Art. -Nr.: HY-151261

HDAC6-IN-13

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HDAC6-IN-13 (Compound 35m) is a potent, highly selective, orally active HDAC6 inhibitor with an IC₅₀ of 0.019 μM. HDAC6-IN-13 also inhibits HDAC1, HDAC2 and HDAC3 with IC₅₀s of 1.53, 2.06 and 1.03 μM, respectively. HDAC6-IN-13 shows significant BBB permeability and anti-inflammatory activity.

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Reinheit: 98.08%
CAS. Nr.: 2837128-41-1
Formel: C₂₃H₂₂N₄O
Molecular Weight:370.45

Speicherung:

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

HDAC6-IN-13 Chemical Structure

CAS. Nr.: 2837128-41-1

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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^[1]

HDAC6

0.019 μM (IC₅₀)

HDAC3

1.03 μM (IC₅₀)

HDAC1

1.53 μM (IC₅₀)

HDAC2

2.06 μM (IC₅₀)

Alle HDAC Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
J774.A1	IC₅₀	2.61 μM Compound: 35m	Antiinflammatory activity against LPS primed mouse J774.A1 cells assessed suppression of LPS/ATP induced IL-beta release preincubated for 30 mins followed by ATP stimulation measured after 30 mins by ELISA Antiinflammatory activity against LPS primed mouse J774.A1 cells assessed suppression of LPS/ATP induced IL-beta release preincubated for 30 mins followed by ATP stimulation measured after 30 mins by ELISA	[PMID: 36073117]

In Vitro

HDAC6-IN-13 (Compound 35m) (0.1-1 μM; 24 h) is highly selective toward HDAC6 versus class I HDACs^[1].
HDAC6-IN-13 is a slow-on and slow-off tight-binding HDAC6 inhibitor, while exhibits fast-on properties for HDAC1, 2, and 3^[1].
HDAC6-IN-13 (5-20 μM; 8 h) shows anti-inflammatory activity in vitro^[1].

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

Western Blot Analysis^[1]

Cell Line:

MV4−11 and J774A.1
Concentration:

0.1, 0.2, 0.5 and 1 μM
Incubation Time:

24 h
Result:

Concentration-related accumulation of acetylated tubulin (Ac-Tubulin) was observed, while upregulation of acetylated histone H3 (AcHH3) and acetylated histone H4 (AcHH4) was not apparent even at the concentration of 1 μM.

Western Blot Analysis^[1]

Cell Line:

J774A.1 cells
Concentration:

5, 10 and 20 μM
Incubation Time:

8 h
Result:

Inhibited the cleavage of pro-caspase 1 to p20 in a dose-dependent manner, inhibited the interaction between HDAC6 and dynein.

In Vivo

HDAC6-IN-13 (Compound 35m) (20 mg/kg; p.o. and i.p.; once) displays a remarkable inhibition in LPS-induced inflammation in mice^[1].
HDAC6-IN-13 (20 mg/kg; p.o.; once) shows very high oral bioavailability (F% = 93.4%) and significant BBB permeability in mice^[1].

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

Animal Model:

Male C57BL/6 WT mice, LPS-induced endotoxic shock model^[1]
Dosage:

20 mg/kg
Administration:

PO and IP, immediately after the LPS injection
Result:

Significantly decreased the serum IL-1β levels in LPS-induced mice via both ip and po administration.

Animal Model:

Male CD-1 mice^[1]
Dosage:

5 mg/kg or 20 mg/kg
Administration:

IV (5 mg/kg) or PO (20 mg/kg) (Pharmacokinetic Study)

Result:

Pharmacokinetics Characterization of HDAC6-IN-13 (Compound 35m) with iv and Oral Administration^a^[1]

PK parameters	HDAC6-IN-13	HDAC6-IN-13
administered dose (mg/kg)	iv at 5 mg/kg	oral at 20 mg/kg
C_max (ng/mL)	4604 ± 551	5570 ± 551
t_1/2 (h)	7.95 ± 0.370	6.80 ± 0.145
AUC_0−inf (ng•h/mL)	2755 ± 395	10292 ± 1385
F%	n/a	93.4 ± 12.6

^aHDAC6-IN-13 was administrated via iv and po (n = 3). The blood sample was collected at different time points after dosing, and the plasma concentration of HDAC6-IN-13 was determined via LC-MS/MS. The area under the plasma concentration versus time curve (AUC) was calculated using the linear trapezoidal method. The pharmacokinetic parameters were obtained using the noncompartmental method. Data are shown as mean ± SD.

Chemical Information

CAS. Nr. 2837128-41-1
Appearance Solid
Molecular Weight 370.45
Formel C₂₃H₂₂N₄O
Color Light yellow to yellow
SMILES

CCNNC(C1=CC=C(C=C1)CN2C3=CC=CC=C3C=CC4=C2C=NC=C4)=O
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 (337.43 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

2.6994 mL

13.4971 mL

26.9942 mL

5 mM

0.5399 mL

2.6994 mL

5.3988 mL

10 mM

0.2699 mL

1.3497 mL

2.6994 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 (281 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]. Yue K, et al. First-in-Class Hydrazide-Based HDAC6 Selective Inhibitor with Potent Oral Anti-Inflammatory Activity by Attenuating NLRP3 Inflammasome Activation. J Med Chem. 2022 Sep 8. [Content Brief]

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	2.6994 mL	13.4971 mL	26.9942 mL	67.4855 mL
	5 mM	0.5399 mL	2.6994 mL	5.3988 mL	13.4971 mL
	10 mM	0.2699 mL	1.3497 mL	2.6994 mL	6.7485 mL
	15 mM	0.1800 mL	0.8998 mL	1.7996 mL	4.4990 mL
	20 mM	0.1350 mL	0.6749 mL	1.3497 mL	3.3743 mL
	25 mM	0.1080 mL	0.5399 mL	1.0798 mL	2.6994 mL
	30 mM	0.0900 mL	0.4499 mL	0.8998 mL	2.2495 mL
	40 mM	0.0675 mL	0.3374 mL	0.6749 mL	1.6871 mL
	50 mM	0.0540 mL	0.2699 mL	0.5399 mL	1.3497 mL
	60 mM	0.0450 mL	0.2250 mL	0.4499 mL	1.1248 mL
	80 mM	0.0337 mL	0.1687 mL	0.3374 mL	0.8436 mL
	100 mM	0.0270 mL	0.1350 mL	0.2699 mL	0.6749 mL

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HDAC6-IN-13

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Histone Modification Research Compound Library

CNS-Penetrant Compound Library

Anti-Aging Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Liver Cancer Compound Library

Osteogenesis Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

High-Throughput Bioactive Compound Library

High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

Alle HDAC Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

HDAC6-IN-13

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Histone Modification Research Compound Library

CNS-Penetrant Compound Library

Anti-Aging Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Liver Cancer Compound Library

Osteogenesis Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

High-Throughput Bioactive Compound Library

High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

Alle HDAC Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

HDAC6-IN-13 Related Classifications

HY-151261 Related Classifications