rsk

RSK-IN-1 (compound 7d) shows anti-tumor activity. RSK-IN-1 is an inhibitor of RSK that inhibits the phosphorylation of YB-1 [1].

RSK2-IN-3 (Compound 26) is a covalent, reversible inhibitor of RPS6KA3 (RSK2) kinase.

RSK2-IN-2 (Compound 25) is a reversible covalent inhibitor of the RPS6KA3 ( RSK2 ) kinase which also inhibits MSK1, MSK2, and RSK3 [1].

RSK4-IN-1 is a compound exhibiting potent inhibition of RSK4, demonstrated by an IC50 value of 9.5 nM.

Forskolin (Coleonol) is a natural product, an adenylate cyclase activator (EC50=0.5 μM). Forskolin increases cAMP levels, activates PXR and FXR, and induces autophagy. Forskolin produces positive inotropic effects in the heart, and has platelet anticoagulant and antihypertensive effects.

BI-D1870 is a cell-permeable, ATP-competitive inhibitor of ribosomal S6 kinases (RSKs; IC50s: 31 24 18 15 nM for RSK1 2 3 4).

Forskolin is known to elevate intracellular cAMP levels.

FMK-MEA is a potent and selective p90 Ribosomal S6 Kinase (RSK) inhibitor.

FMK is an irreversible inhibitor of RSK2 kinase.

Deacetylforskolin is a diterpene and a derivative of forskolin that has been found inC. forskohliiand has diverse biological activities.1,2,3,4It activates rat adipocyte adenylyl cyclase (IC50= 20 μM) and inhibits glucose transport in rat adipocyte plasma membranes.2Deactylforskolin (30-1,000 μg/kg) reduces blood pressure in spontaneously hypertensive rats.3It also attenuates hypercapnia-induced impairments in the passive avoidance response in mice.4 1.Gabetta, B., Zini, G., and Danieli, B.Minor Diterpenoids of Coleus forskohliiPhytochemistry28(3)859-862(1989) 2.Joost, H.G., Habberfield, A.D., Simpson, I.A., et al.Activation of adenylate cyclase and inhibition of glucose transport in rat adipocytes by forskolin analogues: structural determinants for distinct sites of actionMol. Pharmacol.33(4)449-453(1988) 3.Bhat, S.V., Dohadwalla, A.N., Bajwa, B.S., et al.The antihypertensive and positive inotropic diterpene forskolin: Effects of structural modifications on its activityJ. Med. Chem.26(4)486-492(1983) 4.McCulloch, A.J., Thomson, T.A., and Deacon, R.Hypoxic amnesia and its reversal with forskolinBiochem. Soc. Trans.17(1)212-213(1988)

Forskolin J is a natural product for research related to life sciences. The catalog number is TN4074 and the CAS number is 81873-08-7.

The compound is an inactive analog of forskolin(an adenylyl cyclase activator).

Isoforskolin is derived from Coleus forskohlii and reduces the secretion of TNF-α, IL-1β, IL-6 and IL-8 in human mononuclear leukocytes. Isoforskolin can be used in studies about the treatment of Lyme arthritis.

GSK-25 maintains good selectivity against a panel of 31 kinases, as well as RSK1 and p70S6K (RSK1 IC50 of 398 nM, p70S6K IC50 of 1000nM), and a dramatically improved P450 profile (>2.2 uM at all isozymes tested).

AD80, a multikinase inhibitor, inhibits RET, RAF, SRCand S6K, with greatly reduced mTOR activity.

Ulixertinib (VRT752271) (BVD-523, VRT752271) is an effective and reversible ERK1/ERK2 inhibitor. The IC50 of Ulixertinib is less than 0.3 nM for ERK2.

Carnosol is an Nrf2 activator, increasing Nrf2 levels and promoting heme oxygenase 1 (HMOX1) expression. It is a ribosomal S6 kinase (RSK2) inhibitor and can be used in gastric cancer-related research with an IC50 value of approximately 5.5 μM.

Quercitrin (3-rhamnosyl quercetin) is a plant-derived flavonoid compound, displays antioxidant and anti-inflammatory activities. Quercitrin can be found in a number of food items such as garden tomato (var. ), German camomile, endive, and kiwi, which makes quercitrin a potential biomarker for the consumption of these food products.

