MAPK

N-Butyl α-D-fructofuranoside, extracted from the root barks of Ulmus davidiana var.

GAGGVGKSAL, a wild-type KRAS G12D 10mer peptide, serves as an immunogenic neoantigen in cancer immunotherapy research [1].

<p>MLKL-IN-2 is an MLKL inhibitor with potential tumorigenic activity for the study of cellular necrosis-related diseases.</p>

KRAS inhibitor-24 (compound 115c), a pyrido-pyridine class KRAS inhibitor, exhibits potent activity against KRas G12V, KRas WT, and KRas G12R, with IC50 values all below 100 nM.

<p>PPM-3, a selective PROTAC ERK5 degrader, exhibits a potent inhibitory concentration (IC 50) of 62.4 nM.</p>

Cot inhibitor-1 hydrochloride blocks TPL-2 kinase (IC50=28nM) and TNF-α synthesis (IC50=5.7nM) in human blood.

Endothelin-1 (1-31) (Human) TFA, a potent vasoconstrictor and hypertensive agent, originates from the chymase-mediated selective hydrolysis of big ET-1 [1].

<p>PROTAC K-Ras Degrader-4 is a molecule designed to selectively degrade oncogenic K-Ras mutants, a novel strategy for cancer research.</p>

<p>LYMTAC-2 is a lysosome-targeting chimera (LYMTAC) developed to degrade membrane-associated proteins through lysosomal membrane proteins (LMP) such as RNF152, LAPTM4a, and LAPTM5. It forms a ternary complex with target proteins like KRASG12D, facilitating their relocation to lysosomes and resulting in ubiquitin-dependent degradation. This compound has potential for studying membrane protein regulation and devising strategies to counter resistance in KRAS-driven signaling pathways.</p>

Pan-RAS-IN-6 (compound 24) serves as a DUSP6 inhibitor, effectively reducing MAPK activation in the NCI-H1373-Luc model (DUSP6). It concurrently exhibits notable tumor growth inhibition and regression in the NSCLC brain metastasis mouse model. The compound displays high selectivity and potent inhibitory effects, particularly on KRAS mutation-associated signaling pathways. It demonstrates varied inhibitory activities against distinct KRAS mutants and their interacting proteins. The IC 50 values for KRAS G12C, G12D, and G12V are 1.3 nM, 4.7 nM, and 0.3 nM, respectively.

<p>NEK7-IN-2 (compound 23) is a potent inhibitor of the NLRP3-NEK7 interaction. It enhances the thermal stability of NEK7 and modulates the assembly of the NLRP3 inflammasome. Additionally, NEK7-IN-2 inhibits the release of IL-1β.</p>

Debromohymenialdisine is a natural product for research related to life sciences. The catalog number is T35596 and the CAS number is 75593-17-8.

Natsudaidain is a useful organic compound for research related to life sciences and the catalog number is T124974.

Antidesmone from Ajuga decumbens inhibits acute lung injury by modulating MAPK and NF-κB.

JNK-IN-12 (compound P2) is a mitochondrial-targeted JNK inhibitor with an IC50 value of 66.3 nM, comprising a mitochondrial-specific cell-penetrating peptide

Esculin sesquihydrate, a coumarin glucoside with fluorescent properties and a constituent of ash bark, improves cognitive deficits associated with experimental

PROTAC MEK1 Degrader-1, a targeted protein degradation agent, combines a MEK1 inhibitor with a von Hippel-Lindau ligand to effectively inhibit ERK1/2

KRAS inhibitor-33 (compound 115a) is a pyrido[2,3-d]pyrimidine derivative that serves as an effective inhibitor of KRAS, exhibiting an IC50 value of ≤ 100nM.

NEK7-IN-1 (Compound I-15) is an inhibitor of NIMA-related kinase 7 (NEK7) with an IC50 of less than 100 nM. It also effectively inhibits the release of IL-1β, exhibiting an IC50 of less than 50 nM.

