Purinostat
Based on 1 Customer Validation
Purinostat is a selective inhibitor of HDAC I/IIb with anti-leukemic activity. Purinostat mesylate (HY-150109), the mesylate salt of Purinostat, inhibits the survival of Ph+ leukemic cells and CD34+ leukemic cells derived from CML patients. Purinostat mesylate targets HDAC I/IIb to inhibit several important factors for leukemic stem cell (LSC) survival, including c-Myc, β-Catenin, E2f, Ezh2, Alox5, and mTOR. Purinostat mesylate increases glutamate metabolism in LSC by increasing GLS1.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 98.04%
- CAS No.: 1929583-17-4
- 화학식: C23H26N10O3
- 분자량:490.52
-
보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
|
HDAC1 |
HDAC2 |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | EC50 |
112.96 nM
Compound: 10o
|
Inhibition of HDAC1/2/3 in human A2780S cells assessed as histone H3 acetylation incubated for 6 hrs by cytoblot assay
Inhibition of HDAC1/2/3 in human A2780S cells assessed as histone H3 acetylation incubated for 6 hrs by cytoblot assay
|
[PMID: 27186676] |
| A2780 | EC50 |
211.05 nM
Compound: 10o
|
Inhibition of HDAC6 in human A2780S cells assessed as tubulin acetylation incubated for 6 hrs by cytoblot assay
Inhibition of HDAC6 in human A2780S cells assessed as tubulin acetylation incubated for 6 hrs by cytoblot assay
|
[PMID: 27186676] |
| A2780 | IC50 |
6.98 nM
Compound: 10o
|
Cytotoxicity against human A2780S cells assessed as growth inhibition after 24 hrs by MTT assay
Cytotoxicity against human A2780S cells assessed as growth inhibition after 24 hrs by MTT assay
|
[PMID: 27186676] |
| HCT-116 | IC50 |
0.74 nM
Compound: 10o
|
Cytotoxicity against human HCT116 cells assessed as growth inhibition after 24 hrs by MTT assay
Cytotoxicity against human HCT116 cells assessed as growth inhibition after 24 hrs by MTT assay
|
[PMID: 27186676] |
| HeLa | IC50 |
3.2 nM
Compound: 10o
|
Inhibition of HDAC in human HeLa cell nuclear extract using Ac-Leu-Gly-Lys (Ac)-AMC as substrate after 30 mins by fluorescence assay
Inhibition of HDAC in human HeLa cell nuclear extract using Ac-Leu-Gly-Lys (Ac)-AMC as substrate after 30 mins by fluorescence assay
|
[PMID: 27186676] |
| MM1.S | IC50 |
0.78 nM
Compound: 10o
|
Cytotoxicity against human MM1S cells assessed as growth inhibition after 24 hrs by MTT assay
Cytotoxicity against human MM1S cells assessed as growth inhibition after 24 hrs by MTT assay
|
[PMID: 27186676] |
| MV4-11 | IC50 |
0.15 nM
Compound: 10o
|
Cytotoxicity against human MV4-11 cells assessed as growth inhibition after 24 hrs by MTT assay
Cytotoxicity against human MV4-11 cells assessed as growth inhibition after 24 hrs by MTT assay
|
[PMID: 27186676] |
| OCI-Ly1 | IC50 |
0.78 nM
Compound: 10o
|
Cytotoxicity against human OCI-LY1 cells assessed as growth inhibition after 24 hrs by MTT assay
Cytotoxicity against human OCI-LY1 cells assessed as growth inhibition after 24 hrs by MTT assay
|
[PMID: 27186676] |
| Raji | IC50 |
0.78 nM
Compound: 10o
|
Cytotoxicity against human Raji cells assessed as growth inhibition after 24 hrs by MTT assay
Cytotoxicity against human Raji cells assessed as growth inhibition after 24 hrs by MTT assay
|
[PMID: 27186676] |
| Ramos | IC50 |
0.78 nM
Compound: 10o
|
Cytotoxicity against human Ramos cells assessed as growth inhibition after 24 hrs by MTT assay
Cytotoxicity against human Ramos cells assessed as growth inhibition after 24 hrs by MTT assay
|
[PMID: 27186676] |
| RPMI-8226 | IC50 |
0.78 nM
Compound: 10o
|
Cytotoxicity against human RPMI8226 cells assessed as growth inhibition after 24 hrs by MTT assay
Cytotoxicity against human RPMI8226 cells assessed as growth inhibition after 24 hrs by MTT assay
|
[PMID: 27186676] |
| Sf9 | IC50 |
>1000 nM
Compound: 10o
|
Inhibition of full length human recombinant HDAC11 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence
Inhibition of full length human recombinant HDAC11 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence
|
[PMID: 27186676] |
| Sf9 | IC50 |
>1000 nM
Compound: 10o
|
Inhibition of N-terminal GST-tagged human recombinant HDAC7 (518 to end residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measu
Inhibition of N-terminal GST-tagged human recombinant HDAC7 (518 to end residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measu
|
[PMID: 27186676] |
| Sf9 | IC50 |
0.65 nM
Compound: 10o
|
Inhibition of full length C-terminal His/FLAG-tagged human recombinant HDAC1 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured a
Inhibition of full length C-terminal His/FLAG-tagged human recombinant HDAC1 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured a
|
[PMID: 27186676] |
| Sf9 | IC50 |
2.8 nM
Compound: 10o
|
