6H05 is a selective, and allosteric inhibitor of oncogenic K-Ras(G12C).

A novel potent MAP3K14 kinase inhibitor with IC50 of 1.8 nM (NIK autophosphorylation).

A novel potent, selective and orally active ASK1 (MAP3K5) inhibitor with pIC50 of 8.3.

A potent, orally-active MEK1/2 inhibitor with IC50 of 10-100 nM.

A potent, selective, CNS penetrant dual leucine zipper kinase (DLK, MAP3K12) inhibitor with Ki of 3 nM.

Acumapimod (BCT197) is an orally active p38 MAP kinase inhibitor, with an IC50 of less than 1 μM for p38α.

APS-2-79 is a novel modulator of KSR-dependent MAPK signalling,KSR2,IC50=120 nM

APS-2-79 is a novel modulator of KSR-dependent MAPK signalling,KSR2,IC50=120 nM

ARS-1323 is a novel inhibitor of mutant K-ras G12C.

ARS-1620 is a covalent compound with high potency and selectivity for KRAS-G12C.

ARS-1630 is the R-conformational atropisomer of ARS-1620, 1,000-fold less potent than ARS-1620 (1.2 ± 0.6 M-1s-1) and thus acts as a unique inactive control compound..

ARS-853 is a selective, covalent inhibitor of KRAS-G12C that inhibits mutant KRAS driven signaling by binding to the GDP bound oncoprotein and preventing activation.

ASK1-IN-1 is an apoptosis signal regulating kinase 1 (ASK1) inhibitor extracted from patent WO2016025474A1, Compound 4.

AX15836 is a highly potent and selective ERK5 inhibitor.

AZ304 is a novel potent, dual BRAF inhibitor targeting the kinase domains of wild type BRAF, V600E mutant BRAF and wild type CRAF with IC50 of 79 nM, 38 nM and 68 nM, respectively.

AZ6197 (AZ-6197) is a potent, selective, reversible inhibitor of ERK1/2 with IC50 of <0.3 nM (ERK2), inhibits pERK/pRSK with IC50 of 12/62 nM in A375 cells, respectively.

AZD-0364 is a potent and selective ERK2 inhibitor extracted from patent WO2017080979A1, compound example 18, has an IC50 of 0.6 nM.

AZD6244 (Selumetinib, ARRY-142886) is highly potent to inhibit MEK1 with IC50 of 14 nM.

AZD8330(ARRY-424704; ARRY-704) is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM.

Balamapimod (MKI-833) is an orally active, reversible Ras/Raf/MEK inhibitor developed for antineoplastic potential..

Belvarafenib is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC50s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv600E and C-RAF respectively.

BI-78D3 is a competitive c-Jun N-terminal kinase (JNK) inhibitor (IC50 = 280 nM) that displays > 100 fold selectivity over p38α and no activity at mTOR and PI-3K.

BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1.

BI-D1870 is a small molecule, specific inhibitor of p90 RSK (ribosomal S6 kinase) isoforms RSK1, RSK2, RSK3 and RSK4, both in vitro and in vivo, with IC50s are 31 nM, 24 nM, 18 nM, 15 nM, respectively.

BIRB 796 (Doramapimod) is a highly selective p38α MAPK inhibitor with Kd of 0.1 nM, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2, ZAP-70, EGFR, HER2, PKA, PKC, PKCα/β/γ.

BIX02188 is a selective inhibitor of MEK5 with IC50 of 4.3 nM, also inhibits ERK5 catalytic activity with IC50 of 810 nM, and does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2.

BIX02189 is a selective inhibitor of MEK5 with IC50 of 1.5 nM, also inhibits ERK5 catalytic activity with IC50 of 810 nM, and does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2.

B-Raf IN 1 is a highlt potent and selective B-Raf inhibitor with IC50 of 24 nM; equipotent against c-Raf (IC50= 25 nM).

B-Raf inhibitor 1 is a potent and selective B-Raf inhibitor with cell IC50s of 0.31 uM and 2 nM for A375 proliferation and A375 p-ERK respectively.

BRAF inhibitor is a potent BRAF inhibitor.

CC-401 is a second generation ATP-competitive anthrapyrazolone c-Jun N terminal kinase (JNK) inhibitor with potential antineoplastic activity.

CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity.

CEP-32496 Hcl is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret, PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2.

