G007-LK
- Product Name
- G007-LK
- CAS No.
- 1380672-07-0
- Chemical Name
- G007-LK
- Synonyms
- G007-LK;CS-1659;G007 LK;G007LK;G007-LK;G007 LK;G007LK;Tankyrase 1/2 Inhibitor VI, G007-LK - Calbiochem;G007LK,Inhibitor,poly ADP ribose polymerase,G-007-LK,G007 LK,PARP,inhibit,G007-LK;(E)-4-(5-(2-(4-(2-chlorophenyl)-5-(5-(methylsulfonyl)pyridin-2-yl)-4H-1,2,4-triazol-3-yl)vinyl)-1,3,4-oxadiazol-2-yl)benzonitrile;4-[5-[(1E)-2-[4-(2-Chlorophenyl)-5-[5-(methylsulfonyl)-2-pyridinyl]-4H-1,2,4-triazol-3-yl]ethenyl]-1,3,4-oxadiazol-2-yl]benzonitrile;Benzonitrile, 4-[5-[(1E)-2-[4-(2-chlorophenyl)-5-[5-(methylsulfonyl)-2-pyridinyl]-4H-1,2,4-triazol-3-yl]ethenyl]-1,3,4-oxadiazol-2-yl]-
- CBNumber
- CB32707548
- Molecular Formula
- C25H16ClN7O3S
- Formula Weight
- 529.96
- MOL File
- 1380672-07-0.mol
G007-LK Property
- Boiling point:
- 817.3±75.0 °C(Predicted)
- Density
- 1.47±0.1 g/cm3(Predicted)
- storage temp.
- +2C to +8C
- solubility
- ≥26.5 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
- form
- White powder
- pka
- -1.68±0.10(Predicted)
N-Bromosuccinimide Price
- Product number
- 5.04907
- Product name
- Tankyrase 1/2 Inhibitor VI, G007-LK - Calbiochem
- Purity
- Tankyrase 1/2 Inhibitor VI, G007-LK, CAS 1380672-07-0, is a cell-permeable, potent and highly selective inhibitor of tankyrase (IC50 = 33 & 26 nM for TNKS1 and TNKS2, respectively).
- Packaging
- 10MG
- Price
- $280
- Updated
- 2024/03/01
- Product number
- 22934
- Product name
- G007-LK
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 22934
- Product name
- G007-LK
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $139
- Updated
- 2024/03/01
- Product number
- 22934
- Product name
- G007-LK
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $243
- Updated
- 2024/03/01
- Product number
- 22934
- Product name
- G007-LK
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $533
- Updated
- 2024/03/01
G007-LK Chemical Properties,Usage,Production
General Description
A cell-permeable, triazolyl-vinyl-oxadiazole compound that targets adenosine site of the NAD+ pocket in the TNKS PARP domain and acts as a potent and highly selective tankyrase inhibitor (IC50 = 33 and 26 nM, respectively, against TNKS1/PARP5a/ARTD5 and TNKS2/PARP5b/ARTD6 in auto-PARsylation assays), effectively inhibiting murine Wnt3a-induced reporter activity in human HEK293 and murine 10T1/2 cultures (ICmax ~300 and 600 nM, respectively). Shown to display little or no inhibitory potency (IC50 >10 μM) toward 7 other PARP enzymes (PARP1, 2, 3, 6, 7,10,11), 90 kinases, 16 phosphatases, and 75 GPCRs (IC50 >10 μM). Shown to inhibit two CRC lines, COLO-320DM & SW403, colony formation in vitro (200 nM) and tumor expansion in mice in vivo (20 mg/kg via daily i.p.), although G007-LK toxicity is observed at higher dosages (≥30 mg/kg/12 h or 60 mg/kg/d via i.p.).
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Biological Activity
g007-lk is a potent and specific inhibitor of tankyrase 1/2 with ic50 values of 46 and 25 nm [1].the telomeric repeat factor 1 (trf1)-interacting ankyrin-related adp-ribose polymerase 1 (tankyrase 1,tnks1) and tankyrase 2 (tnks2) belong to the subgroup of poly(adp-ribosyl)ating polymerases and regulate the assembly and disassembly of large polymerized structures [1].g007-lk is a potent and specific tankyrase 1/2 inhibitor. g007-lk reduced auto-poly-(adp ribosy)lation of tnks1 and tnks2 with ic50 values of 46 nm and 25 nm, respectively. in wnt3a-induced hek 293 cells, g007-lk inhibited st-luc with ic50 value of 0.05 μm [1]. in sw480 colorectal cancer cell line transfected with gfp-tnks1, g007-lk induces highly dynamic and mobile degradasomes containing phosphorylated beta-catenin, beta-trcp and ubiquitin [2]. in the apc-mutant cell lines, g007-lk reduces cytosolic and nuclear β-catenin protein levels [3].in mice bearing colo-320dm cell xenografts, g007-lk (20 mg/kg twice daily or 40 mg/kg daily) concentration-dependently inhibited tumor growth by 61% and 48%, respectively. also, g007-lk reduced the levels of tnks1/2 and β-catenin, and stabilized axin1/2 [3].
Biochem/physiol Actions
Cell permeable: yes
References
[1]. voronkov a, holsworth dd, waaler j, et al. structural basis and sar for g007-lk, a lead stage 1,2,4-triazole based specific tankyrase 1/2 inhibitor. j med chem, 2013, 56(7): 3012-3023.
[2]. thorvaldsen te, pedersen nm, wenzel em, et al. structure, dynamics and functionality of tankyrase inhibitor-induced degradasomes. mol cancer res, 2015, pii: molcanres.0125.2015.
[3]. lau t, chan e, callow m, et al. a novel tankyrase small-molecule inhibitor suppresses apc mutation-driven colorectal tumor growth. cancer res, 2013, 73(10): 3132-3144.
G007-LK Preparation Products And Raw materials
Raw materials
Preparation Products
G007-LK Suppliers
- Tel
- +1-800-259-7612
- Fax
- +1-800-259-7612
- info@musechem.com
- Country
- United States
- ProdList
- 4662
- Advantage
- 60
- Tel
- +1-708-310-1919 +1-13798911105
- Fax
- 708-557-7486
- sales@invivochem.cn
- Country
- United States
- ProdList
- 6393
- Advantage
- 58
- Tel
- +1 (732)236-3202
- sales@cckinase.com
- Country
- United States
- ProdList
- 2738
- Advantage
- 58
- Tel
- +1-+1(833)-552-7181
- sales@aladdinsci.com
- Country
- United States
- ProdList
- 57511
- Advantage
- 58
- Tel
- +1-781-999-5354
- support@targetmol.com
- Country
- United States
- ProdList
- 19973
- Advantage
- 58
View Lastest Price from G007-LK manufacturers
- Product
- (E)-4-(5-(2-(4-(2-chlorophenyl)-5-(5-(methylsulfonyl)pyridin-2-yl)-4H-1,2,4-triazol-3-yl)vinyl)-1,3,4-oxadiazol-2-yl)benzonitrile 1380672-07-0
- Price
- US $1.00/KG
- Min. Order
- 1KG
- Purity
- Min98% HPLC
- Supply Ability
- g/kg/ton
- Release date
- 2020-01-01