MAPK

MEK1/2-IN-2 is a potent, ATP-competitive MEK1/2 inhibitor that exhibits equal inhibitory effects on wild-type MEK1/2 and a group of MEK1/2 mutant cells.

<p>KU004, a potent dual EGFR/HER2 inhibitor, exhibits anticancer properties. It inhibits the proliferation of human breast cancer SKBR3 cells by inducing G1 phase arrest. KU004 blocks the activation of HER2, EGFR, and the downstream Akt and Erk pathways, primarily inducing apoptosis (Apoptosis) through the extrinsic pathway. Additionally, KU004 is a novel quinazoline derivative.</p>

KRAS G12C inhibitor 44: potent, oral, anti-cancer; halts cell growth in MIA PaCA-2, H358; effective in vivo. IC50: MIA-0.016μM, H358-0.028μM.

<p>G-479, a potent MEK inhibitor and improved analogue of GDC-0623, has distributed polarity enhancing bioactivity.</p>

NHTD, a KRAS-PDEδ inhibitor, exerts its function by targeting the isoprenyl binding pocket of PDEδ, which alters the cellular localization of KRAS. This modification restricts the proliferation of cancer cells with KRAS mutations and induces cell apoptosis (Apoptosis). NHTD is utilized in the study of KRAS-driven non-small cell lung cancer (NSCLC).

SOS1-IN-6 (compound 33-P1) is a potent inhibitor of SOS1, acting on SOS1-G12D (IC50: 14.9 nM) and SOS1-G12V (IC50: 73.3 nM).

MRTX849 acid, used to make PROTAC LC-2, effectively degrades KRAS G12C at 0.25-0.76 μM DC50.

KRAS G12D inhibitor 1 (example 243) is an inhibitor of KRAS G12D with an IC 50 of 0.8 nM for KRAS G12D-mediated ERK phosphorylation [1].

SOS1-IN-10 is a potent inhibitor of SOS1 that acts on KRAS G12C-SOS1 (IC50: 13 nM).

KRASG12C IN-13 (LY3499446), a potent inhibitor of KRAS G12C, shows potential in the study of advanced solid tumors, specifically non-small cell lung cancer and colorectal cancer.

HPK1-IN-14 is a potent inhibitor of HPK1. HPK1-IN-14 has potential for the study of HPK1-related diseases.

p38-α MAPK-IN-5: potent p38α inhibitor, IC50s: 0.1 nM (α), 0.2 nM (β), 944 nM (γ), 4100 nM (δ); anti-inflammatory, promising for asthma/COPD research.

KRAS G12C inhibitor 33 is a KRAS G12C inhibitor that can be used to study cancer.

AMG-548 dihydrochloride, an oral p38α inhibitor (Ki: 0.5 nM), selectively targets p38β, γ, δ, inhibits TNFα (IC50: 3 nM), and suppresses Wnt signaling.

Rho GTPase inhibitor 1 (compound 7) is a potent inhibitor of Rho GTPase. It exhibits high affinity for Cdc42, Rac1, and RhoA, with dissociation constants (KDs) of 151 μM, 352 μM, and 232 μM, respectively. Additionally, Rho GTPase inhibitor 1 reduces cell migration in glioblastoma cell lines.

KRAS ligand 5 acts as the target protein ligand for PROTACK-Ras Degrader-3, which specifically targets and degrades mutated KRAS proteins.

MK2-IN-4 is a MAPKAPK2 (MK2) inhibitor (IC50: 45 nM). MK2-IN-4 can be used in cancer, inflammation and immunology studies.

(R)-STU104-d6 is a deuterium-labeled variant of (R)-STU104. This compound acts as a potent and orally active inhibitor of the interaction between TAK1 and MKK3 proteins, exhibiting IC50 values of 0.58 μM for TNF-α and 4.0 μM for MKK3 phosphorylation. By binding to MKK3, (R)-STU104 hinders TAK1's ability to phosphorylate MKK3, thereby disrupting the TAK1/MKK3/p38/MnK1/MK2/elF4E signaling pathway. It is utilized in research related to ulcerative colitis.

<p>KRAS inhibitor-36 (compound Abd2) directly inhibits KRAS Q61H.</p>

JAK3-IN-13: Oral JAK3 inhibitor, selective & potent. Acts on NK1, JNK2, JNK3, Tyk2. Anti-tumor. IC50: JNK3, 8 nM; Tyk2, 365 nM; JNK2, 2039 nM; NK1, 4728 nM.

SOF-436 is a KRAS inhibitor that can suppress SOS1-mediated KRAS nucleotide exchange (IC50 = 60 μM) and inhibit the interaction between KRAS and the effector protein RAF. SOF-436 is applicable to cancer research.

