Degrasyn (WP1130)

Catalog No.S2243

For research use only.

Degrasyn (WP1130) is a selective deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and also suppresses Bcr/Abl, also a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT). Degrasyn (WP1130) induces apoptosis and blocks autophagy.

Degrasyn (WP1130) Chemical Structure

CAS No. 856243-80-6

Selleck's Degrasyn (WP1130) has been cited by 37 publications

Purity & Quality Control

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Biological Activity

Description Degrasyn (WP1130) is a selective deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and also suppresses Bcr/Abl, also a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT). Degrasyn (WP1130) induces apoptosis and blocks autophagy.
Features WP1130 has an advantage over imatinib mesylate in that its activity is not inhibited by a variety of Abl kinase mutations, including T315I.
Targets
DUB [1]
(Cell-free assay)
Bcr-Abl [1]
(Cell-free assay)
1.8 μM
In vitro

In addition to inducing rapid down-regulation of Bcr/Abl without affecting Bcr or c-Abl, WP1130 also regulates the stability of Jak2 and c-Myc without affecting other kinases (HER1, HER2, c-Kit, FAK, ERK1, ERK2, Akt, Btk, Src and Src-related kinases) or transcription factors (wild-type p53, STAT1, STAT3, STAT5, c-Jun, NF-κB, and Max). Unlike adaphostin and Trisenox, WP1130 induces down-regulation of Bcr/Abl within 60 minutes. WP1130 is more effective in inducing apoptosis of myeloid and lymphoid tumor cells with IC50 of ~0.5-2.5 μM compared with normal CD34+ hematopoietic precursors, dermal fibroblasts, or endothelial cells with IC50 of ~5-10 μM. WP1130 (5 μM) specifically and rapidly down-regulates both wild-type and T315I mutant Bcr/Abl protein without affecting bcr/abl gene expression or engaging the proteasomal degradation pathway in chronic myelogenous leukemia (CML) cells, accompanied by induction of apoptosis. WP1130 is more effective in reducing leukemic cell colony formation compared with normal progenitor cells, and effective against primary leukemic cells harboring the T315I mutation. [1] WP1130 induces rapid proteasomal-dependent degradation of c-Myc protein in MM-1 multiple myeloma and other tumor cell lines, correlated with tumor growth inhibition. [2] Unlike AG490, WP1130 acts as a partly selective deubiquitinase (DUB) inhibitor to induce a rapid and marked accumulation of polyubiquitinated (K48/K63-linked) proteins into juxtanuclear aggresomes without affecting proteasome activity. WP1130 (5 μM) directly inhibits DUB activity of USP9x, USP5, USP14, UCH-L1, and UCH37, but not UCH-L3, resulting in downregulation of antiapoptotic and upregulation of proapoptotic proteins, such as MCL-1 and p53. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Mino NVnaZZduS3m2b4TvfIlkcXS7IHHzd4F6 NF7heZA4OiCqcoO= NV3yfnVFS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVWmwbzDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvQM7:TR?= NGnrNlU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NES1O|A6OSd-MkS0OVcxQTF:L3G+
MM1 NYiyc48zSW62aYT1cY9zKGG|c3H5 M3rX[VI1KHSxIEeyJIhzew>? M4G1OGFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3NNUBk\WyuczDh[pRmeiB{NDD0c{A4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVHPxE1? M3ztU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MEO2NlE{Lz5{MkCzOlIyOzxxYU6=
MM1S NXT5W241S3m2b4TvfIlkcXS7IHHzd4F6 NHrYS5Y4OiCqcoO= M2jjOmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1OOVNiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2xMlLPxE1? Mlz3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2NUewPVEoRjJ2NEW3NFkyRC:jPh?=
U266 MlXtRY51cXS3bX;yJIF{e2G7 NHfzWHozPCC2bzC3NkBpenN? MmruRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVUK2OkBk\WyuczDh[pRmeiB{NDD0c{A4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVEvO87:TR?= MkjwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJyM{[yNVMoRjJ{MEO2NlE{RC:jPh?=
OCI-My4 NVPSZnBySW62aYT1cY9zKGG|c3H5 MXqyOEB1dyB5MjDodpM> NWHQO3ZHSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gU2NKNU27NDDj[YxteyCjZoTldkAzPCC2bzC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUGuOe69VQ>? MlH5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJyM{[yNVMoRjJ{MEO2NlE{RC:jPh?=
A375 MnzrR5l1d3SxeHnjbZR6KGG|c3H5 M{fsO|czKGi{cx?= NGDueohEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCOzd3IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9NU44|ryP Mn61QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2NUewPVEoRjJ2NEW3NFkyRC:jPh?=
K562 MVrDfZRwfG:6aXPpeJkh[XO|YYm= M{THTVczKGi{cx?= MXjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;Mj60{txO NVfw[2IzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0OVcxQTFpPkK0OFU4ODlzPD;hQi=>
Z138 NGHNUndHfW6ldHnvckBie3OjeR?= M33hbFEhcHJ? NGrrc49KdmirYnn0bY9vKG:oIGXDTE1NOSCrbjDoeY1idiCcMUO4JINmdGy|IHHmeIVzKDFiaIKgZpkhcW2vdX7vZoxwfHSrbnegZY5idHm|aYOsJGlEPTB;M988US=> NXiwOolMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3PVExPzZpPkKzO|kyODd4PD;hQi=>
Z138 MXXGeY5kfGmxbjDhd5NigQ>? NFjXZWUyKGi{ M3Xu[mlvcGmkaYTpc44hd2ZiVWPQPZghcW5iaIXtZY4hYjF|ODDj[YxteyCjZoTldkAyKGi{IHL5JIludXWwb3Lsc5R1cW6pIHHuZYx6e2m|LDDJR|UxRTQQvF2= MmDxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUGwO|YoRjJ|N{mxNFc3RC:jPh?=
Z138 NWrZNoFmTnWwY4Tpc44h[XO|YYm= MmfINUBpeg>? M1uyWmlvcGmkaYTpc44hd2ZiVWPQOUBqdiCqdX3hckBbOTN6IHPlcIx{KGGodHXyJFEhcHJiYomgbY1ufW6xYnzveJRqdmdiYX7hcJl{cXNuIFnDOVA:O87:TR?= NVvQ[4ZNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3PVExPzZpPkKzO|kyODd4PD;hQi=>
Z138 M4TaUGZ2dmO2aX;uJIF{e2G7 MVSxMlI2KHSxIEWgeW0> M{LUSlQhcHK| M{frNWlvcGmkaYTpc44hd2ZiVYPwPZghcW5iaIXtZY4hYjF|ODDj[YxteyC3c3nu[{BJSS2XYjD2bY56dC2|dXzmc45mKGG|IIP1ZpN1emG2ZTDheEAyNjJ3IITvJFUhfU1iYX\0[ZIhPCCqcoOgZpkhcW2vdX7vZoxwfHSrbnegZY5idHm|aYO= MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR3N{C5NUc,OjR2NUewPVE9N2F-
Z138 Ml3hSpVv[3Srb36gZZN{[Xl? M33xdVEvOjVidH:gOUB2VQ>? M1e4OVQhcHK| MYnJcohq[mm2aX;uJI9nKFW|cEn4JIlvKGi3bXHuJHoyOzhiY3XscJMh[XRiMT6yOUB1dyB3IIXNJIlv[3WkYYTl[EBnd3JiNDDodpMh[nliU1TTMXBCT0ViYX7kJIludXWwb3Lsc5R1cW6p NVPKcm97RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTl{M{KzN{8oRkOqRV3CUFww[T5?
Z138 M2fpbmZ2dmO2aX;uJIF{e2G7 MkHnNU4zPSC2bzC1JJVO NYTreII2PCCqcoO= MoLhTY5pcWKrdHnvckBw\iCXc4C5fEBqdiCqdX3hckBbOTN6IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBO[2xvMTDwdo91\WmwIHzleoVtKGG2IEGuNlUhfG9iNTD1UUBqdmO3YnH0[YQh\m:{IESgbJJ{KGK7IGPEV{1RSUeHIHHu[EBqdW23bn;icI91fGmwZx?= NUT1SYk1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTl{M{KzN{8oRkOqRV3CUFww[T5?
Z138 NYfOOXVuTnWwY4Tpc44h[XO|YYm= MY[xMlI2KHSxIEWgeW0> NXXmXo5lPCCqcoO= MVLJcohq[mm2aX;uJI9nKFW|cEn4JIlvKGi3bXHuJHoyOzhiY3XscJMh[XRiMT6yOUB1dyB3IIXNJIlv[3WkYYTl[EBnd3JiNDDodpMh[nliaX3teY5w[myxdITpcoch[W6jbInzbZM> NYLNeo9IRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTl{M{KzN{8oRkOqRV3CUFww[T5?
Z138 M4f1cGZ2dmO2aX;uJIF{e2G7 Mk\pNU4zPSC2bzC1JJVO M4\W[lQhcHK| MknnTY5pcWKrdHnvckBw\iCXc4C5fEBqdiCqdX3hckBbOTN6IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBO[2xzIIDyc5RmcW5ibHX2[Yx{KGG2IEGuNlUhfG9iNTD1UUBqdmO3YnH0[YQh\m:{IESgbJJ{KGK7IHntcZVvd2Kub4T0bY5oKGGwYXz5d4l{ NET1[WQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTJ|MkOzM{c,S2iHTVLMQE9iRg>?
In vivo Administration of WP1130 inhibits the growth of K562 tumors as well as both wildtype Bcr/Abl and T315I mutant Bcr/Abl-expressing BaF/3 cells transplanted into nude mice. [1] Consistent with the down-regulation of c-Myc, WP1130 displays potent inhibitory activity against A375 melanoma tumors established in nude mice. [2]