CEP-32496 is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret, PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2.

CGP 57380 is a cell-permeable pyrazolo-pyrimidine compound that acts as a selective inhibitor of Mnk1 (IC50 = 2.2 μM) with no inhibitory activity against p38, JNK1, ERK1/2, PKC, or Src-like kinases.

CI-1040 (PD 184352) is an ATP non-competitive MEK1/2 inhibitor with IC50 of 17 nM.

CMK is a RSK2 kinase inhibitor.

Cot inhibitor-2 is a COT/Tpl2 inhibitor.

Dabrafenib (GSK2118436) is a mutant BRAFV600 specific inhibitor with IC50 of 0.8 nM, with 4- and 6-fold less potency against B-Raf(wt) and c-Raf, respectively. Phase 3.

Dabrafenib is an orally bioavailable inhibitor of B-raf (BRAF) protein with potential antineoplastic activity.

DEL-22379 is a water-soluble ERK dimerization inhibitor with IC50 of ∼0.5 μM.

Tomivosertib (eFT-508) is a potent and selective MNK1/2 inhibitor with IC50s of 2.4 nM and 1 nM, respectively. It potentially results in decreased tumor cell proliferation and tumor growth. Tomivosertib (eFT-508) inhibits eIF4E phosphorylation and dramatically downregulates PD-L1 protein abundance.

Fmk is an irreversible ribosomal S6 kinase inhibitor 1/2 inhibitor.

GDC-0879 is a novel potent, selective B-Raf inhibitor for B-RafV600E with IC50 of 0.13 nM.

GDC-0973 is a potent, highly selective inhibitor of mitogen-activated protein kinase kinase, also known as MEK, a serine/threonine kinase that is a component of the RAS/RAF/MEK/ERK pathway.

GNE-3511 is a potent and selective zipper kinase (DLK, MAP3K12) inhibitors.

GNE-495 is a potent and Selective MAP4K4 Inhibitor with IC50 of 3.7 nM.

GW 5074 is a potent, selective and cell-permeable c-Raf1 kinase inhibitor (IC50 = 9 nM); displays ≥ 100-fold selectivity for raf kinase over CDK1, CDK2, c-src, ERK2, MEK, p38, Tie2, VEGFR2 and c-fms.

GW806742X is a novel VEGFR inhibitor.

IQ-1S is a selective JNK3 inhibitor (IC50 values are 390, 360 and 87 nM for JNK1, 2 and 3 respectively).

KBFM123 (KBFM-123) is a small molecule, allosteric inhibitor of GTP-bound form of H-Ras, weakly inhibits the association of H-RasG12V-GppNHp with c-Raf-1 RBD (Kd=10-100 uM).

KO-947 is a small molecule inhibitor of extracellular-signal-regulated kinases 1 and 2 (ERK1/2), as a potential treatment for cancers in which the mitogen activated protein kinase (MAPK) pathway.

KRAS inhibitor C6ME is a small-molecule compound that blocks biochemical and cellular functions of KRASG12V in vitro..

KRAS inhibitor Cmpd2 is a small-molecule compound that blocks biochemical and cellular functions of KRASG12V with IC50 of 0.8 uM in vitro.

K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of oncogenic K-Ras(G12C).

K-Ras-IN-1 is a K-Ras inhibitor, by binding to K-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure.

L-779,450 is a potent, ATP-competitive Raf (Raf kinase) inhibitor (IC50 = 10 nM) that displays > 7, > 30 and > 70-fold selectivity over p38α, GSK3β and Lck respectively.

LGX818 is an orally available mutated BRaf V600E inhibitor(IC50=0.3 nM) with potential antineoplastic activity.

Lifirafenib（BGB-283） is a Novel potent and selective RAF Kinase and EGFR inhibitor.

LJH685 is a selective and potent RSK inhibitor.

LJI308 is a selective and potent RSK inhibitor.

Losmapimod (GW856553X) is a selective, potent, and orally active p38 MAPK inhibitor with pKi of 8.1 and 7.6 for p38α and p38β, respectively. Phase 3.

LXH254 is a potent CRAF inhibitor extracted from patent WO2018051306A1, Compound A. LXH254 also is a potent BRAF inhibitor.

LY2228820 is a novel and potent p38MAPK inhibitor (the IC50 for p38αMAPK and p38βMAPK were 7 nM and 3 nM, respectively).