AZD4625 (Compound 21) is a selective, potent, orally active, covalent and mutagenic mutant GTPaseKRASG12C inhibitor.

MEK4 Inhibitor-2, a novel MEK4 inhibitor, demonstrates efficacy against pancreatic adenocarcinoma, exhibiting an IC50 value of 83 nM.

HPK1-IN-21 is a potent, orally active HPK1 kinase inhibitor with a Ki value of 0.8 nM.

Dorrigocin A, an analog of Migrastatin, inhibits the carboxymethyltransferase involved in Ras processing, reversing the morphology of Ras-transformed NIH/3T3 cells. Dorrigocin A holds potential for research as an anticancer and anti-arthritis agent.

SML-10-70-1 is a Novel Active Site Inhibitor of Oncogenic K-Ras G12C.

KRAS inhibitor-8 is a potent KRAS G12C inhibitor.

EBI-1051 is a highly potent and orally efficacious inhibitor of MEK (IC50: 3.9 nM).

KRAS G12C inhibitor 46 is a potent inhibitor of KRAS G12C.

<p>KRAS inhibitor-35 (compound 72) is a KRAS inhibitor with an IC50 of 2 nM, utilized in tumor research.</p>

KRAS inhibitor-21 (22b) is a KRAS G12C inhibitor (IC50<0.01 μM) that can be used in cancer research.

Everafenib: potent BRAF inhibitor, crosses blood-brain barrier, hinders MAPK, effective on V600EBRAF cells, outperforms other drugs in trials.

G12Si-1 selectively binds and inhibits K-Ras(G12S) to block oncogenic signaling and nucleotide exchange.

HPK1-IN-31 inhibitor with an IC 50 value of 0.8 nM. HPK1-IN-31 has anti-tumour activity and has great potential for immunotherapy .

KRAS G12D inhibitor 12 targets Ras protein for cancer research. (Patent WO2021108683A1, Compound 134)

MRTX849 is a KRAS G12C ligand and PROTAC linker for creating potent LC-2, degrading KRAS G12C with DC50 of 0.25-0.76 μM.

<p>KRAS inhibitor-31 (compound 33), a potent agent targeting KRAS, exhibits K D (SPR) values of 0.019 nM for KRas G12D, 0.019 nM for KRas G12C, and 0.096 nM for KRas G12V, illustrating its efficacy across these variants.</p>

EBI-907 is a potent, oral B-RafV600E inhibitor with an IC50 of 4.9 nM, over 10x stronger than Vemurafenib, and effective against key cancer kinases.

MAP855: potent, selective, oral MEK1/2 inhibitor; IC50=3 nM, pERKEC50=5 nM; effective on wild-type/mutant MEK1/2.

<p>JNK-IN-19 (Compound Q8) is an inhibitor of c-Jun N-terminal kinase, utilized for the treatment and/or prevention of injuries prior to, during, or following surgery.</p>

ZCL279 is a small molecule modulator (SMM) that inhibits the interaction between CDC42 and intersectin (ITSN). At lower concentrations (<10 μM), ZCL279 activates Cdc42, a cytoplasmic small GTPase in the Ras superfamily, while at higher concentrations (<10 μM) it significantly inhibits it.

<p>SR-302 is a potent and selective inhibitor of DDR/p38, with IC50 values of 0.125 μM for p38α, 0.023 μM for DDR1, and 0.018 μM for DDR2. It is utilized in research related to fibrotic diseases, such as kidney and lung fibrosis, atherosclerosis, and various types of cancer.</p>

KRAS G12D inhibitor 26 (Compound 64B) is an inhibitor of KRAS G12D with an IC50 ≤ 100 nM.

<p>Sosimerasib is an inhibitor of the kirsten rat sarcoma viral oncogene homolog (KRAS) and exhibits antitumor activity.</p>

KRAS G12D Inhibitor 3, a compound targeting the KRAS G12D mutation, demonstrates potent antitumor efficacy with an inhibitory concentration (IC50) of less than

<p>KRAS G12D inhibitor 28 (Compound 1) is an inhibitor of KRAS G12D and can be utilized in cancer research.</p>

MLKL-IN-1 is a covalent inhibitor of MLKL with a Kd value of 50 μM.

KRAS G12C inhibitor 50 is a KRAS G12C inhibitor (IC50: 46.7 nM).

INCB159020 is an orally active inhibitor of KRAS G12D, exhibiting a KRAS G12D SPR value of 2.2 nM. It demonstrates anti-tumor activity.

SOS2 ligand 1 (compound 2) is a selective ligand for son of sevenless 2 (SOS2), exhibiting a KD value of 4.6 µM.