Protocol (from reference)

Cell Research:[1]
  • Cell lines: BV173, BV173R, K562, and BaF/3
  • Concentrations: Dissolved in DMSO, final concentrations ~10 μM
  • Incubation Time: 72 hours
  • Method: Cells are treated with increasing concentrations of WP1130 (0.08-10 μM) in 96-well plates. Plates are incubated at 37 °C for 72 hours, after which 20 μL of MTT reagent is added, and the plates are incubated at 37 °C for another 2 hours. Cells are lysed with 100 μL lysis buffer (20% sodium dodecyl sulfate [SDS] in 50% N, N-dimethylformamide adjusted to pH 4.7 with 80% acetic acid and 1 M hydrochloric acid; final concentration of acetic acid is 2.5% and hydrochloric acid is 2.5%) and incubated for 6 hours. The optical density of each sample at 570 nm is determined with a SPECTRA MAX M2 plate reader.
Animal Research:[1]
  • Animal Models: Swiss Nu/Nu mice transplanted with K562 tumor cells, BaF/3wt cells, or BaF/3/T315I cells
  • Dosages: ~40 mg/kg every other day
  • Administration: Injected intraperitoneally

Solubility (25°C)

In vitro

DMSO 77 mg/mL
(200.37 mM)
Ethanol 18 mg/mL
(46.84 mM)
Water Insoluble

Chemical Information

Molecular Weight 384.27
Formula

C19H18BrN3O

CAS No. 856243-80-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCCC(C1=CC=CC=C1)NC(=O)C(=CC2=NC(=CC=C2)Br)C#N

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