Art. -Nr.: HY-150109A

Puzerinostat

Name: Puzerinostat
Brand: MedChemExpress
SKU: HY-150109A
Price: 560.00 USD
Availability: InStock
Rating: 5 (1 reviews)

(Synonyms: Purinostat)

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Puzerinostat (Purinostat) is a highly selective class I/IIb histone deacetylase (HDAC) inhibitor, with IC₅₀ values of 0.81 nM, 1.4 nM, 1.7 nM, 3.8 nM, 11.5 nM, and 1.1 nM against HDAC1, HDAC2, HDAC3, HDAC8, HDAC6, and HDAC10, respectively. Puzerinostat enhances glutamine metabolism by upregulating GLS1. Puzerinostat induces cell Apoptosis and downregulates the expression of BCR-ABL and c-MYC. Puzerinostat delays the progression of Ph⁺B-cell acute lymphoblastic leukemia and prolongs the survival of relevant mouse models. Puzerinostat regulates the immune microenvironment. Puzerinostat can be used in research related to chronic myeloid leukemia, Philadelphia chromosome-positive B-cell acute lymphoblastic leukemia, relapsed/refractory multiple myeloma, relapsed/refractory lymphoma, diffuse large B-cell lymphoma, and double-expression lymphoma.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 98.04%
CAS. Nr.: 1929583-17-4
Formel: C₂₃H₂₆N₁₀O₃
Molecular Weight:490.52

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Puzerinostat Chemical Structure

CAS. Nr.: 1929583-17-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[2]

HDAC1

0.81 nM (IC₅₀)

HDAC2

1.4 nM (IC₅₀)

HDAC3

1.7 nM (IC₅₀)

HDAC8

3.8 nM (IC₅₀)

HDAC6

11.5 nM (IC₅₀)

HDAC10

1.1 nM (IC₅₀)

Alle HDAC Isoform-spezifische Produkte anzeigen :

Alle Bcr-Abl Isoform-spezifische Produkte anzeigen :

Abl
Bcr-Abl

Cellular Effect

Cell Line	Type	Value	Description	References
MM.1S	IC50	<5 nM	Antiproliferative activity against human MM1S cells assessed as reduction in cell viability incubated for 72 hrs by cell viability antiproliferation assay. Antiproliferative activity against human MM1S cells assessed as reduction in cell viability incubated for 72 hrs by cell viability antiproliferation assay.	40562746
RPMI-8226	IC50	<5 nM	Antiproliferative activity against human RPMI-8226 cells assessed as reduction in cell viability incubated for 72 hrs by cell viability antiproliferation assay. Antiproliferative activity against human RPMI-8226 cells assessed as reduction in cell viability incubated for 72 hrs by cell viability antiproliferation assay.	40562746
AMO1	IC50	<5 nM	Antiproliferative activity against human AMO1 cells assessed as reduction in cell viability incubated for 72 hrs by cell viability antiproliferation assay. Antiproliferative activity against human AMO1 cells assessed as reduction in cell viability incubated for 72 hrs by cell viability antiproliferation assay.	40562746
OPM-2	IC50	<5 nM	Antiproliferative activity against human OPM2 cells assessed as reduction in cell viability incubated for 72 hrs by cell viability antiproliferation assay. Antiproliferative activity against human OPM2 cells assessed as reduction in cell viability incubated for 72 hrs by cell viability antiproliferation assay.	40562746
KMS-11	IC50	<5 nM	Antiproliferative activity against human KMS-11 cells assessed as reduction in cell viability incubated for 72 hrs by cell viability antiproliferation assay. Antiproliferative activity against human KMS-11 cells assessed as reduction in cell viability incubated for 72 hrs by cell viability antiproliferation assay.	40562746
RL	IC50	<5 nM	Antiproliferative activity against human RL cells assessed as reduction in cell viability incubated for 72 hrs by cell viability antiproliferation assay. Antiproliferative activity against human RL cells assessed as reduction in cell viability incubated for 72 hrs by cell viability antiproliferation assay.	40562746
Ramos	IC50	<5 nM	Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by cell viability antiproliferation assay. Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by cell viability antiproliferation assay.	40562746
Daudi	IC50	<5 nM	Antiproliferative activity against human Daudi cells assessed as reduction in cell viability incubated for 72 hrs by cell viability antiproliferation assay. Antiproliferative activity against human Daudi cells assessed as reduction in cell viability incubated for 72 hrs by cell viability antiproliferation assay.	40562746
Raji	IC50	<5 nM	Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 72 hrs by cell viability antiproliferation assay. Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 72 hrs by cell viability antiproliferation assay.	40562746
TMD8	IC50	<5 nM	Antiproliferative activity against human TMD-8 cells assessed as reduction in cell viability incubated for 72 hrs by cell viability antiproliferation assay. Antiproliferative activity against human TMD-8 cells assessed as reduction in cell viability incubated for 72 hrs by cell viability antiproliferation assay.	40562746
KARPAS-299	IC50	<5 nM	Antiproliferative activity against human Karpas299 cells assessed as reduction in cell viability incubated for 72 hrs by cell viability antiproliferation assay. Antiproliferative activity against human Karpas299 cells assessed as reduction in cell viability incubated for 72 hrs by cell viability antiproliferation assay.	40562746

