BX-795

For research use only.

Catalog No.S1274

46 publications

BX-795 Chemical Structure

CAS No. 702675-74-9

BX-795 is a potent and specific PDK1 inhibitor with IC50 of 6 nM, 140- and 1600-fold more selective for PDK1 than PKA and PKC in cell-free assays, respectively. Meanwhile, in comparison to GSK3β more than 100-fold selectivity observed for PDK1. BX-795 modulates autophagy via inhibiting ULK1.

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Selleck's BX-795 has been cited by 46 publications

Purity & Quality Control

Choose Selective PDK Inhibitors

Biological Activity

Description BX-795 is a potent and specific PDK1 inhibitor with IC50 of 6 nM, 140- and 1600-fold more selective for PDK1 than PKA and PKC in cell-free assays, respectively. Meanwhile, in comparison to GSK3β more than 100-fold selectivity observed for PDK1. BX-795 modulates autophagy via inhibiting ULK1.
Targets
PDK-1 [1]
(Cell-free assay)
c-Kit [1]
(Cell-free assay)
CDK2/CyclinE [1]
(Cell-free assay)
Chk1 [1]
(Cell-free assay)
6 nM 320 nM 430 nM 510 nM
In vitro

BX-795 effectively blocks PDK1 activity in PC-3 cells, as shown by their ability to block phosphorylation of S6K1, Akt, PKCδ, and GSK3β. BX-795 potently inhibits tumor cell growth on plastic with IC50 of 1.6, 1.4, and 1.9 μM for MDA-468, HCT-116 and MiaPaca cells, respectively. In soft agar, BX-795 displays higher growth inhibition with IC50 of 0.72, and 0.25 μM for MDA-468, and PC-3 cells, respectively. [1] In addition, BX-795, as an inhibitor of the TBK1/IKKɛ, blocks TBK1- and IKKε-mediated activation of IRF3 and production of IFN-β. [2] In platelet physiological responses, BX795 produces inhibitory effect on 2-MeSADP-induced or collagen-induced aggregation, ATP secretion and thromboxane generation. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
THP1 MoDiSpVv[3Srb36gZZN{[Xl? NUD6XFZrOSCqch?= NYPGS2NmUW6qaXLpeIlwdiCxZjDjS2FUKGmwIHj1cYFvKFSKUEGgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKHOjbH3vckB{eGW{bTDkd2RPSS2rbnT1Z4VlKEmITj3i[ZRiKGW6cILld5Nqd25icILlbY5kfWKjdHXkJIZweiBzIHjyJIZwdGyxd3XkJIJ6KGS|RF7BJJN1cW23bHH0bY9vKG[xcjCxNkBpenNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCLQ{WwJF0hOC5yNjFOwG0v NEXyPVQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEmzOFI1Pid-Mki5N|QzPDZ:L3G+
KRX NEDOUJRHfW6ldHnvckBie3OjeR?= NF3jVHM4KG2rboO= M2XaeWlvcGmkaYTpc44hd2ZiU2XNU{11[WepZXSgWWxMOSBqdX7rco94diCxcnnnbY4qKGurbnHz[UBld22jaX6g[ZhxemW|c3XkJIlvKEuUWDDj[YxteyC3c3nu[{BcOzKSXT3nZY1u[S2DVGCgZY5lKG27ZXzpckBj[XOrYzDwdo91\WmwIIP1ZpN1emG2ZTDpcoN2[mG2ZXSg[o9zKDdibXnud{whUUN3MDC9JFAvODh5IN88UU4> M2DLVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4Mke1OlgyLz5{NkK3OVY5OTxxYU6=
KRX NFfHSJJHfW6ldHnvckBie3OjeR?= MV23JI1qdnN? Mmi3TY5pcWKrdHnvckBw\iCVVV3PMZRi\2enZDDVUGszKCi3bnvuc5dvKG:{aXfpckkhc2mwYYPlJIRwdWGrbjDlfJBz\XO|ZXSgbY4hU1K[IHPlcIx{KHW|aX7nJHs{OlCfLXfhcY1iNUGWUDDhcoQhdXmnbHnuJIJie2mlIIDyc5RmcW5ic4Xid5Rz[XSnIHnuZ5Vj[XSnZDDmc5IhPyCvaX7zMEBKSzVyIE2gNE4{OSEQvF2u MmfZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ{N{W2PFEoRjJ4Mke1OlgyRC:jPh?=
HeLa MULGeY5kfGmxbjDhd5NigQ>? NIDyd4U1KHWP MX2yOEBpenN? NWPE[mJNUW6qaXLpeIlwdiCxZjDheZRweGijZ4mgbY4hcHWvYX6gTIVN[SClZXzsd{Bie3Onc4Pl[EBieyCrbnT1Z5Rqd25ib3[gUGM{NUlicILveIVqdiCjY3P1cZVt[XSrb36gZZQhPCC3TTDpcoN2[mG2ZXSg[o9zKDJ2IHjyd{BjgSCrbX31co9jdG:2dHnu[{Bu\XSqb3S= MkfnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ{N{W2PFEoRjJ4Mke1OlgyRC:jPh?=
TC32 MmjNdWhVWyCjc4PhfS=> M16w[JFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCWQ{OyJINmdGy| MmG3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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BT-12 MlfGdWhVWyCjc4PhfS=> MnzNdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUGyJINmdGy| M4rT[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pTBK1 / TBK1 / pPLK1 / PLK1; 