LY-2584702 is an orally available inhibitor of p70S6K signaling; inhibits p70S6K and prevents phosphorylation of the S6 subunit of ribosomes.

LY3009120 is a potent and selective pan-RAF inhibitor with potential anticancer activity.

LY3214996 is a selective and novel ERK1/2 inhibitor with IC50 of 5 nM for both enzymes in biochemical assays. It potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines.

M2698 is a potent dual-inhibitor of p70S6K and Akt that affects tumor growth in mouse models of cancer and crosses the blood-brain barrier.

ML-098 is an activator of the GTP-binding protein Rab7 (EC50 = 77.6 nM) that demonstrates selectivity against the related GTPases cdc42, Ras, Rab-2A, and Rac1 (EC50s = 588.8, 346.7, 158.5, and 794.3 nM, respectively).

MW-150 is a novel potent, selective, CNS penetrant and orally active inhibitor of p38α MAPK with Ki of 101 nM

MW-150 is a novel potent, selective, CNS penetrant and orally active inhibitor of p38α MAPK with Ki of 101 nM

Necrosulfonamide (NSA) is a very specific and potent necrosis inhibitor with an IC50 less than 0.2 uM.

NQDI-1 is a specific inhibitor of ASK1 (IC50 = 3 μM; Ki = 500 nM) that demonstrates potent selectivity against various serine/threonine and tyrosine protein kinases.

NSC 23766 is a specific inhibitor of the binding and activation of RAC GTPase with IC50 of ~50 μM; does not inhibit the closely related targets, Cdc42 or RhoA.

NSC 23766 is a specific inhibitor of the binding and activation of Rac GTPase.

OTS-514 is a novel TOPK(PDZ binding kinase; PBK) inhibitor. IC50:2.6nM

OTS964 is a novel TOPK(T–lymphokine-activated killer cell–originated protein kinase) inhibitor.

Pamapimod（R-1503）is a novel p38 MAP kinase inhibitor.

Pan-RAS-IN-1 is a pan-Ras inhibitor that disrupts the interaction of Ras proteins and their effectors.

PD 98059 is a selective inhibitor of MEK and blocker of MAPK

PD0325901 (PD325901) is selective and non ATP-competitive MEK inhibitor with IC50 of 0.33 nM.

PD169316 is a potent and selective p38 MAP kinase inhibitor

PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor, binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site.

PF 06260933 is a potent and selective MAP4K4 inhibitor (IC50 value 3.7 nM for MAP4K4 a.k.a. HGK or ZC1) with suitable PK properties in mouse to be used as a tool in an in vivo model of diabetes, vascular inflammation and atherosclerosis.

PF-04880594 is an inhibitor of RAF with IC50 values of 0.19 nM/0.13 nM and 0.39 nM for BRAF/BRAFV599E and c-RAF, respectively.

PLX4032 (Vemurafenib, RG7204, Zelboraf, RO5185426) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM.

PLX4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM, equally potent to c-Raf-1(Y340D and Y341D mutations), 10-fold selectivity for B-RafV600E than wild-type B-Raf.

PLX7904(PB04) is a potent and selective paradox-breaker RAF inhibitor.

Potent, ATP-competitive inhibitor of Raf kinases (IC50 values are 29, 34 and 105 nM For c-Raf1, B-RafV600E and wild-type B-Raf, respectively). Displays selectivity For Raf kinases over a panel of 150 other kinases.

RAF265 (CHIR-265) is a highly selective B-Raf and VEGFR2 inhibitor with IC50 of 3-60 nM and EC50 of 30 nM, including B-Raf, C-Raf and mutant B-Raf.

RAF709 is a novel Raf kinase inhibitor extracted from patent WO2014151616A1, compound example 131, has an IC50 of 0.5 and 1.8 nM for c-Raf and b-Raf, respectively.

RAS inhibitor Abd-7 is a potent RAS-binding compound (Kd=51 nM) that interacts with RAS in cells, prevents RAS-effector interactions and inhibits endogenous RAS-dependent signalling.

RasGRP3 ligand 96 is a potent, selective ligand of Ras guanine-releasing protein 3 (RasGRP3) with Ki of 1.75 nM, showed 73-fold and 45-fold selectivity relative to PKCα and PKCε for in vitro binding activity resepctively.

