
Price
$29
Updated
2024/03/01
Cayman Chemical
Product number
9001799
Product name
A 83-01
Purity
≥95%
Packaging
5mg
Price
$57
Updated
2024/03/01
Sigma-Aldrich
Product number
616454
Product name
TGF-β RI Kinase Inhibitor IV - CAS 909910-43-6 - Calbiochem
Packaging
2mg
Price
$216
Updated
2024/03/01
More
Less

A-83-01 Chemical Properties,Usage,Production

Description

A 83-01 (909910-43-6) is a potent and selective ALK4, 5 and 7 inhibitor.1,2?IC50 = 45, 12 and 7.5 nM respectively. Prevents phosphorylation of Smad2/3 and growth inhibition induced by TGFβ.2?Inhibits differentiation of rat induced pluripotent stem cells and increases clonal expansion efficiency.3?Together with AMI-5, A83-01 enabled Oct4-induced reprogramming of mouse embryonic fibroblasts.4?Cell permeable. Active in vivo.

Uses

A 83-01 is a selective inhibitor of TGF-β type I receptor. A 83-01 treatment increases tumor permeability.

Uses

A 83-01 has been used as an inhibitor of transforming growth factor β kinase type 1 receptor.

Biological Activity

Selective inhibitor of TGF- β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7 (IC 50 values are 12, 45 and 7.5 nM respectively). Blocks phosphorylation of Smad2 and inhibits TGF- β -induced epithelial-to-mesenchymal transition. Only weakly inhibits ALK-1, -2, -3, -6 and MAPK activity. More potent than SB 431542 (4-[4-(1,3-benzodioxol-5-yl)-5-(2-pyridinyl)-1H-imidazol -2-yl]benzamide). Inhibits differentiation of rat induced pluripotent stem cells (riPSCs) and increases clonal expansion efficiency. Helps maintain homogeneity and long-term in vitro self-renewal of human iPSCs.

Biochem/physiol Actions

A 83-01 is a TGFβ kinase/activin receptor-like kinase (ALK 5) inhibitor (IC50=12 nM) that prevents phosphorylation of Smad2/3 and inhibits growth induced by TGFβ. A 83-01 blocks phosphorylation of Smad2 and inhibits TGF-β-induced epithelial-to-mesenchymal transition. Also, A 83-01 inhibits the transcriptional activity induced by TGFβ type I receptor ALK-5, activin type IB receptor ALK-4 and nodal type I receptor ALK-7. A-83-01 induces an expansion of neonatal Nkx2.5-eGFP (+) cells.

Enzyme inhibitor

This TGFb inhibitor (FW = 421.52 g/mol; CAS 909910-43-6; Solubility: 50 mM in DMSO), named 3-(6-methyl-2-pyridinyl)-N-phenyl-4-(4-quinolinyl)-1H-pyrazole-1-carbothioamide, selectively targets TGF-β type I receptor ALK5 kinase (IC50 = 12 nM), Type I Activin/Nodal receptor ALK4 (IC50 = 45 nM), and type I nodal receptor ALK7 (IC50 = 7.5 nM), blocking the phosphorylation of Smad2 and inhibiting TGF-β-induced epithelial-to-mesenchymal transitions. TGF-β signaling inhibitors represent a useful strategy for treating patients with tumor growth and metastasis in advanced cancer. A-83-01 only weakly inhibits ALK-1, ALK-2, ALK-3, ALK-6 and MAPK. It also has little or no effect on bone morphogenetic protein type I receptors, p38 mitogen-activated protein kinase, or extracellular regulated kinase. A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-β. Its use also instrumental in demonstrating that attachment to Laminin-111 facilitates TGF-β-induced expression of matrix metalloproteinase-2 in synovial fibroblasts.

storage

-20°C (protect from light)

References

1) Vogt. et al. (2011), The specificities of small molecule inhibitors of the TGFβ and BMP pathways; Cell Signal., 23 1831 2) Tojo et al. (2012), Characteristic differences among osteogenic cell populations of rat bone marrow stromal cells isolated from untreated, hemolyzed or Ficoll-treated marrow; Cancer Sci., 96 791 3) Li et al. (2009), Generation of rat and human induced pluripotent stem cells by combining genetic reprogramming and chemical inhibitors; Cell Stem Cell, 4 16 4) Yuan et al. (2011), Brief report: combined chemical treatment enables Oct4-induced reprogramming from mouse embryonic fibroblasts; Stem Cells, 29 549

