2. Signaling Pathways
  3. MAPK/ERK Pathway
  4. Ribosomal S6 Kinase (RSK)
  5. RSK2 Isoform

RSK2

RSK2 (ribosomal S6 kinase 2, RPS6KA3) is a widely expressed serine/threonine kinase of the p90RSK family that functions downstream of ERK1/2 and phosphoinositide-dependent kinase 1, positioning it as a critical effector of MAPK signaling that regulates cell survival, proliferation, and transcriptional responses[1][2]. RSK2 integrates extracellular growth-factor signals into intracellular phosphorylation events and contributes to the control of cell-cycle progression and transformation-associated programs through phosphorylation of downstream substrates[1][3]. Mechanistically, RSK2 participates in RAS-MAPK pathway regulation and influences phosphorylation of signaling and transcriptional regulators, thereby affecting cellular growth and adaptive responses[2][4]. In disease-relevant models, genetic deletion or knockdown of RSK2 suppresses cell proliferation, induces G1-phase accumulation, and reduces oncogenic transformation, whereas increased RSK2 activity promotes tumor-promoter-induced cell transformation and cancer-related phenotypes[1][5]. RSK2 is also clinically significant because loss-of-function mutations in RPS6KA3 cause Coffin-Lowry syndrome, linking RSK2-dependent signaling to neurodevelopmental and skeletal abnormalities[6][7]. Compared with related RSK isoforms, RSK2 has been identified as a specific binding partner of SPRED2, revealing isoform-selective regulation within the RAS-MAPK network and highlighting functional distinctions that are not shared uniformly across the RSK family[2]. For experimental applications, pharmacological inhibitors including kaempferol and the RSK inhibitor BI-D1870 have been used to suppress RSK-dependent signaling, making RSK2 a valuable target for mechanistic studies of MAPK-driven proliferation, transformation, and therapeutic intervention strategies[1][4].

RSK2 Related Products (14):

Cat. No. Product Name Effect Purity
  • HY-10510
    BI-D1870
    		Inhibitor 99.43%
    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.
  • HY-N0643
    Carnosol
    		Inhibitor 99.90%
    Carnosol is a potent Ribosomal S6 Kinase (RSK2) inhibitor that could be useful for treating gastric cancer, with an IC50 of ~5.5 μM. Carnosol, a Nrf2 activator, increases the nuclear levels of Nrf2 and can promote the expression of heme oxygenase 1 (HMOX1).
  • HY-136848
    SM1-71
    		Inhibitor
    SM1-71 (compound 5) is a potent TAK1 inhibitor, with a Ki of 160 nM, it also can covalently inhibit MKNK2, MAP2K1/2/3/4/6/7, GAK, AAK1, BMP2K, MAP3K7, MAPKAPK5, GSK3A/B, MAPK1/3, SRC, YES1, FGFR1, ZAK (MLTK), MAP3K1, LIMK1 and RSK2. SM1-71 can inhibit proliferation of multiple cancer cell lines.
  • HY-19713
    LJI308
    		Inhibitor 99.07%
    LJI308 is a potent pan-ribosomal S6 kinase (RSK) inhibitor, with IC50s of 6 nM, 4 nM, and 13 nM for RSK1, RSK2, and RSK3, respectively. LJI308 inhibits the phosphorylation of RSK (T359/S363) and YB-1 (S102) after irradiation, treatment with EGF, and in cells expressing a KRAS mutation.
  • HY-10579
    Pluripotin
    		Inhibitor 98.86%
    Pluripotin is a dual inhibitor of ERK1 and RasGAP with KDs of 98 nM and 212 nM, respectively. Pluripotin also inhibits RSK1, RSK2, RSK3, and RSK4 with IC50s of 0.5, 2.5, 3.3, and 10.0 μM, respectively.
  • HY-52101A
    FMK
    		Inhibitor 99.83%
    FMK is a an irreversible RSK2 kinase inhibitor, that covalently modifies the C-terminal kinase domain of RSK.
  • HY-16104
    BIX 02565
    		Inhibitor 99.61%
    BIX 02565 is a potent ribosomal S6 kinase 2 (RSK2) inhibitor with IC50 of 1.1 nM.
  • HY-52101
    CMK
    		Inhibitor 99.64%
    CMK is a RSK2 kinase inhibitor which exhibits similar potency but less chemical stability compared with FMK.
  • HY-12185
    BRD7389
    		Inhibitor 99.06%
    BRD7389 is a specific RSK family kinase inhibitor with IC50s of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively. BRD7389 is a small-molecule inducer of insulin expression in pancreatic α-cells.
  • HY-52101C
    FMK-MEA
    		Inhibitor 99.40%
    FMK-MEA is a potent and selective p90 Ribosomal S6 Kinase (RSK) inhibitor.
  • HY-173406
    RSK-IN-2
    		Inhibitor 99.32%
    RSK-IN-2 (Compound 3e) is a RSK inhibitor, with IC50 s of 37.89 nM (RSK2), 30.78 nM (RSK1), 20.51 nM (RSK3), 91.28 nM (RSK4). RSK-IN-2 inhibits tumor cell proliferation, induces apoptosis and causes cell cycle arrest in the G2/M phase.
  • HY-150643
    RSK2-IN-2
    		Inhibitor
    RSK2-IN-2 (Compound 25) is a reversible covalent inhibitor of the RPS6KA3 (RSK2) kinase. RSK2-IN-2 is also described to inhibit MSK1, MSK2 and RSK3.
  • HY-178029
    RSK2/TOP2-IN-1
    		Inhibitor
    RSK2/TOP2-IN-1 is a RSK2/TOP2 dual inhibitor. RSK2/TOP2-IN-1 targets key tumor progression enzymes including ribosomal S6 kinase 2 and topoisomerases IIα/IIβ. RSK2/TOP2-IN-1 shows selectivity index > 2 against all squamous cell carcinoma (SCC) cell lines. RSK2/TOP2-IN-1 can induce cell apoptosis, autophagy and ROS production. RSK2/TOP2-IN-1 can be used for the research of cancer, such as squamous cell carcinoma.
  • HY-150717
    RSK2-IN-3
    		Inhibitor
    RSK2-IN-3 (Compound 26) is a reversible covalent inhibitor of the RPS6KA3 (RSK2) kinase.
Cat. No. Product Name / Synonyms Application Reactivity