Cat. No.: HY-126141

JAK/HDAC-IN-1

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

JAK/HDAC-IN-1 is a potent JAK2/HDAC dual inhibitor, exhibits antiproliferative and proapoptotic activities in several hematological cell lines. JAK/HDAC-IN-1 shows IC₅₀s of 4 and 2 nM for JAK2 and HDAC, respectively.

For research use only. We do not sell to patients.

Purity: 98.63%
CAS No.: 2284621-75-4
Formula: C₁₉H₂₁Cl₂N₇O₂
Molecular Weight:450.32

Storage:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

JAK/HDAC-IN-1 Chemical Structure

CAS No.: 2284621-75-4

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

JAK2

4 nM (IC₅₀)

JAK1

4.8 nM (IC₅₀)

JAK3

7.4 nM (IC₅₀)

Tyk2

49 nM (IC₅₀)

HDAC

2 nM (IC₅₀)

HDAC2

14 nM (IC₅₀)

HDAC6

120 nM (IC₅₀)

HDAC8

2470 nM (IC₅₀)

All JAK Isoforms :

All HDAC Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HEL	IC₅₀	0.09 μM Compound: 8m	Antiproliferative activity against HEL cells harboring JAK2 V617F mutant assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against HEL cells harboring JAK2 V617F mutant assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 30901208]
HeLa	IC₅₀	0.002 μM Compound: 8m	Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay	[PMID: 30901208]
Jurkat	IC₅₀	0.06 μM Compound: 8m	Antiproliferative activity against human Jurkat cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human Jurkat cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 30901208]
K562	IC₅₀	0.49 μM Compound: 8m	Antiproliferative activity against human K562 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human K562 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 30901208]
MOLT-4	IC₅₀	0.08 μM Compound: 8m	Antiproliferative activity against human MOLT4 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human MOLT4 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 30901208]

In Vitro

JAK/HDAC-IN-1 (Compound 8m) exhibits IC₅₀s of 4.8, 7.4 and 49 nM for JAK1, JAK3 and TYK2, and 14, 120, 2470 nM for HDAC2, HDAC6 and HDAC8, respectively^[1].

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

Chemical Information

CAS No. 2284621-75-4
Appearance Solid
Molecular Weight 450.32
Formula C₁₉H₂₁Cl₂N₇O₂
Color White to off-white
SMILES

ClC1=CC=C(NC2=NC(NC3=CN(CCCCCC(NO)=O)N=C3)=NC=C2Cl)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (1)

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Journal Impact Factor

J Exp Clin Cancer Res

Combination of dual JAK/HDAC inhibitor with regorafenib synergistically reduces tumor growth, metastasis, and regorafenib-induced toxicity in colorectal cancer. [Abstract]

2024 Jul 11;43(1):192. PMID: 38992681

Solvent & Solubility

In Vitro:

DMSO : 20.83 mg/mL (46.26 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

2.2206 mL

11.1032 mL

22.2064 mL

5 mM

0.4441 mL

2.2206 mL

4.4413 mL

10 mM

0.2221 mL

1.1103 mL

2.2206 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

Mass Mass

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Molecular Weight Molecular Weight

Dilution Calculator

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (4.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (4.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)

References

[1]. Liang X, et al. Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies. J Med Chem. 2019 Apr 25;62(8):3898-3923. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2206 mL	11.1032 mL	22.2064 mL	55.5161 mL
	5 mM	0.4441 mL	2.2206 mL	4.4413 mL	11.1032 mL
	10 mM	0.2221 mL	1.1103 mL	2.2206 mL	5.5516 mL
	15 mM	0.1480 mL	0.7402 mL	1.4804 mL	3.7011 mL
	20 mM	0.1110 mL	0.5552 mL	1.1103 mL	2.7758 mL
	25 mM	0.0888 mL	0.4441 mL	0.8883 mL	2.2206 mL
	30 mM	0.0740 mL	0.3701 mL	0.7402 mL	1.8505 mL
	40 mM	0.0555 mL	0.2776 mL	0.5552 mL	1.3879 mL

Keywords

JAK/HDAC-IN-1

1 Cited Publications

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JAK/HDAC-IN-1

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

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Bioactive Compound Library Max

MCE Bioactive Compound Library

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High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) JAK/HDAC-IN-1

All JAK Isoforms

All HDAC Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

JAK/HDAC-IN-1 Related Classifications

Cat. No.: HY-126141