MAP4K4-IN-6 (Compound 15f) is a MAP4K4 inhibitor with an IC50 of 80 nM. It reduces the phosphorylation of c-Jun and exhibits neuroprotective effects. Additionally, MAP4K4-IN-6 enhances the vitality of motor neurons and can be utilized in the study of amyotrophic lateral sclerosis (ALS).

<p>Ro-3201195 is a novel orally available p38 MAPK inhibitor with high selectivity.</p>

BI1701963 is an orally effective inhibitor that targets the SOS1 and KRAS interaction, specifically inhibiting the activation of KRAS by blocking its GTP loading. This compound is utilized in cancer research to explore potential therapeutic effects against KRAS-driven malignancies.

Antimicrobial agent-21 is a potent mitogen activated protein kinase inhibitor with antibacterial, anti-inflammatory and antitumor activity for the treatment of

TUS-007, a non-proteasome inhibiting CANDDY, is an oral KRAS G12D/V degrader for cell-free chemical knockdown and tumor suppression.

Scio-323是一种可口服的 p38丝裂原活化蛋白（MAPK）激酶抑制剂。

CHPG hydrochloride is a selective agonist of mGluR5.

JNK-IN-18 (compound 23b) is a potent inhibitor of JNK1, boasting an IC50 of 2 nM. It demonstrates superior efficacy when compared to its IC50 values of 125 nM for JNK2 and 98 nM for BRAF(V600E).

BAY-6035 is an inhibitor of SET and MYND domain-containing protein 3 (SMYD3). BAY-6035 has more than 100-fold selectivity over other histone methyltransferases.

The compound p38α inhibitor5 (compound 1) is a PROTAC-type ligand that targets p38 and is utilized in the synthesis of NR-11c.

IQ-1S is an inhibitor of NF-κB/activating protein 1 (AP-1) with an IC50 of 1.8 μM. It exhibits high binding affinity to all three JNKs, with Kd values for JNK3, JNK2, and JNK1 being 87 nM, 360 nM, and 390 nM, respectively.

<p>PROTAC PD-L1 degrader-2, an orally administered compound, targets HPK1 and boosts the efficacy of PD-L1 antibody therapy.</p>

<p>Z16078526 promotes Ucp1, p38 MAPK, lipolysis, thermogenic genes, and mitochondrial activity in mouse brown adipocytes.</p>

<p>KRAS G12D inhibitor 6 is an efficacious compound that effectively inhibits KRAS G12D.</p>

PROTACHPK1 Degrader-2 (compound 3) is a PROTAC degrader of HPK1, exhibiting a DC50 of 23 nM in human PBMCs. This compound plays a crucial role in cancer research.

<p>NecroX-2 is a cell-permeable necrosis inhibitor with antioxidant properties. NecroX-2 selectively suppresses necrotic cell death triggered by oxidative stress. NecroX-2 does not confer protection against apoptosis induced by staurosporine or etoposide but shows protective effects under conditions such as cold shock, hypoxia, and oxidative stress in vitro.</p>

Potent KRAS G12D inhibitor 15 targets cancer, potential for disease research. (WO2022042630A1, compound 243)

<p>RP03707 is a PROTAC degrader of KRASG12D.</p>

PROTAC SOS1 Degrader-4 (compound 10) is a potent degrader of SOS1 and exhibits antiproliferative activity [1].

MLKL-IN-7 (compound 9) is an MLKL inhibitor that exhibits anti-necrotic activity in HT-29 cells, with an IC50 value of 148.4 nM.

<p>HPK1-IN-4 is an HPK1 (MAPK41) inhibitor with an IC 50 of 0.061 nM. HPK1-IN-4 is often used as a preclinical immunotherapy tool compound.</p>

<p>A unique collection of 2720 kinase inhibitors/regulators for high throughput screening and high content screening for drug discovery in kinase related diseases;</p>

Pan-KRAS-IN-10 (Compound 58) acts as an inhibitor of the human tumor mutant gene KRAS. It suppresses the proliferation of KRAS mutant cells, specifically AsPC-1 (G12D mutant) and SW480 (G12V mutant), with IC50 values of 0.7 and 0.24 nM, respectively.