GDC-6036-NH is a precursor of compound 17a /b, which is a RAS inhibitor that can be used in cancer research.

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

<p>HPK1-IN-55 (compound 19) is a selective and orally active inhibitor of hematopoietic progenitor kinase 1 (HPK1) with an IC50 of less than 0.51 nM. It exhibits exceptional kinase selectivity, being over 637 times more selective for HPK1 compared to GCK kinase and over 1022 times compared to LCK. HPK1-IN-55 possesses anti-cancer properties.</p>

MCB-22-174 is a potent agonist of Piezo1 with an EC50 value of 6.28 µM. It activates Ca2+-related extracellular signal-regulated kinase and calcium-calmodulin (CaM)-dependent protein kinase II (CaMKII) pathways, and it promotes mesenchymal stem cell osteogenic differentiation, indicating its potential application in the study of disuse osteoporosis (OP).

<p>Casein kinase1δ-IN-31 (Compound 16) is an inhibitor of casein kinase (CK), specifically targeting CK1α, CK1δ, and p38α, with IC50 values of 196 nM, 17 nM, and 18 nM, respectively. Additionally, Casein kinase1δ-IN-31 inhibits Double Homeobox 4 (DUX4) with an IC50 of 1200 nM.</p>

KRAS inhibitor-13 blocks KRAS G12C (IC50: 0.883 μM) and p-ERK in some cancer cells; promising for pancreatic, colorectal, lung cancer research.

<p>JD123 inhibits the activity of JNK1 and the expression of cJun (1-135). It is an ATP-competitive inhibitor specific to p38-γ MAPK and has no effect on ERK1, ERK2, p38-α, p38-β, and p38-δ.</p>

<p>p38-α MAPK-IN-9 (Compound 25a) is a p38-α MAPK inhibitor with a Ki value of 0.057 nM. It effectively inhibits LPS-induced TNFα production in hPBMC cells, exhibiting an IC50 of 18 nM.</p>

<p>p38-α MAPK-IN-10 (Compound 6) is an inhibitor of p38α, with an IC50 value of 4 nM.</p>

CK1δ-IN-9 (Compound 8) is an inhibitor of casein kinase 1 (CK1), specifically targeting CK1δ with an IC50 of 1.4 nM. The compound also inhibits p38α and p38β with IC50 values of 0.25 μM and 0.78 μM, respectively. CK1δ-IN-9 exhibits favorable pharmacokinetic properties, including high oral bioavailability (70%) and moderate clearance.

ERK-IN-2, an ERK2 inhibitor, exhibits an IC50 value of 1.8 nM. At doses greater than 10 μM, it may induce off-target toxicity and/or activity [1].

K-Ras-IN-4 (compound CP163) is an inhibitor of K-Ras.

<p>KRAS G12C inhibitor 15 is a potent KRAS G12C inhibitor .</p>

MNK1ligand 1 (Compound 5) is an MNK1 ligand used in the synthesis of PROTACMNK1 degrader-1.

AMG-548 hydrochloride: orally active, p38α inhibitor (Ki=0.5 nM), 1000x less for p38γ/δ, also blocks TNFα (IC50=3 nM) & inhibits casein kinase 1 δ/ε.

ABS-752 is an effective and orally active molecular glue degrader targeting GSPT1 and NEK7. It exhibits cytotoxic properties and reduces the protein expression of GSPT1, SALL4, and NEK7. ABS-752 possesses anticancer activity and shows potential for research in hepatocellular carcinoma.

<p>Anti-osteoporosis agent-11 (compound 3k) is an anti-osteoporosis compound targeting osteoclasts. It exhibits its most prominent effect by inhibiting osteoclast differentiation, with an IC50 value of 0.36 μM. Additionally, Anti-osteoporosis agent-11 suppresses osteoclast formation, bone resorption, and the expression of osteoclast-specific genes by blocking the RANKL-induced mitogen-activated protein kinase (MAPK) and NF-κB signaling pathways.</p>

RGT-018 is a potent oral SOS1 inhibitor with antitumor properties. It exerts its anticancer activity by inhibiting KRAS activation, thereby hindering cancer cell proliferation.

<p>JNK-IN-21 (Compound 62) is an inhibitor of JNK-1.</p>

BMS-214662 is a selective farnesyl transferase inhibitor with anti-tumor activity, used in research on pancreatic cancer, head and neck cancer, and lung cancer.

SHR2415: Potent, selective ERK1/2 inhibitor, oral; ERK1 IC50: 2.8 nM, ERK2 IC50: 5.9 nM; effective in Colo205 (IC50: 44.6 nM), for cancer research.