Refametinib (RDEA119, Bay 86-9766) is a potent, ATP non-competitive and highly selective inhibitor of MEK1 and MEK2 with IC50 of 19 nM and 47 nM, respectively.

RO5126766(CH5126766) is a Raf/MEK dual kinase inhibitor.

RWJ67657 is a selective p38α and p38β inhibitor (IC50 values are 1 and 11 μM respectively) that displays no activity at p38γ, p38δ and a range of other kinases.

SB 202190 is a pyridinyl imidazole that inhibits the p38 pathway.

SB 239063 is a potent and selective p38 MAPK inhibitor (IC50 = 44 nM for p38α). SB 239063 displays > 220-fold selectivity over ERK, JNK1 and other kinases; ~ 3-fold more selective than SB 203580.

SB203580 is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM and blocks PKB phosphorylation with IC50 of 3-5 μM.

SB590885 is a potent B-Raf inhibitor with Ki of 0.16 nM, 11-fold greater selectivity for B-Raf over c-Raf, no inhibition to other human kinases.

SC1(Pluripotin) is a sustainer of mES self-renewal and ERK 1 inhibitor

SCH772984 is a novel, specific inhibitor of ERK1/2 with IC50 of 4 nM and 1 nM, respectively.

SD-06 is a p38 MAP kinase inhibitor; inhibits p38α with an IC50 value of 170 nM and inhibits LPS-stimulated TNF-release in rats (83% inhibition at 1mg/kg, po).

Selective ERK inhibitor (IC50 values are 0.14 and 0.31 μM for ERK2 and ERK1 respectively). Displays 30-fold selectivity for ERK over p38α (IC50 = 10 μM); displays no activity against human recombinant MEK1, MKK4, IKKα, PKCα, Src, Syc and PDGFα.

SKF-86002 is a potent inhibitor of p38 MAP kinase wit IC50 of 0.5-1 uM; inhibits LPS-induced IL-1 and TNF-α production in human monocytes (IC50 = 1 μM).

SL 0101-1 is a selective inhibitor of p90 Rsk (ribosomal S6 kinase) (IC50 = 89 nM for Rsk-2).

Sodium Tauroursodeoxycholate (TUDC) is a water soluble bile salt, used for the treatment of gallstones and liver cirrhosis.

Sorafenib Tosylate (Bay 43-9006, Nexavar) is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively.

Sorafenib(BAY 43-9006) is a potent inhibitor of Raf-1 with IC50 values of 6 nM, 22 nM and 90 nM for Raf-1, B-Raf, and VEGFR2 respectively, BAY 43-9006 suppresses both wild-type and V599E mutant BRAF activity in vitro.

SOS1 activator 17 is a small molecule activator of guanine nucleotide exchange factor SOS1 with EC50 of 0.8 uM, modulates RAS signaling in vitro.

SP600125 is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM, respectively.

TA-02 induces cardiomyocyte differentiation from human embryonic stem cells following mesoderm induction. Potently inhibits p38α, CK1δ and CK1ε (IC50 values are 20, 32 and 32 nM respectively).

TAK-632 is a selective pan-RAF kinase inhibitor with IC50 values of 2.4/1.4 nM for BRAF V600E/c-RAF; > 60 fold selectivity over VEGFR.

TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1.

TAK-733 is a potent and selective MEK allosteric site inhibitor for MEK1 with IC50 of 3.2 nM, inactive to Abl1, AKT3, c-RAF, CamK1, CDK2, c-Met, etc.

TCASK10 is a potent, highly specific inhibitor of ASK1 with IC50 of 14 nM, 30-fold selectivity over ASK2 (IC50=510 nM) and no activity against MEKK1, TAK1, IKKβ, ERK1, JNK1, p38α, GSK-3β, PKCθ and B-raf.

Trametinib is a highly specific and potent MEK1 and MEK2 inhibitor with IC50 of 0.92 nM and 1.8 nM, respectively.

U0126-EtOH(U-0126) is a highly selective inhibitor of MEK1/2 with IC50 of 0.07 μM/0.06 μM, 100-fold higher affinity for ΔN3-S218E/S222D MEK than PD098059.

URMC-099 is an orally bioavailable, brain penetrant mixed lineage kinase (MLK) inhibitor with IC50 of 19 nM, 42 nM, 14 nM, and 150 nM, for MLK1, MLK2, MLK3, and DLK, respectively, and also inhibits LRRK2 activity with IC50 of 11 nM.

