this compound

RMC-6236 is an orally effective and novel triple complex RAS (ON) MULTI inhibitor, which is a potent non covalent inhibitor of multiple RAS variants in GTP binding state. RMC-6236 has anti-tumor activity and can be used in research related to RAS driven tumors. With rich experience in compound synthesis, we can provide fast customized synthesis services for this product according to your research needs.

RMC-9805 is a novel, mutant-selective, covalent and oral KRASG12D (ON) inhibitor. A stable and high affinity triple complex is formed between RMC-9805, KRASG12D, and cyclophilin A, which inhibits signal transduction downstream of KRASG12D (ON) by disrupting its interaction with downstream effectors. RMC-9805 can induce cell apoptosis and promote tumor regression in preclinical KRASG12D tumor models. With rich experience in compound synthesis, we can provide fast customized synthesis services for this product according to your research needs.

GA-017 is a potent, selective inhibitor of LATS1 and LATS2 (large tumor suppressor kinase 1 2), exhibiting IC50 values of 4.10 and 3.92 nM, respectively. This compound simultaneously acts as an activator of cell proliferation by promoting YAP TAZ activation and their nuclear translocation. Additionally, GA-017 enhances cell growth in 3D culture conditions and augments the ex vivo formation of mouse intestinal organoids [1].

TDI-011536, a potent Lats kinase inhibitor, disrupts Hippo-Yap signaling and promotes the proliferation of lesioned heart muscle cells. This compound is valuable for research in organ conservation and regeneration.

EACC, a reversible autophagy inhibitor, selectively impedes Stx17, an autophagosome-specific SNARE, from translocating, hence obstructing the fusion between autophagosomes and lysosomes. This compound effectively halts autophagic flux.

LY88074 is a raloxifene analog in which the basic side chain has been removed. LY88074 is an agonist of ERβ (EC50 = 232 nM).This compound stimulates uterine cell proliferation.

NUCC-390, a novel small-molecule CXCR4 receptor agonist, selectively induces CXCR4 receptor internalization while acting antagonistically to AMD3100. This compound facilitates nerve functional recovery following neurodegeneration in vivo.

dMCL1-2 is a potent and selective myeloid leukemia 1 (MCL1) degrading agent based on PROTAC, binding to MCL1 with a KD of 30 nM and activating the apoptosis mechanism by degrading MCL1.

MB07803 is an orally available prodrug of an effective, noncompetitive inhibitor of fructose 1,6-bisphosphatase (FBPase) (EC50: 140 nM and t1/2 of 7.6±2.9 h).This compound is unstable in powder form and other related salt forms are recommended.

MEG hemisulfate (Mercaptoethylguanidine hemisulfate) acts as a highly potent and selective suppressor of inducible NO synthase (iNOS), demonstrating EC50 values of 11.5 μM for iNOS, 110 μM for ecNOS, and 60 μM for bNOS in tissue homogenates. It is notably effective as a peroxynitrite scavenger and blocks peroxynitrite-triggered oxidative mechanisms. Furthermore, this compound offers protective benefits across various experimental inflammation prototypes, such as ischemia reperfusion injury, hemorrhagic shock, periodontitis, inflammatory bowel disease, and both endotoxic and septic shock.

Broad spectrum cation channel blocker .This compound is unstable in powder form and other related salt forms are recommended.

inhibitor of phosphodiesterase type 5 (PDE5).This compound is unstable in powder form and other related salt forms are recommended.

Patamostat mesylate (E-3123) is a potent protease inhibitor with IC50 values of 39 nM for trypsin, 950 nM for plasmin, and 1.9 μM for thrombin. This compound demonstrates promising potential in suppressing the pathogenesis and development of acute pancreatitis.

MSDC-0602K (Azemiglitazone potassium) (Azemiglitazone potassium) is a PPARγ-sparing thiazolidinedione (Ps-TZD) compound that binds to PPARγ with an IC50 of 18.25 μM. It also modulates the mitochondrial pyruvate carrier (MPC). This compound, MSDC-0602K, has potential applications in researching fatty liver conditions, including dysfunctional lipid metabolism, inflammation, and insulin resistance. MSDC-0602K acts as an insulin sensitizer, improving insulinemia and fatty liver disease in mice both individually and in combination with Liraglutide.

