TMP269


CAS No. : 1314890-29-3

TMP269,1314890-29-3
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I001210
Synonyms:(Z)-N-((4-(4-phenylthiazol-2-yl)tetrahydro-2H-pyran-4-yl)methyl)-3-(5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl)benzimidic acid
Molecular Formula:C25H21F3N4O3S
Molecular Weight:514.52
Target:HDAC
IC50:126/80/36/9 nM for HDAC 4/5/7/9
Price:Get quote
Tags:HDAC |HDAC |HDAC |
We would like to match the lowest price on market if possible.

Your information is safe with us.

Appearance:white to off-white solid powder
Purity:98%
Cat No:I001210
Cas No:1314890-29-3
Product-Name:TMP269
InChI:InChI=1S/C25H21F3N4O3S/c26-25(27,28)22-31-20(32-35-22)17-7-4-8-18(13-17)21(33)29-15-24(9-11-34-12-10-24)23-30-19(14-36-23)16-5-2-1-3-6-16/h1-8,13-14H,9-12,15H2,(H,29,33)
InChIKey:HORXBWNTEDOVKN-UHFFFAOYSA-N
SMILES:O=C(NCC1(C2=NC(C3=CC=CC=C3)=CS2)CCOCC1)C4=CC=CC(C5=NOC(C(F)(F)F)=N5)=C4

TMP269(cas 1314890-29-3) is a novel and selective class IIa histone deacetylase inhibitor with IC50s of 126/80/36/9 nM for HDAC 4/5/7/9, respectively; 20-400 fold selectivity over class1 HDACs.


[1]. Lobera M, et al. Selective class IIa histone deacetylase inhibition via a nonchelating zinc-binding group. Nat Chem Biol. 2013 May;9(5):319-25. Abstract In contrast to studies on class I histone deacetylase (HDAC) inhibitors, the elucidation of the molecular mechanisms and therapeutic potential of class IIa HDACs (HDAC4, HDAC5, HDAC7 and HDAC9) is impaired by the lack of potent and selective chemical probes. Here we report the discovery of inhibitors that fill this void with an unprecedented metal-binding group, trifluoromethyloxadiazole (TFMO), which circumvents the selectivity and pharmacologic liabilities of hydroxamates. We confirm direct metal binding of the TFMO through crystallographic approaches and use chemoproteomics to demonstrate the superior selectivity of the TFMO series relative to a hydroxamate-substituted analog. We further apply these tool compounds to reveal gene regulation dependent on the catalytic active site of class IIa HDACs. The discovery of these inhibitors challenges the design process for targeting metalloenzymes through a chelating metal-binding group and suggests therapeutic potential for class IIa HDAC enzyme blockers distinct in mechanism and application compared to current HDAC inhibitors.

Chem Calculators

Related Products
  • CAS No. :128517-07-7
    Product Name:

    FK228

    Cat No: A000730 View details
  • CAS No. :414864-00-9
    Product Name:

    PXD101

    Cat No: A000593 View details
  • CAS No. :541-15-1
    Product Name:

    Levocarnitine

    Cat No: A000581 View details
  • CAS No. :149647-78-9
    Product Name:

    SAHA

    Cat No: A000479 View details
  • CAS No. :956154-63-5
    Product Name:

    TCS HDAC6 20b

    Cat No: R061716 View details
  • CAS No. :1012054-59-9
    Product Name:

    CUDC-101

    Cat No: I000119 View details
  • CAS No. :1316214-52-4
    Product Name:

    ACY-1215

    Cat No: I001219 View details
  • CAS No. :1375465-91-0
    Product Name:

    ACY-738

    Cat No: I001450 View details
  • CAS No. :1622921-15-6
    Product Name:

    Remodelin hydrobromide

    Cat No: I002086 View details
  • CAS No. :209783-80-2
    Product Name:

    MS-275 (Entinostat, SNDX-275)

    Cat No: I002611 View details
  • CAS No. :254964-60-8
    Product Name:

    Tasquinimod

    Cat No: I002871 View details
Recommend Products
  • CAS No. :123354-96-1
    Product Name:

    VAMP regimen

    Cat No: M030471 View details
  • CAS No. :1406-76-4
    Product Name:

    fluoromycin

    Cat No: M047180 View details
  • CAS No. :11017-43-9
    Product Name:

    siomycin

    Cat No: M052130 View details
  • CAS No. :154524-53-5
    Product Name:

    camelliatannin G

    Cat No: M102854 View details
  • CAS No. :130030-59-0
    Product Name:

    rivicycline

    Cat No: M105824 View details
  • CAS No. :1393-48-2
    Product Name:

    Thiostrepton

    Cat No: P000344 View details
  • CAS No. :946075-13-4
    Product Name:

    Isavuconazonium sulfate

    Cat No: I007373 View details
  • CAS No. :246252-06-2
    Product Name:

    Motexafin gadolinium

    Cat No: I007581 View details
  • CAS No. :1160959-55-6
    Product Name:

    LFF 571

    Cat No: I007659 View details
  • CAS No. :1217554-34-1
    Product Name:

    Suftalan Zine

    Cat No: I009626 View details
  • CAS No. :1314891-22-9
    Product Name:

    TMP-195

    Cat No: I009833 View details
  • CAS No. :1314891-22-9
    Product Name:

    TMP195

    Cat No: I013525 View details