RTIL 13 inhibits dynamin GTPase (IC50: 2.3 μM), targets its lipid binding domain, and suppresses endocytosis (IC50: 9.3 & 7.1 μM).

SIAIS562055, a potent cereblon-based SOS1PROTAC, exhibits a dissociation constant (Kd) of 95.9 nM. It effectively degrades SOS1 and inhibits the downstream ERK pathway. SIAIS562055 disrupts the interaction between KRASG12C or KRASG12D and SOS1, with IC50 values of 95.7 nM and 134.5 nM, respectively. This compound demonstrates strong anticancer activity.

A unique collection of 365 compounds targeting MAPK signaling for drug discovery in MAPK related diseases;

<p>OVA-E1 peptide TFA activates the p38 and JNK cascades similarly in mutant and wild-type thymocytes.</p>

<p>HPK1-IN-53 (compound 3a) is the most potent inhibitor of HPK1, exhibiting an IC50 value of 48 nM.</p>

<p>HPK1-IN-54 (Compound 16) is a potent inhibitor of HPK1 (hematopoietic progenitor kinase 1), enhancing T cell activation and proliferation by blocking HPK1 activity to exert antitumor effects. It has an IC50 of 2.67 nM for HPK1, showing excellent selectivity over the MAP4K family (&gt;100-fold) and other selected kinases (&gt;300-fold). HPK1-IN-54 exhibits moderate in vivo clearance and reasonable oral exposure in both mice and rats. Additionally, in the CT26 mouse colon cancer model, HPK1-IN-54 demonstrates significant antitumor activity and shows a synergistic effect when combined with anti-PD-1 therapy. HPK1-IN-54 holds promise for research in the field of immunology.</p>

<p>KRAS G12D inhibitor 7, is a highly potent inhibitor specifically targeting KRAS G12D.</p>

<p>Ras Inhibitory Peptide acetate, involved in cancer-related Ras signaling.</p>

HS220 is an inhibitor of TAK1 which plays a key role in the signaling pathways of inflammation and cell survival.

<p>Pan-RAS-IN-5 (compound 7A) is a molecular glue that facilitates the formation of a ternary complex with cyclophilin A (CYPA) and RAS(ON) protein. This complex inhibits the binding of RAF downstream of RAS, demonstrating antitumor activity.</p>

<p>N-Acetylgalactosaminyltransferase 4 (GALNT4) is a glycosyltransferase capable of inhibiting the activation of ASK1. It functions by directly binding to ASK1, preventing N-terminal dimerization and subsequent phosphorylation. This interaction leads to significant inactivation of downstream JNK/p38 and NF-κB signaling, thereby improving the prognosis of liver surgery.</p>

(R)-5-hydroxy isoindolin-1-one is an RAS protein inhibitor with antiproliferative and antitumor properties.

JNK2-IN-1 (Compound J27), a selective JNK2 inhibitor with a dissociation constant (Kd) of 79.2 µM, exhibits anti-inflammatory effects by attenuating TNF-α and

MEK1/2-IN-3 (Compound M15) is an inhibitor of MEK1, with an IC50 value of 10.29 nM. It effectively suppresses tumor cell proliferation and migration, induces apoptosis, and exhibits good liver microsomal stability. MEK1/2-IN-3 is applicable in the study of solid tumors.

HSND80 (Compound 1) is an orally active MNK/p70S6K inhibitor, exhibiting a Kd value of 44 nM for MNK1 and 4 nM for MNK2. The residence time of HSND80 on MNK1 and MNK2 is 45 minutes and 58 minutes, respectively. HSND80 effectively inhibits non-small cell lung cancer (NSCLC) both in vitro and in vivo, and suppresses the growth of triple-negative breast cancer (TNBC) cells in vitro.