A-83-01 Preparation Products And Raw materials

Raw materials

Preparation Products

More
Less

A-83-01 Suppliers

Wuhan Topule
Tel
+86-02787215551 +86-19945035818
Fax
027-87215551
Email
2936752263@qq.com
Country
China
ProdList
8084
Advantage
58
Dezhou LonWel Pharmaceutical Technology Co., Ltd.
Tel
13761310616
Fax
QQ: 39324283
Email
39324283@qq.com
Country
China
ProdList
1991
Advantage
58
J & K SCIENTIFIC LTD.
Tel
010-82848833 400-666-7788
Fax
86-10-82849933
Email
jkinfo@jkchemical.com
Country
China
ProdList
96815
Advantage
76
3B Pharmachem (Wuhan) International Co.,Ltd.
Tel
821-50328103-801 18930552037
Fax
86-21-50328109
Email
3bsc@sina.com
Country
China
ProdList
15839
Advantage
69
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6005
Advantage
61
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7552
Advantage
61
Zhengzhou HSH Science & Technology Co., Ltd.
Tel
0371-55932928 18937192232
Fax
0086-0371-55932928
Email
1282296214@qq.com
Country
China
ProdList
491
Advantage
55
Jinan Mingya Medical Technology Co., Ltd.
Tel
0531-85828981
Fax
+86-531-85806006
Email
864598798@qq.com
Country
China
ProdList
588
Advantage
58
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185 18149758185
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
3466
Advantage
58
ChemStrong Scientific Co.,Ltd
Tel
0755-0755-66853366 13670046396
Fax
0755-28363542
Email
sales@chem-strong.com
Country
China
ProdList
18070
Advantage
56
Shanghai Macklin Biochemical Co.,Ltd.
Tel
15221275939 15221275939
Fax
021-50706099
Email
shenlinxing@macklin.cn
Country
China
ProdList
16166
Advantage
55
Shanghai HuanChuan Industry Co.,Ltd.
Tel
021-61478794
Fax
021-61478794
Email
sales@hcshhai.com
Country
China
ProdList
9793
Advantage
50
AdooQ Bioscience CHINA
Tel
025-58849295 18951903616;
Fax
025-68650336
Email
info@adooq.cn
Country
China
ProdList
2990
Advantage
60
Sigma-Aldrich
Tel
021-61415566 800-8193336
Email
orderCN@merckgroup.com
Country
China
ProdList
51456
Advantage
80
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696,15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4575
Advantage
55
SPIRO PHARMA
Tel
Fax
-
Email
eric_feng1954@126.com
Country
China
ProdList
9248
Advantage
55
Pharmacodia (Beijing) Co.,Ltd
Tel
+86-400-851-9921
Fax
+86-10-82826195
Email
sales@pharmacodia.com
Country
China
ProdList
2317
Advantage
55
Guangzhou QiYun Biotechnology Co., Ltd.
Tel
020-61288194 61288195
Fax
020-61288700
Email
505721671@qq.com
Country
China
ProdList
3866
Advantage
58
Shanghai QianYan Bio-technology Co., Ltd
Tel
02781293128
Email
orders@biochemsafebuy.com
Country
China
ProdList
9923
Advantage
55
Shanghai Changyan Chem & Tech Co., Ltd.
Tel
021-20242659 18930833303
Fax
+86 (21) 2024-2659
Email
Sales@changyanchem.cn
Country
China
ProdList
5010
Advantage
55
Lancrix Chemicals
Tel
86-21-50817262
Fax
86-21-57712035
Email
sales@lancrix.com
Country
China
ProdList
1502
Advantage
55
Tianjin Kailiqi Biotechnology Co., Ltd.
Tel
15076683720
Fax
022-23754520
Email
klq@cw-bio.com
Country
China
ProdList
5931
Advantage
55
ShangHai Biochempartner Co.,Ltd
Tel
177-54423994 17754423994
Fax
QQ:2853530913
Email
2853530910@QQ.com
Country
China
ProdList
8011
Advantage
62
Shanghai Rechem science Co., Ltd.
Tel
21-31433387 15618786686
Fax
QQ:1369748377
Email
sales@rechemscience.com
Country
China
ProdList
2986
Advantage
58
Shanghai Chaolan Chemical Technology Center
Tel
021-QQ:65489617 15618227136
Fax
21-5161 9052
Email
Sales@ATKchemical.com
Country
China
ProdList
7295
Advantage
58
Shanghai SuperLan Chemcial Technique Centre
Tel
021-2022843681 15618226720
Fax
+86-21-51601218
Email
lucy@atkchemical.com
Country
China
ProdList
9952
Advantage
58
Beijing Solarbio Science & Tecnology Co., Ltd.
Tel
010-50973130 4009686088
Email
3193328036@qq.com
Country
China
ProdList
29785
Advantage
68
Amadis Chemical Company Limited
Tel
571-89925085
Fax
0086-571-89925065
Email
sales@amadischem.com
Country
China
ProdList
131957
Advantage
58
Beijing Jin Ming Biotechnology Co., Ltd.
Tel
010-60605840 18892239720
Fax
010-60605840
Email
psaitong@jm-bio.com
Country
China
ProdList
12306
Advantage
58
Medi-tech Bioscientific Co., Ltd.
Tel
0519-83246372 13585352506
Fax
0519-83246372
Country
China
ProdList
1844
Advantage
58
Lynnchem
Tel
86-(0)29-85992781 17792393971
Email
info@lynnchem.com
Country
China
ProdList
4587
Advantage
58
Shanghai BetterBioChem Co., Ltd.
Tel
+86-18017644823
Fax
- QQ:1910610264
Email
sales@betterbiochem.com
Country
China
ProdList
325
Advantage
58
Twochem Co.Ltd.
Tel
021-58111628 15800915896
Fax
QQ 3285589261
Email
sales@twochem.com
Country
China
ProdList
1788
Advantage
58
Angel Pharmatech, Ltd.
Tel
17317130613
Fax
QQ3358272972
Email
3358272972@qq.com
Country
China
ProdList
3253
Advantage
58
Beijing OKA biological technology co., LTD
Tel
010-010-010-62971590 18548936886
Fax
010-62340519
Email
jack@oka-vip.com
Country
China
ProdList
6897
Advantage
58
Shenzhen Polymeri Biochemical Technology Co., Ltd.
Tel
+86-400-002-6226 +86-13028896684;
Email
sales@rrkchem.com
Country
China
ProdList
57423
Advantage
58
Taizhou Crene Biotechnology Co. Ltd.
Tel
+86-0576-88813233 +86-13396860566
Email
sales@pharm-intermediates.com
Country
China
ProdList
1991
Advantage
58
Henan Alpha Chemical Co., Ltd.
Tel
0371-0371-55055611 18137792234
Fax
QQ:3002694073
Email
3002694073@qq.com
Country
China
ProdList
10436
Advantage
58
Zhejiang J&C Biological Technology Co.,Limited
Tel
+1-2135480471 +1-2135480471
Email
sales@sarms4muscle.com
Country
China
ProdList
10473
Advantage
58
Career Henan Chemica Co
Tel
+86-0371-86658258 +8613203830695
Fax
0371-86658258
Email
laboratory@coreychem.com
Country
China
ProdList
30238
Advantage
58
DC Chemicals
Tel
021-58447131 13564518121
Email
sales@dcchemicals.com
Country
China
ProdList
9409
Advantage
58
Changzhou Chenhong Biotechnology Co., Ltd.
Tel
0519-85788828 13775037613
Email
sales@chemrenpharm.com
Country
China
ProdList
3600
Advantage
58
Wuxi Donghe Pharmaceutical Technology Co., Ltd.
Tel
63313187 15358055255
Fax
QQ:63313187
Email
63313187@qq.com
Country
China
ProdList
1987
Advantage
58
Guangzhou Younan Technology Co., Ltd
Tel
020-82000279 18988968278
Fax
QQ:3283937693
Email
sales@ubiochem.com
Country
China
ProdList
4297
Advantage
58
Absin Bioscience Inc.
Tel
021-38015121 15000105423
Email
wulan@absin.cn
Country
China
ProdList
24731
Advantage
58
Cangzhou Pintuo Biotechnology Co., Ltd.
Tel
15231732623
Email
1979763395@qq.com
Country
China
ProdList
187
Advantage
58
Advanced chemblocks inc
Tel
650-6922368
Email
sales@achemblock.com
Country
China
ProdList
2992
Advantage
58
ShangHai ChuanQian Chemcial Technique Centre
Tel
15869524721
Email
3525679403@qq.com
Country
China
ProdList
4013
Advantage
58
Shanghai Puluokai Medical Technology Co., LTD
Tel
17269768198
Fax
QQ:1213744847
Email
prochemx@163.com
Country
China
ProdList
613
Advantage
58
Chunchuang (Wuhan) Technology Co., Ltd
Tel
15342225168
Email
yutianchun2007@126.com
Country
China
ProdList
10003
Advantage
58