BRK inhibitor P21d hydrochloride is a highly potent inhibitor of breast tumor kinase (BRK PTK6), displaying an IC50 of 30 nM, and effectively suppresses p-SAM68 with an IC50 of 52 nM. This compound serves as a valuable tool for evaluating BRK inhibitors' efficacy in xenograft breast tumor models, enabling in vivo activity assessment.

P53R3 is a potent reactivator of p53, effectively restoring sequence-specific DNA binding to several p53 hot spot mutants, namely p53 R175H, p53 R248W, and p53 R273H. This compound exhibits p53-dependent antiproliferative effects with significantly higher specificity compared to PRIMA-1 and promotes the recruitment of both wild-type p53 and p53 M237I to various target gene promoters. Additionally, P53R3 markedly increases the mRNA, total protein, and cell surface expression of death receptor 5 (DR5), demonstrating its utility in cancer research.

PF-04753299 is a potent and selective inhibitor of UDP-3-O-(R-3-hydroxymyristol)-N-acetylglucosamine deacetylase (LpxC), demonstrating bactericidal effects against gonococcal isolates and exhibiting inhibitory activity against E. coli, P. aeruginosa, and K. pneumoniae, with minimum inhibitory concentration (MIC) 90 values of 2 μg ml, 4 μg ml, and 16 μg ml, respectively. This compound is utilized in researching gram-negative bacterial infections [1].

PBRM1-BD2-IN-7, a selective and cell-active inhibitor targeting the polybromo-1 (PBRM1) bromodomain, demonstrates inhibitory efficacy against PBRM1-BD2 with an IC50 value of 0.29 μM. This compound is utilized in cancer research.

PBRM1-BD2-IN-2, a selective and cell-active inhibitor of the polybromo-1 (PBRM1) bromodomain, exhibits binding affinity and inhibitory activity specifically targeting the PBRM1-BD2 domain, with Kd and IC50 values of 9.3 μM and 1.0 μM, respectively. This compound is utilized in cancer research.

PBRM1-BD2-IN-5 is a potent inhibitor of the PBRM1 Bromodomain, with dissociation constant (Kd) values of 1.5 μM and 3.9 μM for PBRM1-BD2 and PBRM1-BD5 respectively, and an inhibitory concentration 50 (IC50) value of 0.26 μM for PBRM1-BD2. This compound effectively diminishes the interaction between full-length PBRM1 and acetylated histone peptide within the PBAF complex in cell lysates, making it a promising candidate for anticancer research.

UNC1062 is a highly selective tyrosine kinase inhibitor that specifically targets MERTK. This compound effectively suppresses MERTK-mediated downstream signaling, induces apoptosis in cell cultures, reduces colony formation in soft agar, and inhibits invasion of melanoma cells. Notably, UNC1062 demonstrates potent inhibition of MERTK kinase activity, with an IC50 of 1.1 nM and a Morrison Ki of 0.33 nM. It also displays specificity within the TAM family, exhibiting IC50 values of 60 nM for TYRO3 and 85 nM for AXL [1].

(Rac)-Upacicalcet is a racemate of Upacicalcet, which serves as an intravenous calcimimetic agent. Upacicalcet acts by directly targeting calcium-sensing receptors on parathyroid cell membranes, effectively suppressing the release of excessive parathyroid hormone (PTH) and reducing blood PTH levels. This compound holds the potential for researching secondary hyperparathyroidism (SHPT) [1].

ARN25068 is a potent inhibitor of GSK-3β, FYN, and DYRK1A protein kinases, exerting its activity in the sub-micromolar range. This compound effectively addresses tau hyperphosphorylation [1].

HTT-D3 is an orally active, highly efficient Huntington splicing modulator. It induces HTT mRNA degradation, reduces HTT protein levels, and inhibits P-glycoprotein (P-gp) efflux. This compound can be used in Huntington's disease research.