Anti-osteoporosis agent-8 (Compound 4aa) is a RANKL inhibitor, capable of preventing RANKL-induced osteoclastogenesis and osteoclast differentiation, with an IC50 of 2.41 μM. Furthermore, Anti-osteoporosis agent-8 has been shown to mitigate bone loss in an ovariectomized (OVX) mouse model.

<p>KRAS G12C Inhibitor 60 (compound 23), a selective inhibitor targeting the Kras-G12C mutation, is utilized in the investigation of lung, colorectal, and</p>

<p>SOS1-IN-18 (Compound 8) is an inhibitor of the Son of Sevenless 1 protein (SOS1) with a dissociation constant (KD) of 2.6 nM. It disrupts the SOS1-KRAS G12C interaction with an IC50 of 3.4 nM, inhibits ERK phosphorylation in H358 cells with an IC50 of 31 nM, and curtails the proliferation of H358 cells with an IC50 of 5 nM.</p>

<p>KRAS G12C inhibitor 69 (Compound K09) is an inhibitor of the mutant RAS protein KRAS G12C with an IC50 of 4.36 nM. In the cell lines NCI-H358 and MIA-PACA-2, it suppresses ERK phosphorylation with IC50 values of 12 nM and 7 nM, respectively. Additionally, KRAS G12C inhibitor 69 hinders the proliferation of NCI-H358 and MIA-PACA-2 cancer cells, with IC50 values of 3.15 nM and 2.33 nM, respectively.</p>

JH295: potent, selective Nek2 inhibitor (IC50 = 770 nM), irreversibly targets Cys22, no effect on Cdk1, Aurora B, Plk1, or spindle mechanisms.

<p>Enniatin B1, a Fusarium mycotoxin, crosses the blood-brain barrier and modulates ERK, NF-κB, and ACAT with an IC50 of 73 μM.</p>

LC-2 (PROTAC KRASG12C Degrader-LC-2) is a novel von Hippel-Lindau-based PROTAC degrader of endogenous KRAS G12C with a DC50 between 0.25 and 0.76 μM.LC-2 is a

Anti-ERK2 Antibody (4F551) is a Rabbit antibody targeting ERK2. Anti-ERK2 Antibody (4F551) can be used in ELISA,FCM.

Anti-ERK2 Antibody (9C922) is a Mouse antibody targeting ERK2. Anti-ERK2 Antibody (9C922) can be used in WB,ELISA.

Cephradine (Standard) is the standard substance of Cephradine, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Cephradine (Anspor) is a beta-lactam, first-generation cephalosporin antibiotic with bactericidal activity.

Tunlametinib is a MEK1/2 inhibitor (IC50=1.9 nM) for treating RAS/RAF-driven cancers.

<p>TRPM4 inhibitor 8 is an inhibitor of Transient receptor potential melastatin 4(TRPM4) which contributes to viability, migration, cell cycle shift, and adhesion.</p>

Enniatins B decreases the activation of ERK (p44/p42).

S6K1-IN-DG2(S6K1InhibitorDG2) is a potent p70S6K inhibitor with an IC50 value of less than 100 nM.

Anti-ERK2 Antibody (5V598) is a Rabbit antibody targeting ERK2. Anti-ERK2 Antibody (5V598) can be used in ELISA.

RAS GTPase inhibitor 1 is a RAS GTPase inhibitor with potential antitumor activity.

TAK1-IN-3 is a novel ATP-competitive TAK1 inhibitor for the study of cancer.

MLK-IN-1 is a potent and selective mixed-lineage kinase 3 (MLK-3) inhibitor, showing excellent brain penetration and high specificity for MLK-3. MLK-IN-1 at 100 nM supports sustained axonogenesis in cultures challenged with HIV-1 Tat-activated microglia and protects neuronal cells from Tat-induced damage, establishing it as a valuable probe for neuroinflammation and neurodegeneration research.

GS87 is a highly specific inhibitor of GSK3 (glycogen synthase kinase 3) that induces extensive differentiation of AML cells.