Vacquinol-1 is an activator of MKK4-dependent macropinocytotic cell death in glioblastoma cells.

VX-11e is a potent, selective, and orally bioavailable inhibitor of ERK (Extracellular Signal-Regulated Kinase); antitumor agent.

VX-702 is a highly selective inhibitor of p38 MAPKα with IC50 of 4-20 nM.

VX-745 is a potent and selective inhibitor of p38α MAPK and p38β MAPK with IC50 of 10 nM and 220 nM, respectively.

ZCL278 is a Cdc42 small molecule modulator that directly binds to Cdc42 (Kd=11.4 uM) and inhibits Cdc42-intersectin interaction.

ZM 336372 is a potent and selective c-Raf inhibitor with IC50 of 70 nM, 10-fold selectivity over B-RAF, no inhibition to PKA/B/C, AMPK, p70S6, etc.

AS703026(Pimasertib) is a highly selective, potent, ATP non-competitive allosteric inhibitor of MEK1/2 with IC50 of 5 nM-2 μM in MM cell lines.

BAY-885 is a highly potent, selective ERK5 (MAPK7) inhibitor with IC50 of 40 nM.

JNK-IN-8 is a potent and irreversible JNK inhibitor that inhibits the phosphorylation of c-Jun.

RO4987655(CH-4987655) is an orally active small molecule, targeting mitogen-activated protein kinase kinase 1 (MAP2K1/MEK1 IC50=5.2 nM), with potential antineoplastic activity.

SB-242235 is a potent and selective p38 MAP kinase inhibitor with IC50 of 1.0 uM.

Selonsertib（GS-4997）is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities.

MRTX849(Adagrasib) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. MRTX849 covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bou

Rp-cAMPS triethylammonium salt is an analog of cAMP which acts as a potent, competitive and cell-permeable antagonist of cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 6.05 µM and 9.75 µM, respectively). Rp-cAMPS triethylammonium salt is resistant to hydrolysis by phosphodiesterases.

SU3327 is a potent, selective and substrate-competitive JNK inhibitor with an IC50 of 0.7 μM. SU3327 also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC50 of 239 nM. SU3327 shows less active against p38α and Akt kinase.

Muramyl dipeptide (MDP) is a synthetic immunoreactive peptide, consisting of N-acetyl muramic acid attached to a short amino acid chain of L-Ala-D-isoGln. Muramyl dipeptide is an inducer of bone formation through induction of Runx2. Muramyl dipeptide directly enhances osteoblast differentiation by up-regulating Runx2 gene expression through MAPK pathways. Muramyl dipeptide indirectly attenuates osteoclast differentiation through a decreased RANKL/OPG ratio.

RAS GTPase inhibitor 1 (example 51) is a RAS GTPase inhibitor with anti-tumor activity, extracted from patent WO2018212774A1. RAS GTPase inhibitor 1 (example 51) exhibits an EC50 less than 1 μM for at least one nucleotide exchange and an IC50 less than 1 μM in H727 cells.

ERK-IN-2 is a potent, highly seletive and orally active ERK2 inhibitor probe with an IC50 value of 1.8 nM. ERK-IN-2 might lead to off-target toxicity and/or off-target activity at dose >10 μM.

SR-318 is a potent and highly selective p38 MAP kinase inhibitor with IC50s of 5 nM, 32nM and 6.11 μM for p38α, p38βand p38α/β, respectively. SR-318 potently inhibits the TNF-α release in whole blood with an IC50 of 283 nM. SR-318 has anti-cancer and anti-inflammatory activity.

Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.

BI-3406 (compound I-6) is a potent, selective and orally active inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with IC50 of 6 nM. BI-3406 reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. BI-3406 exhib

Sorafenib D3 (Bay 43-9006 D3) is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 15 nM, 20 nM and 22 nM for Raf-1, mVEGFR-2, mVEGFR-3 and B-RAF, respectively.

Rp-cAMPS, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 μM and 4.5 μM, respectively) antagonist. Rp-cAMPS is resistant to hydrolysis by phosphodiesterases.

Sp-cAMPS, a cAMP analog, is potent activator of cAMP-dependent PKA I 和 PKA II. Sp-cAMPS is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 μM. Sp-cAMPS binds the PDE10 GAF domain with an EC50 of 40 μM.

