501A054 is an autophagy activator. 501A054 induces autophagy-dependent cell death via autophagy activation. 501A054 can be used in studies on autophagy regulation such as cervical cancer.

1-Methyl-1H-indazol-5-amine is a drug intermediate that can be used for the synthesis of TRPM5 agonists.

(S,S,S)-AHPC-PEG2-NH2 is an isomer of Compound 15b. Compound 15b is a conjugate of a VHL ligand and linker. Compound 15b can be used to synthesize PROTAC. Compound 15b can be used in leukemia research.

(-)-P7C3-S243 is an orally active, blood-brain barrier permeable neuroprotective agent. (-)-P7C3-S243 binds to μ-opioid Receptor and TSPO. (-)-P7C3-S243 inhibits the premature apoptosis death of newborn hippocampal neurons, protects mature nigral dopaminergic neurons, promotes neuronal survival and prevents cognitive impairment. (-)-P7C3-S243 ameliorates depression-like behaviors in rat models. (-)-P7C3-S243 is applicable to research related to Parkinson's disease and Alzheimer's disease.

C3 sodium is an aptamer that binds to Erk2. C3 binds to the MAP kinase insert domain, a unique site on Erk1/2. Due to this recognition profile C3 inhibits Erk2 activation by its upstream kinase MKK1.

Calderasib (MK-1084) is a selective KRAS G12C inhibitor demonstrating antitumor efficacy. It can be utilized as monotherapy or in combination with pembrolizumab () for oncology research.

RMC5127 is a first-in-class, orally bioavailable mutant-selective tri-complex inhibitor of the GTP-bound (ON) form of RASG12V. It non-covalently binds to cyclophilin A (CypA), forming a binary complex that engages RASG12V(ON) to form a high-affinity tri-complex, sterically inhibiting RAS binding. It inhibits the RAS pathway in KRASG12V-mutant cancer cells, reducing proliferation, inducing apoptosis, and showing strong potential for use in RASG12V-mutated cancer research.

BBO-8956 is a highly potent, covalent inhibitor of GTP-KRAS G12C, BBO-8956 is effective against both GDP and GTP-bound KRAS G12C.

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

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.

AH001 is a orally active RhoA inhibitor, which binds a cryptic pocket proximate to GDP within RhoA with a KD of 73.16 nM. AH001 interacts with GDP, stabilizing RhoA’s interaction with its endogenous inhibitor, RhoGDIα. AH001 reduces the downstream MRTFA nuclear translocation and downregulates fibrosis/hypertrophy proteins. AH001 mitigates myocardial remodeling in multiple HF animal models, and in the 3D myocardial tissue model. AH001 exerts its cardioprotective effects through the RhoA-RhoGDIα axis, effectively inhibiting downstream RhoA activation signaling.

NuP-3 is a potent and selective MAPK13 and MAPK14 inhibitor (IC50 of 7 nM and 14 nM, respectively) that effectively targets respiratory inflammation and mucus overproduction. In human tracheal epithelial cell (hTEC) cultures, it markedly inhibits IL-13-induced MUC5AC and CLCA1 expression without causing cell toxicity, showing superior efficacy compared to the MAPK14 inhibitor NuP-43. Beyond its success in minipig models of airway disease and viral infection, NuP-3 also down-regulates biomarkers associated with basal-epithelial stem cell activation, demonstrating its role as a precise upstream therapeutic agent for chronic lung conditions.

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.

ACA22 is a small molecule KRAS inhibitor, inhibits KRAS-mediated signal transduction in cells expressing wild type (WT) and G12D mutant KRAS.

ACA-14 is a small molecule direct inhibitor of KRAS, impedes the interaction of KRAS with its effector Raf and reduces both intrinsic and SOS-mediated nucleotide exchange rates.

AMG410 is a non-covalent and selective pan-KRAS inhibitor with IC50 values of 1-4 nM for KRAS G12D, KRAS G12V, and KRAS G13D. AMG410 shows greater than 100-fold selectivity against both HRAS and NRAS. AMG410 is a dual GTP(on)- and GDP(off)-state inhibitor (Kd(GDP-state) of 1 nM; Kd(GTP-state) of 22 nM). AMG410 blocks KRAS signaling in a cycling state-independent manner and also blocks proliferation in wildtype KRAS-amplified tumor cells. AMG410 can be used for the study of colorectal, pancreatic, and lung cancers.