PubMed: 26772203     


TBK1 mediated activation of the mitotic kinase PLK1. SW210.5 cells were treated with indicated TBK1 inhibitors for 1 hour and then exposed to 50 ng/mL of nocodazole for 18 hours. Western blot detected the signaling change using indicated antibodies, and β䲧疝Ỵ疞㧀疜膉痘 瘿⟸෕ᾰƌ෕Ð 㺣痖帉痖Ѐ

p-p38 / p38 / p-JNK / JNK / gD-2 ; 

PubMed: 28112176     


BX-795 inhibition on HSV replication attenuated by overexpression of p38/JNK. HeLa cells with or without JNK1 or p38 overexpression were infected with HSV-2 and total cellular protein was prepared for WB analysis. gD-2, the phosphorylation level of p38 MA䲧疝Ỵ疞㧀疜膉痘 瘿뙠ෆᾰƌෆĀ 㺣痖帉痖Ѐ瑖堘

26772203 28112176
Growth inhibition assay
Cell viability ; 

PubMed: 26772203     


Four SCLC cell lines with no MYC amplification were treated with TBK1 inhibitor BX-795 at the titration concentration. Cell viability was performed by CellTiter Glo 4 days after treatment. The growth curve was constructed by GraphPad Prism 6. 

26772203

Protocol

Kinase Assay:[1]
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Kinase assays:

PDK1 is assayed in a direct kinase assay and a coupled assay format measuring PDK1- and PtdIns-3,4-P2-mediated activation of AKT2. For the coupled assay, the final assay mixture (60 μL) contained: 15 mM MOPS, pH 7.2, 1 mg/mL bovine serum albumin, 18 mM β-glycerol phosphate, 0.7 mM dithiothreitol, 3 mM EGTA, 10 mM MgOAc, 7.5 μM ATP, 0.2 μCi of [γ-33P]ATP, 7.5 μM biotinylated peptide substrate (biotin-ARRRDGGGAQPFRPRAATF), 0.5 μL of PtdIns-3,4-P2-containing phospholipid vesicles, 60 pg of purified recombinant human PDK1, and 172 ng of purified recombinant human AKT2. After incubation for 2 h at room temperature, the biotin-labeled peptide is captured from 10 μl of the assay mixture on streptavidin-coated SPA beads, and product formation is measured by scintillation proximity in a Wallac MicroBeta counter. The product formed is proportional to the time of incubation and to the amount of PDK1 and inactive AKT2 added. PDK1 is added at suboptimal levels so that the assay could sensitively detect inhibitors of AKT2 activation as well as direct inhibitors of PDK1 or AKT2. To measure PDK1 activity directly, the final assay mixture (60 μL) contained 50 mM Tris-HCl, pH 7.5, 0.1 mM EGTA, 0.1 mM EDTA, 0.1% β-mercaptoethanol, 1 mg/mL bovine serum albumin, 10 mM MgOAc, 10 μM ATP, 0.2 μCi of [γ-33P]ATP, 7.5 μM substrate peptide (H2N-ARRRGVTTKTFCGT), and 60 ng of purified recombinant human PDK1. After 4 h at room temperature, we add 25 mM EDTA and spotted a portion of the reaction mixture on Whatman P81 phosphocellulose paper. The filter paper is washed three times with 0.75% phosphoric acid and once with acetone. After drying, the filter-bound labeled peptide is quantified using a Fuji phosphorimager.
Cell Research:[1]
- Collapse
  • Cell lines: MDA-468, PC-3, HCT-116 and MiaPaca cells
  • Concentrations: ~10 μM
  • Incubation Time: 72 hours
  • Method: Cells seeded at a low density (1,500–3,000 cells/well, 0.1 mL/well, 96-well plates) are incubated overnight. Compound treatments are made by adding 10 μL/well of the compound in 1% dimethyl sulfoxide and growth medium (final concentration of dimethyl sulfoxide, 0.1%), followed by brief shaking. Treated cells are incubated for 72 hours, and viability is measured by the addition of 10 μL of the metabolic dye WST-1. The WST-1 signal is read in a plate reader at 450 nm, and a no cell, or zero time cell, background is subtracted to calculate the net signal. Results are reported as the average ± S.E. of two or more replicates.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (169.07 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG +2% Tween 80+ddH2O
For best results, use promptly after mixing.
4mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 591.47
Formula

C23H26IN7O2S

CAS No. 702675-74-9
Storage powder
in solvent
Synonyms N/A
Smiles C1CCN(C1)C(=O)NC2=CC=CC(=C2)NC3=NC=C(C(=N3)NCCCNC(=O)C4=CC=CS4)I

In vivo Formulation Calculator (Clear solution)

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    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Frequently Asked Questions

  • Question 1:

    Can you suggest an in vivo formulation of S1274 for animal studies?

  • Answer:

    We recommend to use the vehicle 2% DMSO+30% PEG +2% Tween 80+ddH2O for in vivo study.

PDK Signaling Pathway Map

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