Sp-cAMPS sodium salt, a cAMP analog, is potent activator of cAMP-dependent PKA I 和 PKA II. Sp-cAMPS sodium salt is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 μM. Sp-cAMPS sodium salt binds the PDE10 GAF domain with an EC50 of 40 μM.

Rp-cAMPS sodium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 μM and 4.5 μM, respectively) antagonist. Rp-cAMPS sodium salt is resistant to hydrolysis by phosphodiesterases.

IQ-3 is a specific inhibitor of the c-Jun N-terminal kinase (JNK) family, with preference for JNK3. IQ-3 exhibits Kd values of 0.24 μM, 0.29 μM and 0.066 μM for JNK1, JNK2 and JNK3, respectively.

Rp-8-CPT-cAMPS sodium, a cAMP analog, is a potent and competitive antagonist of cAMP-induced activation of cAMP-dependent PKA I and II. Rp-8-CPT-cAMPS sodium preferentially selects site A of RI compares to site A of RII and site B of RII compares to site B of RI.

Rp-8-CPT-cAMPS, a cAMP analog, is a potent and competitive antagonist of cAMP-induced activation of cAMP-dependent PKA I and II. Rp-8-CPT-cAMPS preferentially selects site A of RI compares to site A of RII and site B of RII compares to site B of RI.

Sp-8-CPT-cAMPS, a cAMP analog, is a potent and selective activator of the cAMP-dependent protein kinas A (PKA I and PKA II). Sp-8-CPT-cAMPS selects site A of RI compares to site A of RII by 153-fold and site B of RII compares to site B of RI by 59-fold.

APS6-45 is an orally active tumor-calibrated inhibitor (TCI). APS6-45 inhibits RAS/MAPK signaling and exhibits antitumor activity.

ERK1/2 inhibitor 2 (Example 1) is a potent dual ERK1/2 inhibitor. ERK1/2 inhibitor 2 has anti-cancer activity.

PD0325901-O-C2-dioxolane has main portion of MEK inhibitor PD0325901. PD0325901-O-C2-dioxolane and a ligand of VHL or CRBN E3 ligase can be used in the synthesis of MEK1/2 degrader.

CID44216842 (Cdc42-IN-1) is a potent Cdc42-selective guanine nucleotide binding lead inhibitor. The EC50s for Cdc42 WT and Cdc42Q61L mutant are 1.0 and 1.2 μM in GTP binding assay, respectively. The EC50s for Cdc42 WT and Cdc42Q61L mutant are 0.3 and 0.5 μM in GDP binding assay, respectively. Use as a molecular probe.

AZA1 is a potent dual inhibitor of Rac1 and Cdc42. AZA1 induces prostate cancer cells apoptosis and inhibits prostate cancer cells proliferation, migration and invasion.

KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells.

Eudesmin ((-)-Eudesmin) impairs adipogenic differentiation via inhibition of S6K1 signaling pathway. Eudesmin possesses diverse therapeutic effects, including anti-tumor, anti-inflammatory, and anti-bacterial activities.

(-)-Zuonin A (D-Epigalbacin), a naturally occurring lignin, is a potent, selective JNKs inhibitor, with IC50s of 1.7 μM, 2.9 μM and 1.74 μM for JNK1, JNK2 and JNK3, respectively.

PKI(5-24) is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor.

PKI(5-24) TFA is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) TFA corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor.

JIP-1(153-163) (TI-JIP) is a peptide inhibitor of c-JNK, based on residues 153-163 of JNK-interacting protein-1 (JIP-1) (Modifications: Phe-11 = C-terminal amide).

JIP-1(153-163) TFA (TI-JIP TFA) is a peptide inhibitor of c-JNK, based on residues 153-163 of JNK-interacting protein-1 (JIP-1) (Modifications: Phe-11 = C-terminal amide).

PKA Inhibitor Fragment (6-22) amide is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide can significantly reverse low-level morphine antinociceptive tolerance in mice.

PKA Inhibitor Fragment (6-22) amide TFA is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide TFA can significantly reverse low-level morphine antinociceptive tolerance in mice.

PKI 14-22 amide,myristoylated is a potent cAMP-dependent PKA inhibitor. PKI 14-22 amide,myristoylated reduces the IgG-mediated phagocytic response and also inhibits neutrophil adhesion.

