2. Cell Cycle/DNA Damage
  3. CDK
  4. JH-XVI-178

JH-XVI-178 is a highly efficient and selective CDK8/19 inhibitor, with IC50 values of 1 and 2 nM for CDK8 and CDK19, respectively. JH-XVI-178 has a low clearance rate and moderate oral pharmacokinetic properties.

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

JH-XVI-178 Chemical Structure

JH-XVI-178 Chemical Structure

CAS No. : 2648453-53-4

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Customer Review

Based on 1 publication(s) in Google Scholar

JH-XVI-178 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE JH-XVI-178

View All CDK Isoform Specific Products:

View All Isoforms
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

JH-XVI-178 is a highly efficient and selective CDK8/19 inhibitor, with IC50 values of 1 and 2 nM for CDK8 and CDK19, respectively. JH-XVI-178 has a low clearance rate and moderate oral pharmacokinetic properties[1].

IC50 & Target

CDK8

1 nM (IC50)

CDK19

2 nM (IC50)

In Vitro

JH-XVI-178 (0-1000 nM, 24 h) inhibits the phosphorylation of S727-STAT1 in Jurkat cells[1].
JH-XVI-178 shows off-target inhibition for STK16 and FLT3 (D835V), with an IC50 of 107 nM for STK16[1].

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

JH-XVI-178 Related Antibodies
In Vivo


Pharmacokinetic Analysis in Mice Model[1]

Route Dose (mg/kg) AUClast (ng•min/mL) T1/2 (h) Cmax (μM) Clobs (mL•min/kg) Vss (L/kg) F (%)
Oral 10 51863 1.3 1.04 17 0.8 8

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

435.91

Formula

C22H22ClN7O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=NNC2=NC=C(C3=CC(C=NN4C)=C4C=C3)C(N5CCC6(CCNC6=O)CC5)=C21
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (143.38 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2941 mL 11.4703 mL 22.9405 mL
5 mM 0.4588 mL 2.2941 mL 4.5881 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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 2.2941 mL 11.4703 mL 22.9405 mL 57.3513 mL
5 mM 0.4588 mL 2.2941 mL 4.5881 mL 11.4703 mL
10 mM 0.2294 mL 1.1470 mL 2.2941 mL 5.7351 mL
15 mM 0.1529 mL 0.7647 mL 1.5294 mL 3.8234 mL
20 mM 0.1147 mL 0.5735 mL 1.1470 mL 2.8676 mL
25 mM 0.0918 mL 0.4588 mL 0.9176 mL 2.2941 mL
30 mM 0.0765 mL 0.3823 mL 0.7647 mL 1.9117 mL
40 mM 0.0574 mL 0.2868 mL 0.5735 mL 1.4338 mL
50 mM 0.0459 mL 0.2294 mL 0.4588 mL 1.1470 mL
60 mM 0.0382 mL 0.1912 mL 0.3823 mL 0.9559 mL
80 mM 0.0287 mL 0.1434 mL 0.2868 mL 0.7169 mL
100 mM 0.0229 mL 0.1147 mL 0.2294 mL 0.5735 mL
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JH-XVI-178 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JH-XVI-1782648453-53-4CDKCyclin dependent kinaseJurkatCDK8oralInhibitorinhibitorinhibit

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