In Vitro

Puzerinostat (20 nM; 0-48 h) induces time-dependent hyperacetylation of α-tubulin and histone H3 in LAMA84 Ph⁺ chronic myeloid leukemia cells^[1].
Puzerinostat is a highly selective class I/IIb HDAC inhibitor with favorable cardiac safety profiles due to its weak inhibitory effect on hERG channels^[3].
Puzerinostat (10-200 nM; 24-72 h) potently reduces the viability of LAMA84 and K562 Ph⁺ chronic myeloid leukemia cells, with an IC₅₀ of less than 10 nM, and its effect is dose- and time-dependent^[1].
Puzerinostat (72 h) potently inhibits the proliferation of multiple myeloma (MM) and lymphoma cell lines, with all IC₅₀ values below 5 nM^[3].
Treatment with Puzerinostat (5-150 nM; 24 h) induces dose-dependent G0/G1 cell cycle arrest in LAMA84 and K562 Ph⁺ chronic myeloid leukemia cells^[1].
Puzerinostat (0.25-0.5 nM; 24 h) upregulates the expression of MHC-I and MHC-II on MM1S cells in a concentration-dependent manner^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

LAMA84 Ph+ chronic myelogenous leukemia cells
Concentration:

20 nM
Incubation Time:

0 h, 12 h, 24 h, 36 h, 48 h
Result:

Increased acetylation of α-tubulin and histone H3 (Ac-α-tubulin and Ac-H3) in a time-dependent manner, with visible increases starting at 12 h and peaking at 48 h, relative to unacetylated α-tubulin, histone H3, and GAPDH loading controls.\nIncreased levels of pro-apoptotic proteins P53 and BAD, decreased anti-apoptotic protein BCL-XL, and induced cleavage of caspase-8, caspase-9, caspase-3, and PARP in a time-dependent manner.
Suppressed phosphorylation of RAF, MEK, ERK, and AKT (the RAF-MEK-ERK-AKT signaling axis) in a time-dependent manner.
Reduced protein levels of BCR-ABL, c-MYC, ALOX5, EZH2, p-STAT5, and p-FAK, while increasing levels of ALOX15 and β-CATENIN, all in a time-dependent manner.

Cell Viability Assay^[1]

Cell Line:

Luciferase-tagged LAMA84 and K562 Ph+ chronic myelogenous leukemia cells
Concentration:

10-100 nM (LAMA84); 150-200 nM (K562)
Incubation Time:

24 h, 36 h, 48 h, 60 h, 72 h
Result:

Reduced cell viability in a dose- and time-dependent manner for both cell lines.
Caused near-complete viability loss in LAMA84 cells at 100 nM by 48 h, and near-complete viability loss in K562 cells at 200 nM by 48 h.
Achieved an IC₅₀ of less than 10 nM against Ph+ cell lines.

Cell Cycle Analysis^[1]

Cell Line:

LAMA84 and K562 Ph+ chronic myelogenous leukemia cells
Concentration:

5-20 nM (LAMA84); 20-150 nM (K562)
Incubation Time:

24 h
Result:

Arrested LAMA84 and K562 cells in the G0/G1 phase in a dose-dependent manner.
Increased G0/G1 phase proportion in LAMA84 cells from 47.3% (control) to 84.0% at 20 nM; increased G0/G1 phase proportion in K562 cells from 31.5% (control) to 90.3% at 150 nM, with corresponding decreases in S and G2/M phases.

