Cat. No.: HY-10510

BI-D1870

Name: BI-D1870
Brand: MedChemExpress
SKU: HY-10510
Price: 89.00 USD
Availability: InStock
Rating: 5 (22 reviews)

22 Cited Publications

Customer Review

Based on 22 publication(s) in Google Scholar

BI-D1870 is an ATP-competitive, cell permeable and brain penetrated inhibitor of RSK isoforms, with IC₅₀s of 31 nM/24 nM/18 nM/15 nM for RSK1/RSK2/RSK3/RSK4, respectively.

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

Purity : 99.43%
CAS No.: 501437-28-1
Formula: C₁₉H₂₃F₂N₅O₂
Molecular Weight:391.42

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

BI-D1870 Chemical Structure

CAS No.: 501437-28-1

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (22)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

BI-D1870 is an ATP-competitive, cell permeable and brain penetrated inhibitor of RSK isoforms, with IC₅₀s of 31 nM/24 nM/18 nM/15 nM for RSK1/RSK2/RSK3/RSK4, respectively^[1]^[2]^[3]^[4]^[5].

IC₅₀ & Target

RSK1

RSK2

RSK3

RSK4

All Ribosomal S6 Kinase (RSK) Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MOLM-13	EC₅₀	1.89 μM Compound: 1; BI-D1870	Antiproliferative activity against human MOLM13 assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MOLM13 assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 31982240]
MOLM-13	EC₅₀	2.8 μM Compound: 1; BI-D1870	Antiproliferative activity against human MOLM13 assessed as reduction in cell viability incubated for 72 hrs by MTS assay Antiproliferative activity against human MOLM13 assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 31982240]
MOLM-13	EC₅₀	3.41 μM Compound: 1; BI-D1870	Antiproliferative activity against human MOLM13 assessed as reduction in cell viability incubated for 72 hrs by CellTox green assay Antiproliferative activity against human MOLM13 assessed as reduction in cell viability incubated for 72 hrs by CellTox green assay	[PMID: 31982240]
TE-10	IC₅₀	1.89 μM Compound: 2; BI-D1870	Inhibition of cell invasion in human TE-10 cells measured after 24 hrs by Giemsa staining based transwell invasion assay Inhibition of cell invasion in human TE-10 cells measured after 24 hrs by Giemsa staining based transwell invasion assay	[PMID: 34496560]
TE-10	IC₅₀	4.553 μM Compound: 2; BI-D1870	Antiproliferative activity against human TE-10 cells assessed as inhibition of cell proliferation measured up to 48 hrs by CCK-8 assay Antiproliferative activity against human TE-10 cells assessed as inhibition of cell proliferation measured up to 48 hrs by CCK-8 assay	[PMID: 34496560]

In Vitro

BI-D1870 inhibits a mutant of RSK2 lacking the C-terminal kinase catalytic domain (RSK2^1-389:S381E) with an IC₅₀ of approx. 30 nM. BI-D1870 inhibits RSK1 and RSK2 with IC₅₀ values of 10 nM and 20 nM respectively, when the kinase assays are performed with 100 μM ATP. When the assays are performed at a 10-fold lower ATP concentration, the IC₅₀ of BI-D1870 is reduced to 5 nM for RSK1 and 10 nM for RSK2^[1].
BI-D1870 inhibits PLK1 with an IC₅₀ of 100 nM, whilst the IC₅₀ values for Aurora B, DYRK1a, CDK2-A, Lck, CK1 and GSK3β are 10- to 100-fold higher than that of the RSK isoforms. BI-D1870 (10 μM) inhibits the PMA-induced phosphorylation of GSK3α and GSK3β in HEK-293 cells. In HEK-293 cells, BI-D1870 inhibits the EGF-induced phosphorylation of LKB1 at Ser431 with an IC₅₀ of approx. 1 μM^[1].
BI-D1870 does not affect the activation of ERK1/ERK2 and MSK1, nor does it inhibit the phosphorylation of CREB^[1].
BI-D1870 is a potent RSK family kinase inhibitor (K_ds: 10-100 nM), and also interact with BRD4(1) and PLK family, with K_ds of 3.5 μM and appr 10 nM^[2].
BI-D1870 (10 μM) strongly induces p70S6K activation in serum-starved LN-229 cells, and alao stimulates the phosphorylation of rpS6 and p70S6K in LN-18 cells. BI-D1870 (1 μM) potently inhibits rpS6 phosphorylation, and inhibits PMA-induced rpS6 phosphorylation at concentrations higher than 1 μM^[4].
BI-D1870 (1-5 μM) induces a dose- and time-dependent inhibition of cell proliferation in all cell types. BI-D1870 (1-3 μM) induces apoptosis in SCC4 cells and HSC-3 cells. BI-D1870 (0-5) modulates cell survival signaling pathways including Akt and p38 MAPK dose-dependently^[5].

