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
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.
Safety
- Hazard Codes
- Xn
- Risk Statements
- 22-36/37/38
- Safety Statements
- 26-36
- WGK Germany
- 3
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.
N-Bromosuccinimide Price
- Product number
- SML0788
- Product name
- A 83-01
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $93.5
- Updated
- 2024/03/01
- Product number
- SML0788
- Product name
- A 83-01
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $377
- Updated
- 2024/03/01
- Product number
- 9001799
- Product name
- A 83-01
- Purity
- ≥95%
- Packaging
- 1mg
- Price
- $29
- Updated
- 2024/03/01
- Product number
- 9001799
- Product name
- A 83-01
- Purity
- ≥95%
- Packaging
- 5mg
- Price
- $57
- Updated
- 2024/03/01
- Product number
- 616454
- Product name
- TGF-β RI Kinase Inhibitor IV - CAS 909910-43-6 - Calbiochem
- Packaging
- 2mg
- Price
- $216
- Updated
- 2024/03/01
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
A-83-01 Suppliers
- Tel
- +86-02787215551 +86-19945035818
- Fax
- 027-87215551
- 2936752263@qq.com
- Country
- China
- ProdList
- 8084
- Advantage
- 58
- Tel
- 13761310616
- Fax
- QQ: 39324283
- 39324283@qq.com
- Country
- China
- ProdList
- 1991
- Advantage
- 58
- Tel
- 010-82848833 400-666-7788
- Fax
- 86-10-82849933
- jkinfo@jkchemical.com
- Country
- China
- ProdList
- 96815
- Advantage
- 76
- Tel
- 821-50328103-801 18930552037
- Fax
- 86-21-50328109
- 3bsc@sina.com
- Country
- China
- ProdList
- 15839
- Advantage
- 69
- Tel
- +86-21-20908456
- Fax
- 021-58180499
- sales@BioChemBest.com
- Country
- China
- ProdList
- 6005
- Advantage
- 61
- Tel
- 021-58950125
- Fax
- (86) 21-58955996
- info@chemexpress.com
- Country
- China
- ProdList
- 7552
- Advantage
- 61
- Tel
- 0371-55932928 18937192232
- Fax
- 0086-0371-55932928
- 1282296214@qq.com
- Country
- China
- ProdList
- 491
- Advantage
- 55
- Tel
- 0531-85828981
- Fax
- +86-531-85806006
- 864598798@qq.com
- Country
- China
- ProdList
- 588
- Advantage
- 58
- Tel
- 18149758185 18149758185
- sales-cpd@caerulumpharma.com
- Country
- China
- ProdList
- 3466
- Advantage
- 58
- Tel
- 0755-0755-66853366 13670046396
- Fax
- 0755-28363542
- sales@chem-strong.com
- Country
- China
- ProdList
- 18070
- Advantage
- 56
- Tel
- 15221275939 15221275939
- Fax
- 021-50706099
- shenlinxing@macklin.cn
- Country
- China
- ProdList
- 16166
- Advantage
- 55
- Tel
- 021-61478794
- Fax
- 021-61478794
- sales@hcshhai.com
- Country
- China
- ProdList
- 9793
- Advantage
- 50
- Tel
- 025-58849295 18951903616;
- Fax
- 025-68650336
- info@adooq.cn
- Country
- China
- ProdList
- 2990
- Advantage
- 60
- Tel
- 021-61415566 800-8193336
- orderCN@merckgroup.com
- Country
- China
- ProdList
- 51456
- Advantage
- 80
- Tel
- 021-52996696,15000506266 15000506266
- Fax
- +86-21-52996696
- Country
- China
- ProdList
- 4575
- Advantage
- 55
- Tel
- Fax
- -
- eric_feng1954@126.com
- Country
- China
- ProdList
- 9248
- Advantage
- 55
- Tel
- +86-400-851-9921
- Fax
- +86-10-82826195
- sales@pharmacodia.com
- Country
- China
- ProdList
- 2317
- Advantage
- 55
- Tel
- 020-61288194 61288195
- Fax
- 020-61288700
- 505721671@qq.com
- Country
- China
- ProdList
- 3866
- Advantage
- 58
- Tel
- 02781293128
- orders@biochemsafebuy.com
- Country
- China
- ProdList
- 9923
- Advantage
- 55
- Tel
- 021-20242659 18930833303
- Fax
- +86 (21) 2024-2659
- Sales@changyanchem.cn
- Country
- China
- ProdList
- 5010
- Advantage
- 55
- Tel
- 86-21-50817262
- Fax