SHR902275: potent RAF inhibitor, hits RAS mutations, oral use. cRAF IC50=1.6 nM, bRAFwt IC50=10 nM, bRAFV600E IC50=5.7 nM, hinders cell growth.

ADT-1004 is an inhibitor of RAS. It can be used for research involving Ras-mediated diseases.

Cot inhibitor-3 (Compound 33) is an effective and selective cancerosaka thyroid (COT) kinase inhibitor with an IC50 of 4 nM. It can be used to prevent limpness caused by inflammation.

<p>Casein kinase1δ-IN-27 (Compound 8) is an inhibitor of casein kinase 1 (CK1), effectively inhibiting CK1α, CK1δ, CK1ε, and p38α with IC50 values of 22, 16.5, 9.41, and 14.8 nM, respectively. It also suppresses DUX4 expression, with an IC50 of 10 nM.</p>

HPK1 ligand-Linker Conjugate 1 is a synthetic target protein ligand-linker compound used in the synthesis of PROTACs, such as PROTACHPK1 Degrader-5. PROTACHPK1 Degrader-5 is a potent and orally active HPK1 PROTAC degrader with anti-tumor activity.

p38 MAP Kinase-IN-1 (Compound 4) is an inhibitor of p38, suitable for studies related to inflammation and autoimmune responses.

p38 Kinase inhibitor 7 (Comp:XXXIX) is an inhibitor of p38α, with an IC50 value of 5.25 nM. It also effectively suppresses TNFα production in THP-1 cells, demonstrating an IC50 of 5.88 nM.

L 739749 is a CAAX peptidomimetic. It is also an inhibitor of farnesyl-protein transferase.

p38α inhibitor8 (Compound 1) demonstrates inhibitory activity against p38αMAPK and CK1δ, with IC50 values of 0.21 µM and 0.202 µM, respectively.

NDI-101150 (NMBS-2) is an HPK1 inhibitor with antitumor activity, inhibiting BLNK phosphorylation, and used in metastatic solid tumor research.

Emprumapimod, an oral p38α MAPK inhibitor, targets RPMI-8226 cells, curbs LPS-induced IL-6; IC50: 100 pM; for cardiomyopathy, acute pain.

Rineterkib (ERK-IN-1) is an inhibitor of RAF and ERK1/2 activating mutations in the MAPK pathway.

CMK, an RSK2 kinase inhibitor, shows similar potency but less chemical stability compared with FMK.

<p>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).</p>

Omtriptolide, triptolide purified from the Chinese herb, is a water-soluble derivative prodrug.

2413035-41-1 is a useful organic compound for research related to life sciences. The catalog number is T8743 and the CAS number is 2413035-41-1.

<p>PLX7922, a RAF inhibitor, demonstrates binding affinity with BRAF V600E and exhibits inhibitory effects on pERK in BRAF V600E cell lines, while inducing pERK activation in mutant NRAS cell lines.</p>

HPK1-IN-19 is an inhibitor of hematopoietic progenitor kinase 1 (HPK1).

<p>WQ-C-401 is an orally active inhibitor of the platelet-derived growth factor receptor (PDGFR). It inhibits cell proliferation by blocking PDGFR auto-phosphorylation in a concentration-dependent manner, with EC50 values of 3.5 nM for PDGFRαY849 and 5.8 nM for PDGFRβY1021. Additionally, WQ-C-401 suppresses the proliferation and migration of PASMCs by inhibiting PDGF-BB-induced phosphorylation of ERK1/2, reduces collagen I synthesis, and increases α-SMA expression, thereby preventing pulmonary vascular remodeling. This compound shows promise for research in the field of pulmonary arterial hypertension.</p>

<p>IHMT-RAF-128 is a potent pan-RAF inhibitor that demonstrates robust antitumor activity in xenograft mouse tumor models without causing significant toxicity.</p>

<p>SKLB646 is an orally active multitarget kinase inhibitor that exhibits potent suppression of several kinases. It demonstrates significant inhibitory effects on SRC and VEGFR2, with IC50 values of 0.002 μmol/L and 0.012 μmol/L, respectively. Additionally, SKLB646 shows notable inhibition of B-Raf and C-Raf, with IC50 values of 0.022 μmol/L and 0.019 μmol/L, respectively. The compound inhibits the activation of the SRC signaling pathway and blocks the MAPK signaling pathway by inhibiting Raf kinases. Furthermore, SKLB646 inhibits the proliferation, migration, and invasion of human umbilical vein endothelial cells (HUVEC), thereby suppressing tumor-induced angiogenesis. SKLB646 also displays significant anti-proliferative and anti-survival effects on triple-negative breast cancer (TNBC) cell lines.</p>