PKI 14-22 amide,myristoylated TFA is a potent cAMP-dependent PKA inhibitor. PKI 14-22 amide,myristoylated TFA reduces the IgG-mediated phagocytic response and also inhibits neutrophil adhesion.

Rac1 Inhibitor W56 is a peptide comprising residues 45-60 of the guanine nucleotide exchange factor (GEF) recognition/activation site of Rac1. Rac1 Inhibitor W56 selectively inhibits Rac1 interaction with Rac1-specific GEFs TrioN, GEF-H1 and Tiam1.

Rac1 Inhibitor W56 TFA is a peptide comprising residues 45-60 of the guanine nucleotide exchange factor (GEF) recognition/activation site of Rac1. Rac1 Inhibitor W56 TFA selectively inhibits Rac1 interaction with Rac1-specific GEFs TrioN, GEF-H1 and Tiam1.

Malantide TFA is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide TFA is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts. Malantide TFA is also an efficient substrate for PKC with a Km of 16 μM.

OVA-E1 peptide, is an antagonist variant of SIINFEKL [OVA (257-264). OVA-E1 peptide, activates the p38 and JNK cascades similarly in mutant and wild-type thymocytes.

OVA-E1 peptide TFA, is an antagonist variant of SIINFEKL [OVA (257-264). OVA-E1 peptide, activates the p38 and JNK cascades similarly in mutant and wild-type thymocytes.

Pamoic acid disodium is a potent GPR35 agonist with an EC50 value of 79 nM. Pamoic acid disodium induces GPR35 internalization and activates ERK1/2 with EC50 values of 22 nM and 65 nM, respectively. Pamoic acid disodium potently recruits β-arrestin2 to GPR35 and has an antinociceptive effect.

ERK-IN-3 is a potent and oral of ERK. ERK-IN-3 inhibits ERK1/2 with low single-digit nM IC50 values. ERK-IN-3 has the potential to be used to study cancers driven by RAS mutations.

ML786 dihydrochloride potent and orally bioavailable Raf, with IC50s of 2.1, 4.2, and 2.5 nM for V600EΔB-Raf, wt B-Raf, and C-Raf, respectively. ML786 dihydrochloride also inhibits Abl-1, DDR2, EPHA2, KDR, and RET (IC50=<0.5, 7.0, 11, 6.2, 0.8 nM). ML786 dihydrochloride can be used for the research of cancers.

Antineoplaston A10 is a naturally occurring substance in the human body that that can be potentially used for the treatment of glioma, lymphoma, astrocytoma and breast cancer. The main ingredient active of antineoplaston A10 (Phenylacetylglutamine, PG) inhibits RAS and promotes apoptosis.

GW806742X hydrochloride, an ATP mimetic and a potent MLKL (Mixed Lineage Kinase Domain-Like protein) inhibitor, binds the MLKL pseudokinase domain with a Kd of 9.3 μM. GW806742X hydrochloride has activity against VEGFR2 (IC50=2 nM). GW806742X hydrochlorid

CC-90001 is a potent, selective and orally active inhibitor of c-Jun N-terminal kinase (JNK). CC-90001 shows 12.9-fold selectivity for JNK1 over JNK2 in a cell-based model. CC-90001 can be used for the research of idiopathic pulmonary fibrosis.

p38α inhibitor 2 is a highly potent and selective p38α MAPK inhibitor, with a pIC50 of 9.6. p38α inhibitor 2 inhibits the hERG ion channel (IC50=27 μM) and shows a promising selectivity profile when tested in a panel of 51 other protein kinases (<30% inhibition at 10 μM concentration) and a panel of 141 other biological targets.

RAS/RAS-RAF-IN-1 is a potent RAS and RAS-RAF inhibitor. RAS/RAS-RAF-IN-1 has a KD of 5.0 μΜ-15 μΜ for cyclophilin A (CYPA) binding affinity. RAS/RAS-RAF-IN-1 has antitumor activity.

KRAS inhibitor-10 selectively and effectively inhibit RAS proteins, and particularly KRAS proteins. KRAS inhibitor-10 is an orally active anti-cancer agent and can be used for cancer research, such as pancreatic cancer, breast cancer, multiple myeloma, leukemia and lung cancer. KRAS inhibitor-10 is a tetrahydroisoquinoline compound (compound 11) extracted from patent WO2021005165 A1.