- 86-21-57712035
- sales@lancrix.com
- Country
- China
- ProdList
- 1502
- Advantage
- 55
- Tel
- 15076683720
- Fax
- 022-23754520
- klq@cw-bio.com
- Country
- China
- ProdList
- 5931
- Advantage
- 55
- Tel
- 177-54423994 17754423994
- Fax
- QQ:2853530913
- 2853530910@QQ.com
- Country
- China
- ProdList
- 8011
- Advantage
- 62
- Tel
- 21-31433387 15618786686
- Fax
- QQ:1369748377
- sales@rechemscience.com
- Country
- China
- ProdList
- 2986
- Advantage
- 58
- Tel
- 021-QQ:65489617 15618227136
- Fax
- 21-5161 9052
- Sales@ATKchemical.com
- Country
- China
- ProdList
- 7295
- Advantage
- 58
- Tel
- 021-2022843681 15618226720
- Fax
- +86-21-51601218
- lucy@atkchemical.com
- Country
- China
- ProdList
- 9952
- Advantage
- 58
- Tel
- 010-50973130 4009686088
- 3193328036@qq.com
- Country
- China
- ProdList
- 29785
- Advantage
- 68
- Tel
- 571-89925085
- Fax
- 0086-571-89925065
- sales@amadischem.com
- Country
- China
- ProdList
- 131957
- Advantage
- 58
- Tel
- 010-60605840 18892239720
- Fax
- 010-60605840
- psaitong@jm-bio.com
- Country
- China
- ProdList
- 12306
- Advantage
- 58
- Tel
- 0519-83246372 13585352506
- Fax
- 0519-83246372
- Country
- China
- ProdList
- 1844
- Advantage
- 58
- Tel
- 86-(0)29-85992781 17792393971
- info@lynnchem.com
- Country
- China
- ProdList
- 4587
- Advantage
- 58
- Tel
- +86-18017644823
- Fax
- - QQ:1910610264
- sales@betterbiochem.com
- Country
- China
- ProdList
- 325
- Advantage
- 58
- Tel
- 021-58111628 15800915896
- Fax
- QQ 3285589261
- sales@twochem.com
- Country
- China
- ProdList
- 1788
- Advantage
- 58
- Tel
- 17317130613
- Fax
- QQ3358272972
- 3358272972@qq.com
- Country
- China
- ProdList
- 3253
- Advantage
- 58
- Tel
- 010-010-010-62971590 18548936886
- Fax
- 010-62340519
- jack@oka-vip.com
- Country
- China
- ProdList
- 6897
- Advantage
- 58
- Tel
- +86-400-002-6226 +86-13028896684;
- sales@rrkchem.com
- Country
- China
- ProdList
- 57423
- Advantage
- 58
- Tel
- +86-0576-88813233 +86-13396860566
- sales@pharm-intermediates.com
- Country
- China
- ProdList
- 1991
- Advantage
- 58
- Tel
- 0371-0371-55055611 18137792234
- Fax
- QQ:3002694073
- 3002694073@qq.com
- Country
- China
- ProdList
- 10436
- Advantage
- 58
- Tel
- +1-2135480471 +1-2135480471
- sales@sarms4muscle.com
- Country
- China
- ProdList
- 10473
- Advantage
- 58
- Tel
- +86-0371-86658258 +8613203830695
- Fax
- 0371-86658258
- laboratory@coreychem.com
- Country
- China
- ProdList
- 30238
- Advantage
- 58
- Tel
- 021-58447131 13564518121
- sales@dcchemicals.com
- Country
- China
- ProdList
- 9409
- Advantage
- 58
- Tel
- 0519-85788828 13775037613
- sales@chemrenpharm.com
- Country
- China
- ProdList
- 3600
- Advantage
- 58
- Tel
- 63313187 15358055255
- Fax
- QQ:63313187
- 63313187@qq.com
- Country
- China
- ProdList
- 1987
- Advantage
- 58
- Tel
- 020-82000279 18988968278
- Fax
- QQ:3283937693
- sales@ubiochem.com
- Country
- China
- ProdList
- 4297
- Advantage
- 58
- Tel
- 021-38015121 15000105423
- wulan@absin.cn
- Country
- China
- ProdList
- 24731
- Advantage
- 58
- Tel
- 15231732623
- 1979763395@qq.com
- Country
- China
- ProdList
- 187
- Advantage
- 58
- Tel
- 650-6922368
- sales@achemblock.com
- Country
- China
- ProdList
- 2992
- Advantage
- 58
- Tel
- 15869524721
- 3525679403@qq.com
- Country
- China
- ProdList
- 4013
- Advantage
- 58
- Tel
- 17269768198
- Fax
- QQ:1213744847
- prochemx@163.com
- Country
- China
- ProdList
- 613
- Advantage
- 58
- Tel
- 15342225168
- yutianchun2007@126.com
- Country
- China
- ProdList
- 10003
- Advantage
- 58