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

In Vivo

BI-D1870 (0.5 mg/kg)-injected experimental autoimmune encephalomyelitis (EAE) mice exhibits a delayed neural deficit without obvious weight loss. Histopathological analyses shows inflammatory cell infiltration and demyelination in the spinal cord in control mice, but not in BI-D1870-treated mice. BI-D1870 protects against the infiltration of TH1 or TH17 cells into the CNS^[3].

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

Chemical Information

CAS No. 501437-28-1
Appearance Solid
Molecular Weight 391.42
Formula C₁₉H₂₃F₂N₅O₂
Color White to off-white
SMILES

OC1=C(F)C=C(NC2=NC(N(CCC(C)C)C(C)C(N3C)=O)=C3C=N2)C=C1F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (22)

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Journal Impact Factor

Nat Commun

RSK1 is an exploitable dependency in myeloproliferative neoplasms and secondary acute myeloid leukemia. [Abstract]

2025 Jan 16;16(1):492. PMID: 39820365
Gut Microbes

Salmonella effector SopF regulates PANoptosis of intestinal epithelial cells to aggravate systemic infection. [Abstract]

2023 Jan-Dec;15(1):2180315. PMID: 36803521
Theranostics

RSK-3 promotes cartilage regeneration via interacting with rpS6 in cartilage stem/progenitor cells. [Abstract]

2020 May 25;10(15):6915-6927. PMID: 32550912
Theranostics

Kartogenin hydrolysis product 4-aminobiphenyl distributes to cartilage and mediates cartilage regeneration. [Abstract]

2019 Sep 21;9(24):7108-7121. PMID: 31695756
Adv Sci (Weinh)

Functional Phosphoproteomics in Cancer Chemoresistance Using CRISPR-Mediated Base Editors. [Abstract]

2022 Oct;9(30):e2200717. PMID: 36045417
Cell Rep Med

Insulin- and exercise-induced phosphoproteomics of human skeletal muscle identify REPS1 as a regulator of muscle glucose uptake. [Abstract]

2025 Jun 17;6(6):102163. PMID: 40482643
Blood Cancer J

RSK1 dependency in FLT3-ITD acute myeloid leukemia. [Abstract]

2024 Nov 26;14(1):207. PMID: 39592591
Oncogene

Discovery of a novel dual-target inhibitor against RSK1 and MSK2 to suppress growth of human colon cancer. [Abstract]

2020 Oct;39(43):6733-6746. PMID: 32963350
Cell Syst

Deciphering protein mutation-phenotype linkages from CRISPR-based tiling mutagenesis screens. [Abstract]

2026 Jun 26:101651. PMID: 42361799
PLoS Biol

RSK1 promotes mammalian axon regeneration by inducing the synthesis of regeneration-related proteins. [Abstract]

2022 Jun 1;20(6):e3001653. PMID: 35648763
Transl Res

Ribosomal proteins as distinct "passengers" of microvesicles: new semantics in myeloma and mesenchymal stem cells' communication. [Abstract]

2021 Oct:236:117-132. PMID: 33887527
PLoS Pathog

ORF45-induced Filamin A phosphorylation promotes cell motility and cell-contact dependent viral infection of Kaposi's sarcoma-associated herpesvirus. [Abstract]

2025 Nov 24;21(11):e1013737. PMID: 41284726
Cancers (Basel)

BI-D1870 Induces Mitotic Dysfunction and Apoptosis in Neuroblastoma by Regulating the PI3K-Akt-mTORC1 Signal Axis. [Abstract]

2023 Mar 28;15(7):2023. PMID: 37046682
iScience

RSK1-SRF signaling axis drives fibroblast activation and pulmonary fibrosis: Genetic causality and therapeutic targeting. [Abstract]

2026 Mar 30;29(5):115495. PMID: 42004028
J Biol Chem

The E3 ligase β-TRCP1 earmarks OTUD3 for destruction to fine-tune cGAS activation. [Abstract]

2026 Jun;302(6):111461. PMID: 41999888
Viruses

Combination Kinase Inhibitor Treatment Suppresses Rift Valley Fever Virus Replication. [Abstract]

2018 Apr 13;10(4):191. PMID: 29652799

BI-D1870 purchased from MedChemExpress. Usage Cited in: Viruses. 2018 Apr 13;10(4):191. [Abstract]

H2.35 cells are serum starved for 72 h and then are pre-treated with either DMSO or 10 µM PD0325901 (ERK IN). Cells are infected with MP12 (MOI 5) for one hour, followed by removal of viral inoculum, and addition of growth medium containing DMSO or 10 µM ERK IN. At 18 hpi, cell lysates are collected for western blot analysis.