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.

(E)-Osmundacetone is the isomer of Osmundacetone. Osmundacetone significantly suppresses the phosphorylation of MAPKs, including JNK, ERK, and p38 kinases. Osmundacetone has a neuroprotective effect against oxidative stress.

CCG-100602 is a specific inhibitor of myocardin-related transcription factor A/serum response factor (MRTF-A/SRF) signaling. CCG-100602 specifically block MRTF-A nuclear localization and thus inhibit the fibrogenic transcription factor SRF.

Andrograpanin, a bioactive compound from Andrographis paniculata, exhibits anti-inflammatory and anti-infectious properties.

Atrovastatin-PEG3-FITC (compound S31) is a KRAS-PDEδ interaction inhibitor. Atrovastatin-PEG3-FITC acts as a ligand in fluorescence anisotropy assay.

SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS.

Gypenoside L is a saponin that can be found in Gynostemma pentaphyllum. Gypenoside L increases the SA-β-galactosidase activity, promotes the production of senescence-associated secretory cytokines. Gypenoside L also can activate p38 and ERK MAPK pathways and NF-κB pathway to induce senescence. Gypenoside L exhibits anti-tumor and anti-inflammatory activities.

StRIP16, bioavailable StRIP3 analogue, is a double-stapled peptide which can bind to Rab8a GTPase, with a Kd of 12.7 μM.

JTP10-△-TATi TFA is a selective JNK2 peptide inhibitor, with an IC50 of 92 nM, exhibiting 10-fold selectivity for JNK2 over JNK1 and JNK3.

AMG-548 hydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 hydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM). AMG-548 hydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε.

HPK1-IN-7 is a potent, orally active HPK1 (hematopoietic progenitor kinase 1, MAP4K1) inhibitor (IC50=2.6 nM) with excellent family and kinome selectivity. HPK1-IN-7 shows selectivity against IRAK4 (59 nM) and GLK (140 nM). HPK1-IN-7 shows robust efficacy against MC38 syngeneic tumor model in combination with anti-PD1.

CC-99677 is a potent, covalent, and irreversible inhibitor of the mitogen-activated protein (MAP) kinase-activated protein kinase-2 (MK2) pathway in both biochemical (IC50=156.3 nM) and cell based assays (EC50=89 nM).

SKF-86002 dihydrochloride is an orally active p38 MAPK inhibitor, with anti-inflammatory, anti-arthritic and analgesic activities. SKF-86002 dihydrochloride inhibits lipopolysaccharide (LPS)-stimulate human monocyte IL-1 and TNF-α production (IC50 = 1 μM). SKF-86002 dihydrochloride inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid.

MRTX849 acid, a derivative of MRTX849, can be used in the synthesis of PROTAC LC-2. LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C (DC50s between 0.25 and 0.76 μM).

Edaxeterkib is a potent extracellular signal-​regulated kinase (ERK) inhibitor for the research of cancer.

PKA-IN-1 is a potent and selective cyclic AMP-dependent protein kinase (PKA) catalytic subunit (cAK) inhibitor with an IC50 of 0.03 μM.

8-CPT-Cyclic AMP (8-CPT-cAMP) sodium is a selective activator of cyclic AMP-dependent protein kinase (PKA). 8-CPT-Cyclic AMP sodium is also a potent inhibitor of the cyclic GMP-specific phosphodiesterase (PDE VA) with an IC50 of 0.9 μM. 8-CPT-Cyclic AMP sodium also inhibits PDE III and PDE IV with IC50Epac and is a potent Epac activator.

MRTX1133 is a highly selective, first-in-class inhibitor of KRAS G12D. MRTX1133 targets the KRAS G12D protein in both active and inactive states. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells.

JDQ443 (example 1a) is a covalent KRAS G12C inhibitor (extracted from patent WO2021120890A1).

Zunsemetinib (CDD-450) is an orally active and selective p38α mitogen-activated protein kinase-activated protein kinase 2 (MK2) pathway inhibitor. Zunsemetinib can be used for the research of immuno-inflammatory diseases.

Zapnometinib (PD0184264), an active metabolite of CI-1040, is a MEK inhibitor, with an IC50 of 5.7 nM. Zapnometinib exhibits antiviral activity against influenza virus and antibacterial activities.