Inhibition of human recombinant HDAC10 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay
Inhibition of human recombinant HDAC10 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay
|
[PMID: 27186676] |
| Sf9 | IC50 |
2.9 nM
Compound: 10o
|
Inhibition of full length human recombinant HDAC2 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence a
Inhibition of full length human recombinant HDAC2 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence a
|
[PMID: 27186676] |
| Sf9 | IC50 |
24 nM
Compound: 10o
|
Inhibition of full length C-terminal His-tagged human recombinant HDAC8 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after
Inhibition of full length C-terminal His-tagged human recombinant HDAC8 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after
|
[PMID: 27186676] |
| Sf9 | IC50 |
3.4 nM
Compound: 10o
|
Inhibition of full length C-terminal His-tagged human recombinant HDAC3/NCOR2 (395 to 489 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substr
Inhibition of full length C-terminal His-tagged human recombinant HDAC3/NCOR2 (395 to 489 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substr
|
[PMID: 27186676] |
| Sf9 | IC50 |
6.4 nM
Compound: 10o
|
Inhibition of full length human recombinant HDAC6 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence a
Inhibition of full length human recombinant HDAC6 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence a
|
[PMID: 27186676] |
| Sf9 | IC50 |
750 nM
Compound: 10o
|
Inhibition of human recombinant HDAC5 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay
Inhibition of human recombinant HDAC5 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay
|
[PMID: 27186676] |
| Sf9 | IC50 |
>1000 nM
Compound: 10o
|
Inhibition of C-terminal His-tagged human recombinant HDAC9 (604 to 1066 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition meas
Inhibition of C-terminal His-tagged human recombinant HDAC9 (604 to 1066 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition meas
|
[PMID: 27186676] |
| Sf9 | IC50 |
>1000 nM
Compound: 10o
|
Inhibition of N-terminal GST/C-terminal His-tagged human recombinant HDAC4 (627 to 1084 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrat
Inhibition of N-terminal GST/C-terminal His-tagged human recombinant HDAC4 (627 to 1084 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrat
|
[PMID: 27186676] |
| Sf9 | IC50 |
>10000 nM
Compound: 10o
|
Inhibition of N-terminal His6-tagged recombinant full-length human p110delta/untagged recombinant full length human p85alpha expressed in baculovirus infected insect Sf9 cells incubated for 2 hrs by kinase-glo assay
Inhibition of N-terminal His6-tagged recombinant full-length human p110delta/untagged recombinant full length human p85alpha expressed in baculovirus infected insect Sf9 cells incubated for 2 hrs by kinase-glo assay
|
[PMID: 27186676] |
| Sf9 | IC50 |
>10000 nM
Compound: 10o
|
Inhibition of recombinant human p110beta expressed in baculovirus infected insect Sf9 cells incubated for 1 hr by ADP-gloreagen assay
Inhibition of recombinant human p110beta expressed in baculovirus infected insect Sf9 cells incubated for 1 hr by ADP-gloreagen assay
|
[PMID: 27186676] |
| SUD4 | IC50 |
0.78 nM
Compound: 10o
|
Cytotoxicity against human SUDHL4 cells assessed as growth inhibition after 24 hrs by MTT assay
Cytotoxicity against human SUDHL4 cells assessed as growth inhibition after 24 hrs by MTT assay
|
[PMID: 27186676] |
| U-266 | IC50 |
0.78 nM
Compound: 10o
|
Cytotoxicity against human U266 cells assessed as growth inhibition after 24 hrs by MTT assay
Cytotoxicity against human U266 cells assessed as growth inhibition after 24 hrs by MTT assay
|
[PMID: 27186676] |
Chemical Information
-
CAS No. 1929583-17-4
-
Appearance Solid
-
분자량 490.52
-
화학식 C23H26N10O3
-
SMILES
O=C(C1=CN=C(N(CC2=NC3=C(N4CCOCC4)N=C(C5=CC=C(N)C=C5)N=C3N2C)C)N=C1)NO
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 125 mg/mL (254.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
-
Data Sheet (269 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0387 mL | 10.1933 mL | 20.3865 mL | 50.9663 mL |
| 5 mM | 0.4077 mL | 2.0387 mL | 4.0773 mL | 10.1933 mL | |
| 10 mM | 0.2039 mL | 1.0193 mL | 2.0387 mL | 5.0966 mL | |
| 15 mM | 0.1359 mL | 0.6796 mL | 1.3591 mL | 3.3978 mL | |
| 20 mM | 0.1019 mL | 0.5097 mL | 1.0193 mL | 2.5483 mL | |
| 25 mM | 0.0815 mL | 0.4077 mL | 0.8155 mL | 2.0387 mL | |
| 30 mM | 0.0680 mL | 0.3398 mL | 0.6796 mL | 1.6989 mL | |
| 40 mM | 0.0510 mL | 0.2548 mL | 0.5097 mL | 1.2742 mL | |
| 50 mM | 0.0408 mL | 0.2039 mL | 0.4077 mL | 1.0193 mL | |
| 60 mM | 0.0340 mL | 0.1699 mL | 0.3398 mL | 0.8494 mL | |
| 80 mM | 0.0255 mL | 0.1274 mL | 0.2548 mL | 0.6371 mL | |
| 100 mM | 0.0204 mL | 0.1019 mL | 0.2039 mL | 0.5097 mL |