909910-43-6, A-83-01Related Search:


  • 3-(6-Methyl-2-pyridinyl)-N-phenyl-4-(4-quinolinyl)-1H-pyrazole-1-carbothioamide
  • A 83-01;A83-01
  • TGF inhibitor A-83-01
  • 3-(6-methylpyridin-2-yl)-N-phenyl-4-(quinolin-4-yl)-1H-pyrazole-1-carbothioamide
  • TGF-β RI Kinase Inhibitor IV
  • A-83-01AB142092)
  • ALK5 Inhibitor IV
  • A 83-01, >=98%
  • 1H-Pyrazole-1-carbothioamide,3-(6-methyl-2-pyridinyl)-N-phenyl-4-(4-quinolinyl)-
  • 3-(6-methylpyridin-2-yl)-N-phenyl-4-quinolin-4-ylpyrazole-1-carbothioamide
  • A83-01; A-83-01;A8301;A-8301;A 8301
  • TGF-β RI Kinase Inhibitor IV - CAS 909910-43-6 - Calbiochem
  • CS-578
  • A 83-01 (DMSO solution
  • 3-(6-Methyl-2-pyridyl)-N-phenyl-4-(4-quinolinyl)pyrazole-1-carbothioamide
  • A 83-01, ALK4, 5 and 7 kinase inhibitor
  • 909910-43-6
  • C25H19N5S
  • Inhibitors
  • TGF-beta/Smad
  • Protein Kinase