Art. -Nr.: HY-120350

BI-1347

Name: BI-1347
Brand: MedChemExpress
SKU: HY-120350
Price: 100.00 USD
Availability: InStock
Rating: 5 (10 reviews)

10 Cited Publications

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Based on 10 publication(s) in Google Scholar

BI-1347 is an orally active, selective and potent CDK8 inhibitor (IC₅₀=1.1 nM). BI-1347 shows anti-tumoral activity.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

The BI-1347 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.

Reinheit : 99.85%
CAS. Nr.: 2163056-91-3
Formel: C₂₂H₂₀N₄O
Molecular Weight:356.42

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

BI-1347 Chemical Structure

CAS. Nr.: 2163056-91-3

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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
Publications (10)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

BI-1347 is an orally active, selective and potent CDK8 inhibitor (IC₅₀=1.1 nM). BI-1347 shows anti-tumoral activity^[1]^[2].

IC₅₀ & Target

^[1]

CDK8

1.1 nM (IC₅₀)

Alle CDK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	32.94 μM Compound: BI-1347	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 4 days by Celltiter glo luminescent assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 4 days by Celltiter glo luminescent assay	[PMID: 36930701]
HEK293	EC₅₀	5 nM Compound: 28; BI-1347	Inhibition of mouse derived homozygous Tg0N4R P301S mutant tau-induced human ON4R tau aggregation harboring P301S mutant transfected in HEK293 cells preincubated for 2 hrs followed by compound addition and measured after 3 hrs by YFP-based fluorescence as Inhibition of mouse derived homozygous Tg0N4R P301S mutant tau-induced human ON4R tau aggregation harboring P301S mutant transfected in HEK293 cells preincubated for 2 hrs followed by compound addition and measured after 3 hrs by YFP-based fluorescence as	[PMID: 32071678]
MDA-MB-231	IC₅₀	28.65 μM Compound: BI-1347	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 4 days by Celltiter glo luminescent assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 4 days by Celltiter glo luminescent assay	[PMID: 36930701]
MDA-MB-468	IC₅₀	28.82 μM Compound: BI-1347	Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 4 days by Celltiter glo luminescent assay Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 4 days by Celltiter glo luminescent assay	[PMID: 36930701]

In Vitro

BI-1347 (150 nM; 44 h) enhances granzyme B (GZMB+) production in mouse splenic NK cells^[2].
BI-1347 (0.1 nM-10 μM; 24 h) treatment increases perforin secretion from NK92MI cells^[2].

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

Western Blot Analysis^[2]

Cell Line:

Mouse splenic NK cells
Concentration:

150 nM
Incubation Time:

44 hours
Result:

Increased the proportion of granzyme B-positive NK cells by approximately 4-fold.

Western Blot Analysis^[2]

Cell Line:

Human NK92MI cells
Concentration:

0.1 nM-10 μM
Incubation Time:

24 hours
Result:

Increased perforin levels with an EC₅₀ value of 7.2 nM.

In Vivo

BI-1347 (oral gavage; 10 mg/kg; once daily; 30 d) modulates STAT1^S727 phosphorylation and shows anti-tumor activity in vivo^[2].
BI-1347 (oral gavage; 10 mg/kg) intermittent schedule and BI-8382 continuous treatment combination treatment increases efficacy compared to each monotherapy in the mammary carcinoma EMT6 model^[2].

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

Animal Model:

B16-F10-luc2 syngeneic melanoma model^[2]
Dosage:

10 mg/kg
Administration:

Oral gavage; 10 mg/kg; once daily; 30 d
Result:

Reduced phosphorylation of STAT1^S727 for at least 6 h by 60%.
Showed minimal effect on body weight at 10 mg/kg.
Showed lower tumor burden both on day 23 and 29, compared to the control group.

Chemical Information

CAS. Nr. 2163056-91-3
Appearance Solid
Molecular Weight 356.42
Formel C₂₂H₂₀N₄O
Color Light yellow to yellow
SMILES

O=C(N(C)C)CN1N=CC(C2=CC=C(C3=CN=CC4=C3C=CC=C4)C=C2)=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (10)

All Cell Proliferation/Viability AssayFlow CytometryRT-PCRWB

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Journal Impact Factor

Cell

BET inhibition blocks inflammation-induced cardiac dysfunction and SARS-CoV-2 infection. [Abstract]

2021 Apr 15;184(8):2167-2182.e22. PMID: 33811809
EMBO J

CDK8 remodels the tumor microenvironment and promotes resistance to KRASG12D inhibitors and daraxonrasib in PDAC. [Abstract]

2026 Aug;45(16):5727-5758. PMID: 42436354
Oncogenesis

Cyclin E modulates vulnerability to CDC7 kinase inhibition. [Abstract]

2026 Apr 24;15(1):27. PMID: 42031714
Pharmaceuticals (Basel)

New Assay Systems to Characterize the Broad-Spectrum Antiherpesviral and Non-Herpesviral Activity of Cyclin-Dependent Kinase (CDK) 8 Inhibitors. [Abstract]

2025 Oct 16;18(10):1560. PMID: 41155676

BI-1347 purchased from MedChemExpress. Usage Cited in: Pharmaceuticals (Basel). 2025 Oct 16;18(10):1560. [Abstract]

CDK8 inhibitor (BI-1347 (0.0001-100 μM; 4 days) were assessed for their level of cytotoxicity by a Neutral Red uptake assay (orange) and their antiviral activity (black) on COS-7 cells.