KRAS inhibitor-42 (compound 8) is a potent USP7 inhibitor. KRAS inhibitor-42 has high affinity against GDP-bound KRASG12D with a Ki of 2.7 μM.

WEIZ-WX-04-008 (Compound 1) is a covalent Lysine-targeting MKK7 inhibitor with IC50 of 738 nM.

R-03201195 is an efficient and selective p38 MAP kinase inhibitor with an IC50 for p38α of 0.7 nM. R-03201195 has inhibitory activity against TNF-α in THP-1 cells and against IL-1β in human whole blood, with IC50 values of 0.25 and 0.57 nM respectively. R-03201195 BIRB-1017 can be used for inflammatory diseases such as rheumatoid arthritis.

Sonvuterkib (WX001) is a potent and orally active extracellular signal-regulated kinases (ERK) inhibitor with IC50 values of 1.4, 0.54 nM for ERK1, ERK2, respectively. Sonvuterkib inhibits cell proliferation. Sonvuterkib shows anticancer activity.

WMJ-J-09 is an HDAC inhibitor with IC50 values of 7.5 nM (HDAC1), 21.3 nM (HDAC2), 18.4 nM (HDAC3), 90.9 nM (HDAC8), 3.9 nM (HDAC6) and 8715.7 nM (HDAC4). WMJ-J-09 blocks the cell cycle and induces apoptosis in cancer cells. WMJ-J-09 induces cancer cell death through the LKB1-AMPK-p38MAPK-p63-survivin signaling cascade.WMJ-J-09 inhibits HDAC enzyme activity, leading to acetylation of key proteins and thereby regulating cancer cell death. WMJ-J-09 can be used in HCT116 cells and FaDu cells research[1][2].

ADT-1004 is an inhibitor of RAS. ADT-1004 can be studied in research for Ras-mediated diseases.

A2073 is a flavagline derivative that potently inhibits the proliferation of erythroleukemia cells by causing cell cycle arrest and suppressing the MAPK, NF-κB, and PI3K signaling pathways. A2073 formes stable interactions with cell cycle-related proteins (CDK1, CCNA2, PRIM1). A2073 exhibits significant anti-proliferative activity against tumor cells while maintaining a favorable toxicity profile in a zebrafish xenograft tumor model. A2073 can be used for the study of acute erythroleukemia.

PHI-501 is a dual inhibitor targeting RAF/DDR. PHI-501 exhibits significant anti-proliferative effects in melanoma cell lines and significantly inhibits the colony formation of drug-resistant cells. PHI-501 strongly inhibits ERK and AKT phosphorylation. PHI-501 downregulates the gene sets in drug-resistant cells of TNFA-NFKB, IL6-JAK-STAT3, and KRAS signaling pathways as well as the epithelial-mesenchymal transition (EMT) signaling pathways. PHI-501 demonstrates significant anti-tumor effects in the SK-MEL3DR xenograft model. PHI-501 can be used for research on the problem of drug resistance in melanoma.

BMS-626531 is a potent and selective p38α MAP kinase inhibitor. BMS-626531 can be used for the research of cancer.

(R)-MK-8353 ((R)-SCH900353) is the R-enantiomer of MK-8353). MK-8353 (SCH900353) is a potent, selective and orally active ERK1 and ERK2 inhibitor with IC50s of 23.0 nM and 8.8 nM, respectively.

MCB-294 is a dual-state pan-KRAS inhibitor that selectively inhibits KRAS over NRAS and HRAS. MCB-294 capable of binding both the active (GTP-bound) and inactive (GDP-bound) forms of KRAS with Kds of approximately 1 pM and 10 nM, respectively. MCB-294 broadly impairs the growth of hTERT-HPNE cells expressing G12D, G12C, G12V, G12S, G13D, and wild-type KRAS, with IC50s of approximately 700 nM. MCB-294 induces irreversible apoptosis in KRAS-mutated tumors. MCB-294 effectively suppress KRASG12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-294 can be used for the study of pancreatic cancer, colorectal cancer and lung cancer.

Z56 is a Ras protein inhibitor. Z56 can be used for the research of cancer, such as pancreatic cancer.

Z52 is a Ras protein inhibitor. Z52 can be used for the research of cancer, such as pancreatic cancer.

Z52-L16 is Drug-Linker Conjugates for ADC, which is composed of a linker and a Ras inhibitor Z52. Z52-L16 can be used for the research of cancer, such as pancreatic cancer.