In Vivo

Purinostat (Purinostat mesylate formulation; 5-10 mg/kg; intravenous injection; three times per week) significantly prolongs the survival of mice with chronic myeloid leukemia (CML) induced by BCR-ABL^T315I, reduces leukemia cell burden, decreases the number of leukemia stem cells (LSCs) and impairs their viability, but monotherapy fails to completely eliminate LSCs^[1].
Puzerinostat (5-10 mg/kg; i.p., i.v.; three times per week; for 5 consecutive weeks) significantly prolongs survival and eliminates leukemia cells in BL-2 secondary transplanted Ph⁺ B-ALL mouse models, with 60% of mice surviving up to day 100 at the dose of 10 mg/kg^[2].
Puzerinostat (2.5-10 mg/kg) significantly prolongs survival and reduces tumor burden in PDX models of Ph⁺ B-ALL relapsed after tyrosine kinase inhibitor treatment, with a median overall survival (OS) of 73 days in the 10 mg/kg dose group^[2].
Puzerinostat (10 mg/kg) significantly extends the median survival to 86 days, reduces serum calcium levels, ameliorates osteolytic lesions, and enhances innate and adaptive anti-tumor immune responses in the 5TMM mouse model^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

donor mice (treated with fluorouracil); recipient mice (γ-ray irradiated)^[1]
Dosage:

5 mg/kg; 10 mg/kg
Administration:

i.v.; three times a week
Result:

Maintained 71.4% survival (10/14 mice) at day 90 post-BMT for 5 mg/kg dose, and 87.5% survival (7/8 mice) at day 90 post-BMT for 10 mg/kg dose, compared to 0% survival in placebo group by day 40.
Reduced peripheral blood leukemia cell (GFP+Gr-1+) burden to 1.21% (5 mg/kg) and 0.62% (10 mg/kg) by day 40.
Reduced bone marrow GFP+LSC counts to ~200 (5 mg/kg) and ~100 (10 mg/kg), compared to ~700 in placebo group.
Increased GFP+LSC apoptosis to ~38% (5 mg/kg) and ~45% (10 mg/kg), compared to ~22% in placebo group.
Reduced residual bone marrow GFP+LSC percentages to 2.0% (5 mg/kg) and 1.0% (10 mg/kg) by day 90 post-BMT, down from ~7.2% at day 14.
Reduced myeloid leukemia cell infiltration in lungs and spleens, with tissue structure comparable to healthy mice after long-term treatment.
Reduced leukemia cells in peripheral blood again upon retreatment after relapse following treatment suspension.

Animal Model:

C57BL/6 (7-8-week female; secondary transplantation model via intravenous injection of 1×10⁶ BL-2 cells)^[2]
Dosage:

5 mg/kg; 10 mg/kg
Administration:

i.p.; three times a week; five weeks; i.v.; three times a week
Result:

Prolonged median overall survival to 25.5 days in the 5 mg/kg group.
Achieved 60% (6/10) survival rate to 100 days in the 10 mg/kg group.
Nearly eliminated GFP+B220+ cells in peripheral blood of surviving mice after five weeks of treatment, with no tumor cells detected one week after treatment cessation.
Completely eliminated GFP+B220+ cells in spleens of a separate cohort after two doses of 10 mg/kg, maintaining inhibition for 26 days.
Decreased spleen weights significantly, reaching levels identical to healthy mice by day 19.
Significantly reduced GFP+B220+ cell proportions in bone marrow.
Increased Ac-H3 and Ac-H4 levels and decreased BCR-ABL, HSP90, HCK, p-SRC, and c-MYC levels in bone marrow cells.
Restored normal organ morphology in mice after three weeks of treatment.

Chemical Information

CAS. Nr. 1929583-17-4
Appearance Solid
Molecular Weight 490.52
Formel 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
Synonyms

Purinostat
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0387 mL

10.1933 mL

20.3865 mL

5 mM

0.4077 mL

2.0387 mL

4.0773 mL

10 mM

0.2039 mL

1.0193 mL

2.0387 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Qiu Q, et al. HDAC I/IIb selective inhibitor Purinostat Mesylate combined with GLS1 inhibition effectively eliminates CML stem cells. Bioactive materials. 2023 Mar;21:483-498. [Content Brief]

[2]. Yang L, et al. Purinostat Mesylate Is a Uniquely Potent and Selective Inhibitor of HDACs for the Treatment of -Induced B-Cell Acute Lymphoblastic Leukemia. Clinical cancer research : an official journal of the American Association for Cancer Research. 2019 Dec 15;25(24):7527-7539. [Content Brief]

[3]. Yang L, et al. Preclinical and first-in-human of purinostat mesylate, a novel selective HDAC I/IIb inhibitor, in relapsed/refractory multiple myeloma and lymphoma. Signal transduction and targeted therapy. 2025 Jun 23;10(1):201.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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Puzerinostat

Alle HDAC Isoform-spezifische Produkte anzeigen

Alle Bcr-Abl Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Puzerinostat Related Classifications

HY-150109A Related Classifications

Bioz