BI-D1870
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
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) BI-D1870
More- Nat Commun. 2025 Jan 16;16(1):492. [Abstract]
- Adv Sci (Weinh). 2022 Oct;9(30):e2200717. [Abstract]
- Theranostics. 2020 May 25;10(15):6915-6927. [Abstract]
- Theranostics. 2019 Sep 21;9(24):7108-7121. [Abstract]
- Blood Cancer J. 2024 Nov 26;14(1):207. [Abstract]
- Gut Microbes. 2023 Jan-Dec;15(1):2180315. [Abstract]
- Cell Rep Med. 2025 May 29:102163. [Abstract]
- Cell Syst. 2026 Jun 26:101651. [Abstract]
- Oncogene. 2020 Oct;39(43):6733-6746. [Abstract]
- PLoS Biol. 2022 Jun 1;20(6):e3001653. [Abstract]
- Transl Res. 2021 Oct:236:117-132. [Abstract]
- PLoS Pathog. 2025 Nov 24;21(11):e1013737. [Abstract]
- Cancers (Basel). 2023 Mar 28;15(7):2023. [Abstract]
- iScience. 2026 Mar 30;29(5):115495. [Abstract]
- J Biol Chem. 2026 Jun;302(6):111461. [Abstract]
- Viruses. 2018 Apr 13;10(4). pii: E191. [Abstract]
- Harvard University. 2026.
- bioRxiv. 2025 April 23.
- University of Washington. 2025.
- bioRxiv. 2025 March 03.
- Universidad de Granada. 2020 Sep.
- Oncotarget. 2016 Mar 1;7(9):10283-96. [Abstract]
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Biological Activity
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RSK1 |
RSK2 |
RSK3 |
RSK4 |
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Cell Line
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Type | Value | Description | References |
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| MOLM-13 | EC50 |
1.89 μM
Compound: 1; BI-D1870
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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
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[PMID: 31982240] |
| MOLM-13 | EC50 |
2.8 μM
Compound: 1; BI-D1870
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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
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[PMID: 31982240] |
| MOLM-13 | EC50 |
3.41 μM
Compound: 1; BI-D1870
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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
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[PMID: 31982240] |
| TE-10 | IC50 |
1.89 μM
Compound: 2; BI-D1870
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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
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[PMID: 34496560] |
| TE-10 | IC50 |
4.553 μM
Compound: 2; BI-D1870
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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
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[PMID: 34496560] |
BI-D1870 inhibits a mutant of RSK2 lacking the C-terminal kinase catalytic domain (RSK21-389: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 (Kds: 10-100 nM), and also interact with BRD4(1) and PLK family, with Kds 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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 501437-28-1
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Appearance Solid
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Molecular Weight 391.42
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Formula C19H23F2N5O2
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Color White to off-white
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SMILES
OC1=C(F)C=C(NC2=NC(N(CCC(C)C)C(C)C(N3C)=O)=C3C=N2)C=C1F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (22)
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Journal Impact Factor
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Most Recent
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Nat Commun
RSK1 is an exploitable dependency in myeloproliferative neoplasms and secondary acute myeloid leukemia. [Abstract]2025 Jan 16;16(1):492. PMID: 39820365 -
Adv Sci (Weinh)
Functional Phosphoproteomics in Cancer Chemoresistance Using CRISPR-Mediated Base Editors. [Abstract]2022 Oct;9(30):e2200717. PMID: 36045417 -
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 -
Blood Cancer J
2024 Nov 26;14(1):207. PMID: 39592591 -
Gut Microbes
Salmonella effector SopF regulates PANoptosis of intestinal epithelial cells to aggravate systemic infection. [Abstract]2023 Jan-Dec;15(1):2180315. PMID: 36803521 -
Cell Rep Med
Insulin- and exercise-induced phosphoproteomics of human skeletal muscle identify REPS1 as a regulator of muscle glucose uptake. [Abstract]2025 May 29:102163. PMID: 40482643 -
Cell Syst
Deciphering protein mutation-phenotype linkages from CRISPR-based tiling mutagenesis screens. [Abstract]2026 Jun 26:101651. PMID: 42361799 -
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 -
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
2026 Jun;302(6):111461. PMID: 41999888 -
Viruses
2018 Apr 13;10(4). pii: E191. PMID: 29652799
BI-D1870 purchased from MedChemExpress. Usage Cited in: Viruses. 2018 Apr 13;10(4). pii: E191. [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). pii: E191. [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.
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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
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Purified His6-RSK1, His6-RSK2 or GST-RSK21-389:S381E (1-2 units/mL) are assayed for 10 min at 30°C in a 50 μL assay mixture in Buffer A containing 30 μM substrate peptide (KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK), 10 mM magnesium acetate and 100 μM of [γ-32P]ATP. Reactions are terminated and analysed. The amount of enzyme that catalysed the phosphorylation of 1 nmol of substrate peptide in 1 min is termed one unit.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Measurement of cell growth is assessed using the MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide] assay in six replicates. The cells (5×103/200 μL) are seeded in 96-well, flat-bottom plates for 24 h and then exposed to various concentrations of test agents for the indicated time intervals. After removing the culture medium, 200 μL of the medium containing MTT at a concentration of 0.5 mg/mL is added, and the cells are incubated at 37°C for 2 h. The medium is removed, and the reduced MTT dye in each well is dissolved in 200 μL DMSO. Absorbance is determined with a multimode microplate reader Synergy HT at 570 nm.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Myelin oligodendrocyte glycoprotein (MOG) peptide 35-55 MEVGWYRSPFSRVVHLYRNGK) (BEX) is used to induce EAE in C57/BL6J mice. Mice are injecteds.c. with 200 g of MOG peptide in 100 μL of PBS emulsified in 100 μL complete Freund’s adjuvant (CFA) that is further supplemented with five mg/mL Mycobacterium tuberculosis. In addition, 500 ng pertussis toxin is injected i.p. on days zero and two. The RSK inhibitor (BI-D1870; 0.5 mg/kg) is injected i.p. into mice two days after immunization with MOG peptide, and injection is repeated every other day for 11 days. Mice that receive only dimethyl sulfoxide (DMSO) solution are used as controls. Paralysis is evaluated according to the following scale: zero, no disease; one, tail limpness; two, hind limb weakness; three, hind limb paralysis; four, fore limb weakness; five, quadriplegia; six, death. For histological analysis, CNS samples are fixed with 4% paraformaldehyde and sliced at 4 μm, and then hematoxylin & eosin (H & E) staining is performed.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (282 KB)
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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)
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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]
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, 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 | 2.5548 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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