LY-2584702 tosylate salt is a selective, ATP-competitive p70S6K inhibitor, used in trials studying the treatment of cancer.

Eudesmin shows antiinflammatory, neuritogenic, anticonvulsant and sedative effects, the mechanism of eudesmin may be related to up-regulation of GABAA and GAD65 expressions, and anti-apoptosis of neuron the in brain.50 microM (+)-eudesmin can induce neurite outgrowth and enhance nerve growth factor (NGF)-mediated neurite outgrowth from PC12 cells by stimulating up-stream MAPK, PKC and PKA pathways.

BIX 02565 is a potent inhibitor of ribosomal S6 kinase 2 (RSK2, IC50: 1.1 nM).

Bisindolylmaleimide V, a bisindolylmaleimide derivative, is an inactive of a kinase inhibitor.

SL 0101-1 (SL0101) is a selective, efficient, reversible and ATP-competitive inhibitor of p90 ribosomal S6 kinase (RSK) that can permeate cell membranes, with an IC50 value of 89 nM for RSK.SL 0101-1 (SL0101) is also a potent RSK1/2 inhibitor with a Ki value of 1 μM. SL 0101-1 (SL0101) is also a potent RSK1/2 inhibitor with a Ki value of 1 μM.

TAS0612, a novel oral inhibitor of RSK, AKT, and S6K, exhibits broad-spectrum antitumor activity by impeding cell growth [1].

LJI308 is a potent, and pan-RSK (p90 ribosomal S6 kinase) inhibitor with IC50 of 6 nM, 4 nM, and 13 nM for RSK1, RSK2, and RSK3, respectively.

DD1 (HUN85111) is a proteasome inhibitor that induces human myeloid tumor-selective apoptosis.

RMM-46 is a reversible and selective covalent inhibitor for MSK/RSK-family kinases.

Prexasertib dihydrochloride (LY2606368) is an ATP-competitive CHK1 inhibitor (Ki: 0.9 nmol/L). in the cell-free assay, its IC50 values are 8 nM and 9 nM for CHK2 and RSK, respectively.

Sodium salicylate (2-Hydroxybenzoic acid sodium salt), a metabolite of acetylsalicylic acid, can inhibit NF-kB and reduce oxidative stress.

SB-747651A is a potent, ATP-competitive inhibitor of mitogen- and stress-activated kinase 1 (MSK1, IC50 = 11 nM). It targets the N-terminal kinase domain. SB-747651A inhibits MSK1, MSK2, PKA, PKB, RSK and p70S6K activity in cells.

AT13148 is an oral-active and ATP-competitive, multi-AGC kinase inhibitor for Akt1/2/3, p70S6K, PKA, and ROCKI/II.

BRD7389 is an inhibitor of RSK family kinase with IC50s of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively.

PF-4708671 is a cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) .In cell-free assays, PF-4708671(PF4708671) is potent for S6K1(Ki50=20 nM, IC50=160 nM).

LY2584702 is a selective, ATP-competitive p70S6K inhibitor(IC50: 4 nM).

3Ac-SL0101 is a potent RSK-specific inhibitor. It facilitates the development of RSK inhibitors as anti-cancer chemotherapeutic agents.

Pluripotin (SC1) (SC1), which keep embryonic stem cell (ESC) self-renewal, is a dual inhibitor of extracellular signal-regulated kinase 1 (ERK1, MAPK3) and RasGAP.

Ravoxertinib hydrochloride is an orally bioavailable and selective inhibitor for ERK kinase activity (IC50: 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively).

LJH685 is an effective pan-RSK inhibitor for RSK1/2/3 (IC50: 6/5/4 nM).

S6K-18, a highly selective S6K1 inhibitor, inhibits S6K1 with IC50 of 52nM.

CKI-7 is a potent and ATP-competitive inhibitor of casein kinase 1 (CK1; IC50: 6 μM; Ki: 8.5 μM) and a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1), and MSK1.

AT7867 is a potent ATP-competitive inhibitor of Akt1 2 3 and p70S6K PKA with IC50 of 32 nM 17 nM 47 nM and 85 nM 20 nM, respectively; little activity outside the AGC kinase family.