Isoliquiritin apioside, from Glycyrrhizae radix, inhibits MMP9, MAPK, NF-κB, reduces cancer cell invasion, angiogenesis, and fights oxidative DNA damage.

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

<p>SCH772984 is an ERK inhibitor and is highly selective and ATP-competitive. SCH772984 exhibits antitumor activity. Cost-effective and quality-assured.</p>

Nardosinone inhibits H9c2 cell hypertrophy, protects neurons from OGD, and boosts neurite outgrowth by modifying key signaling pathways.

TAK-580 (MLN2480) is an oral, selective pan-Raf kinase inhibitor in Clinicalal trials.

BI-882370 is a specific RAF kinase inhibitor.

<p>Ravoxertinib (GDC-0994) is an effective and orally available ERK1/2 inhibitor (IC50: 1.1/0.3 nM).</p>

CID-1067700 is one of the first identified competitive inhibitors of nucleotide binding by Ras-related GTPases（Rab7 with a Ki of 13 nM).

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

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

<p>HPK1-IN-7 is an orally active HPK1 inhibitor. It shows selectivity against IRAK4 (59 nM) and GLK (140 nM).</p>

<p>Regorafenib HCl (BAY73-4506) is an oral inhibitor targeting angiogenic, stromal, and cancer kinases with strong antitumor effects.</p>

<p>UM-164 (DAS-DFGO-II), a highly potent c-Src inhibitor with a dissociation constant (Kd) of 2.7 nM, also effectively inhibits p38α and p38β.</p>

R1487 is an orally bioavailable and highly selective p38α mitogen-activated protein kinase inhibitor.

LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I.

Gypenoside L inhibits autophagic flux and induces cell death in human esophageal cancer cells through endoplasm reticulum stress-mediated Ca2+ release.

GNE-495 is a potent and specific MAP4K4 inhibitor (IC50: 3.7 nM).

PROTAC BRAF-V600E degrader-1 (Compound 23) selectively induces degradation of BRAF-V600E but not wildtype BRAF.

DMX-5804 is a potent, selective MAP4K4 inhibitor, with an IC50 of 3 nM.DMX-5804 enhances cardiomyocyte survival, and reduces ischemia-reperfusion injury in mice

Kobe 2602 is an inhibitor of Ras that exhibits anticancer chemotherapeutic activities.

Dabrafenib Mesylate (GSK2118436 Mesylate) is a B-Raf inhibitor(IC50s of 0.6 and 5.0 nM for RafV600E and c-Raf, respectively).

NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC50s of 149 nM and 21.7 nM, respectively.

Belvarafenib (HM95573) is a potent pan-RAF inhibitor with antitumor activity and inhibits B-RAF, B-RAFv600E, and C-RAF.Cost-effective and quality-assured.

Cichoric Acid (Dicaffeoyltartaric acid) is a potent inhibitor of human immunodeficiency virus type-1 (HIV-1) integrase and the replication in tissues.

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

methyl 5-(3,4-dimethoxyphenyl)isoxazole-3-carboxylate is a biochemical.

APS-2-79 hydrochloride (APS-2-79 HCl) is a MAPK antagonist that modulating KSR-dependent MAPK signalling by antagonizing RAF heterodimerization.

RO4987655 (RG7167) is an orally active and highly selective MEK inhibitor (IC50: 5.2 nM for MEK1/MEK2).

<p>IQ3 inhibits JNK3 (Kd 66 nM), JNK1/2, NF-κB/AP1 in THP1-Blue cells (IC50 1.4 μM), and reduces TNF-α/IL-6 production.</p>

SLV-2436 (SEL201-88) is a novel effective and ATP-competitive inhibitor of MNK1 and MNK2 (IC50: 10.8/5.4 nM).

<p>Necrosulfonamide ((E)-Necrosulfonamide) is a necroptosis inhibitor that targets MLKL and is selective. High-Quality, Low-Cost!</p>