BI-D1870 purchased from MedChemExpress. Usage Cited in: Viruses. 2018 Apr 13;10(4):191. [Abstract]

H2.35 cells are serum starved for 72 h and then were pre-treated with either DMSO or BI-D1870 (p90 IN, 10 µM). Cells are infected with MP12 (MOI 5) for one hour, followed by removal of viral inoculum, and addition of growth medium containing DMSO or p90 IN (10 µM). At 18 hpi, cell lysates are collected for western blot analysis.
Harvard University

2026.
bioRxiv

2025 April 23.
University of Washington

2025.
bioRxiv

2025 March 03.
Universidad de Granada

2020 Sep.
Oncotarget

Ras-activated RSK1 phosphorylates EBP50 to regulate its nuclear localization and promote cell proliferation. [Abstract]

2016 Mar 1;7(9):10283-96. PMID: 26862730

BI-D1870 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Mar 1;7(9):10283-96. [Abstract]

HeLa cells synchronized at mitotic phase are treated with BI-D1870 at indicated concentrations. Phosphorylation of EBP50 is assayed by Western blotting using p-EBP50 (T156) antibody. Phosphorylation of RSK1 at S380 and ribosomal protein S6 (rpS6) at S235-236 are assayed to examine activation of RSK1 at mitotic phase. GAPDH or α-tubulin is examined as a loading control. The morphology of cells at the moment of harvest for the above experiment is shown in photographs.

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (255.48 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

2.5548 mL

12.7740 mL

25.5480 mL

5 mM

0.5110 mL

2.5548 mL

5.1096 mL

10 mM

0.2555 mL

1.2774 mL

2.5548 mL

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

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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: ≥ 2.5 mg/mL (6.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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
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g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
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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 (282 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]. Sapkota GP, et al. BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo. Biochem J. 2007 Jan 1;401(1):29-38. [Content Brief]

[2]. Ciceri P, et al. Dual kinase-bromodomain inhibitors for rationally designed polypharmacology. Nat Chem Biol. 2014 Mar 2. [Content Brief]

[3]. Takada I, et al. The ribosomal S6 kinase inhibitor BI-D1870 ameliorated experimental autoimmune encephalomyelitis in mice. Immunobiology. 2016 Feb;221(2):188-92. [Content Brief]

[4]. Roffe M, et al. Two widely used RSK inhibitors, BI-D1870 and SL0101, alter mTORC1 signaling in a RSK-independent manner. Cell Signal. 2015 Aug;27(8):1630-42. [Content Brief]

[5]. Chiu CF, et al. Antitumor effects of BI-D1870 on human oral squamous cell carcinoma. Cancer Chemother Pharmacol. 2014 Feb;73(2):237-47. [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	2.5548 mL	12.7740 mL	25.5480 mL	63.8700 mL
	5 mM	0.5110 mL	2.5548 mL	5.1096 mL	12.7740 mL
	10 mM	0.2555 mL	1.2774 mL	2.5548 mL	6.3870 mL
	15 mM	0.1703 mL	0.8516 mL	1.7032 mL	4.2580 mL
	20 mM	0.1277 mL	0.6387 mL	1.2774 mL	3.1935 mL
	25 mM	0.1022 mL	0.5110 mL	1.0219 mL	2.5548 mL
	30 mM	0.0852 mL	0.4258 mL	0.8516 mL	2.1290 mL
	40 mM	0.0639 mL	0.3194 mL	0.6387 mL	1.5968 mL
	50 mM	0.0511 mL	0.2555 mL	0.5110 mL	1.2774 mL
	60 mM	0.0426 mL	0.2129 mL	0.4258 mL	1.0645 mL
	80 mM	0.0319 mL	0.1597 mL	0.3194 mL	0.7984 mL
	100 mM	0.0255 mL	0.1277 mL	0.2555 mL	0.6387 mL

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BI-D1870

Publications Citing Use of MedChemExpress (MCE) BI-D1870

All Ribosomal S6 Kinase (RSK) Isoforms