| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C19H23F2N5O2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
BI-D1870 is an ATP-competitive, cell-permeable, brain-penetrating inhibitor of the RSK isoforms, with IC50 values of 31 nM, 24 nM, 18 nM and 15 nM for RSK1, RSK2, RSK3 and RSK4, respectively[1][2][3][4][5]. It is supplied as a white to off-white solid (C19H23F2N5O2, MW 391.42) at 99.43% purity.
Physical & Chemical Properties
| CAS Number | 501437-28-1 |
|---|---|
| Molecular Formula | C19H23F2N5O2 |
| Molecular Weight | 391.42 g/mol |
| Purity | 99.43% |
| Appearance | Solid |
| 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 |
| Target | RSK1, RSK2, RSK3, RSK4 |
| Signaling Pathway | MAPK/ERK Pathway; Autophagy |
| Solubility | In Vitro: DMSO: 100 mg/mL (255.48 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 100 mg/mL (255.48 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (6.39 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.5 mg/mL (6.39 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (6.39 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
BI-D1870 inhibits an RSK2 mutant, RSK21-389:S381E, which lacks the C-terminal kinase catalytic domain, with an IC50 of approx. 30 nM. In kinase assays run with 100 μM ATP, the IC50 values of BI-D1870 are 10 nM for RSK1 and 20 nM for RSK2. With a 10-fold lower ATP concentration, the IC50 of BI-D1870 drops to 5 nM (RSK1) and 10 nM (RSK2)[1]. BI-D1870 inhibits PLK1 (IC50 100 nM), while Aurora B, DYRK1a, CDK2-A, Lck, CK1 and GSK3β show IC50 values 10- to 100-fold higher than those of the RSK isoforms. In HEK-293 cells, BI-D1870 (10 μM) blocks PMA-induced phosphorylation of GSK3α and GSK3β. Also in HEK-293 cells, BI-D1870 blocks EGF-induced phosphorylation of LKB1 at Ser431, with an IC50 of approx. 1 μM[1]. BI-D1870 leaves activation of ERK1/ERK2 and MSK1 unaffected, and does not inhibit CREB phosphorylation[1]. BI-D1870 acts as a potent RSK family kinase inhibitor (Kds: 10-100 nM) that also interacts with BRD4(1) (Kd 3.5 μM) and the PLK family (appr 10 nM)[2]. In serum-starved LN-229 cells, BI-D1870 (10 μM) strongly induces p70S6K activation, and it also stimulates phosphorylation of rpS6 and p70S6K in LN-18 cells. At 1 μM, BI-D1870 potently inhibits rpS6 phosphorylation; PMA-induced rpS6 phosphorylation is inhibited at concentrations higher than 1 μM[4]. BI-D1870 (1-5 μM) inhibits cell proliferation in all cell types in a dose- and time-dependent manner. In SCC4 cells and HSC-3 cells, BI-D1870 (1-3 μM) triggers apoptosis. Cell survival signaling pathways, including Akt and p38 MAPK, are modulated dose-dependently by BI-D1870 (0-5)[5].
In Vivo
Experimental autoimmune encephalomyelitis (EAE) mice injected with BI-D1870 (0.5 mg/kg) display a delayed neural deficit, with no obvious weight loss. Histopathological analyses reveal inflammatory cell infiltration and demyelination within the spinal cord of control mice, while BI-D1870-treated mice lack them. BI-D1870 guards against TH1 or TH17 cell infiltration into the CNS[3].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Animal Administration[3]
Induce EAE in C57/BL6J mice with myelin oligodendrocyte glycoprotein (MOG) peptide 35-55 MEVGWYRSPFSRVVHLYRNGK) (BEX). Inject mice s.c. with 200 g of MOG peptide in 100 μL of PBS, mixed with 100 μL complete Freund’s adjuvant (CFA), further supplemented with five mg/mL Mycobacterium tuberculosis, as an emulsion. Additionally, inject 500 ng pertussis toxin i.p. on days zero and two. Two days after immunization with MOG peptide, inject the RSK inhibitor (BI-D1870; 0.5 mg/kg) i.p. into the mice, and repeat the injection every other day for 11 days. Use mice receiving only dimethyl sulfoxide (DMSO) solution as controls. Score paralysis on the following scale: zero for no disease; one for tail limpness; two for hind limb weakness; three for hind limb paralysis; four for fore limb weakness; five for quadriplegia; six for death. For histological analysis, fix CNS samples with 4% paraformaldehyde, slice them at 4 μm, and then perform hematoxylin & eosin (H & E) staining.
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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RSK1 is an exploitable dependency in myeloproliferative neoplasms and secondary acute myeloid leukemia. Nat Commun 2025 Jan 16;16(1):492. PMID: 39820365
Salmonella effector SopF regulates PANoptosis of intestinal epithelial cells to aggravate systemic infection. Gut Microbes 2023 Jan-Dec;15(1):2180315. PMID: 36803521
RSK-3 promotes cartilage regeneration via interacting with rpS6 in cartilage stem/progenitor cells. Theranostics 2020 May 25;10(15):6915-6927. PMID: 32550912
Kartogenin hydrolysis product 4-aminobiphenyl distributes to cartilage and mediates cartilage regeneration. Theranostics 2019 Sep 21;9(24):7108-7121.
Functional Phosphoproteomics in Cancer Chemoresistance Using CRISPR-Mediated Base Editors. Adv Sci (Weinh) 2022 Oct;9(30):e2200717. PMID: 36045417
Insulin- and exercise-induced phosphoproteomics of human skeletal muscle identify REPS1 as a regulator of muscle glucose uptake. Cell Rep Med 2025 Jun 17;6(6):102163. PMID: 40482643
RSK1 dependency in FLT3-ITD acute myeloid leukemia. Blood Cancer J 2024 Nov 26;14(1):207. PMID: 39592591
Discovery of a novel dual-target inhibitor against RSK1 and MSK2 to suppress growth of human colon cancer. Oncogene 2020 Oct;39(43):6733-6746. PMID: 32963350
Deciphering protein mutation-phenotype linkages from CRISPR-based tiling mutagenesis screens. Cell Syst 2026 Jun 26:101651. PMID: 42361799
RSK1 promotes mammalian axon regeneration by inducing the synthesis of regeneration-related proteins. PLoS Biol 2022 Jun 1;20(6):e3001653. PMID: 35648763