BI-1347 purchased from MedChemExpress. Usage Cited in: Pharmaceuticals (Basel). 2025 Oct 16;18(10):1560. [Abstract]

Summarized results for different cell types (Vero, COS-7 and HFFs) or different method approaches (GFP or qPCR) for the CDK8 inhibitors (BI-1347, CCT-251921, MSC-2530818) or reference compounds (BCV, CDV, GCV) based on the EC₅₀, CC₅₀, and SI of at least three replications; n.d. not determined.
Virus Res

2026 Sep 12:199799. PMID: 42731638
SSRN

2026 Jun 24.
Technical University of Dresden

2025.
bioRxiv

2025 Dec 9.

BI-1347 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Dec 9.

MCF10A cells were plated at equal low density and either mock treated or treated with 31 nM BI-1347, in the presence or absence of 1.25 µM or 10 µM XL413 over a 7-day period. Representative image of plates stained with crystal violet. The results showed that adding the CDK8 inhibitor BI-1347 to MCF10A cells only marginally inhibited their proliferation; in contrast, BI-1347 strongly reduced cell growth when BI-1347 was combined with either 1.25 µM or 10 µM of the CDC7i XL413.

BI-1347 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Dec 9.

MCF10A cells were mock treated or treated for 24 hours with three different CDK8 inhibitors: 31 nM BI-1347, 5 µM Senexin A, or 100 nM CCT-251921, alone or in combination with either 10 µM XL413 or 0.3 µM TAK-931 CDC7 inhibitors. Cells were labelled with EdU for last 30 minutes and DNA synthesis, DNA content and cell cycle distribution were assessed by flow cytometry.

BI-1347 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Dec 9.

MCF10A cells were either mock treated, treated with 31 nM BI-1347 alone, with 10 µM XL413 with or in combination of both or with 2mM Hydroxyurea (HU) for 24 hours. Whole cell extracts, or soluble and chromatin-enriched fractions were analysed by immunoblotting for the indicated proteins. TPS (total protein stain) is used as a loading control. Asterisks indicate non-specific bands.
bioRxiv

2025 Oct 11.
University of Washington

2025.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 125 mg/mL (350.71 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

2.8057 mL

14.0284 mL

28.0568 mL

5 mM

0.5611 mL

2.8057 mL

5.6114 mL

10 mM

0.2806 mL

1.4028 mL

2.8057 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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)}

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 (5.84 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 (5.84 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 (5.84 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 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)

Verweise

[1]. Harald Engelhardt, et al. New phenylpyrazolylacetamide compounds and derivatives as cdk8/cdk19 inhibitors.

[2]. Hofmann MH, et al. Selective and Potent CDK8/19 Inhibitors Enhance NK-Cell Activity and Promote Tumor Surveillance. Mol Cancer Ther. 2020 Apr;19(4):1018-1030. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.8057 mL	14.0284 mL	28.0568 mL	70.1420 mL
	5 mM	0.5611 mL	2.8057 mL	5.6114 mL	14.0284 mL
	10 mM	0.2806 mL	1.4028 mL	2.8057 mL	7.0142 mL
	15 mM	0.1870 mL	0.9352 mL	1.8705 mL	4.6761 mL
	20 mM	0.1403 mL	0.7014 mL	1.4028 mL	3.5071 mL
	25 mM	0.1122 mL	0.5611 mL	1.1223 mL	2.8057 mL
	30 mM	0.0935 mL	0.4676 mL	0.9352 mL	2.3381 mL
	40 mM	0.0701 mL	0.3507 mL	0.7014 mL	1.7535 mL
	50 mM	0.0561 mL	0.2806 mL	0.5611 mL	1.4028 mL
	60 mM	0.0468 mL	0.2338 mL	0.4676 mL	1.1690 mL
	80 mM	0.0351 mL	0.1754 mL	0.3507 mL	0.8768 mL
	100 mM	0.0281 mL	0.1403 mL	0.2806 mL	0.7014 mL

Bioz

Keywords

BI-1347

10 Cited Publications

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BI-1347

Publications Citing Use of MedChemExpress (MCE) BI-1347

Alle CDK Isoform-spezifische Produkte anzeigen