Bioactive Small Molecules
Medchemexpress LLC Apilimod (mesylate) | 870087-36-8 | 99.8% | 610.70 | 1 ML
Apilimod (STA 5326) mesylate is a potent IL-12/IL-23 inhibitor, strongly inhibiting IL-12 with IC50s of 1 nM and 2 nM in IFN-γ/SAC-stimulated human and monkey PBMCs. It is also a potent and highly selective PIKfyve inhibitor.
- Potent IL-12/IL-23 inhibitor
- Strongly inhibits IL-12
- Potent and highly selective PIKfyve inhibitor
- Inhibits IFN-γ production in human PBMCs
- Reduces severity of experimental autoimmune uveoretinitis (EAU)
Medchemexpress LLC NTRC 0066-0 | 1817791-73-3 | 99.01% | 565.71 | 5 MG
NTRC 0066-0 is a selective threonine tyrosine kinase (TTK) inhibitor, demonstrating potent anti-proliferative activity against diverse cancer cell lines. With an IC50 of 0.9 nM, it is utilized in cancer research, exhibiting low selectivity entropy and a prolonged target residence time on TTK.
- Selective threonine tyrosine kinase (TTK) inhibitor (IC50=0.9 nM).
- Used for cancer research.
- Exhibits low selectivity entropy.
- Relatively long target residence time on TTK.
- Inhibits proliferation of diverse cancer cell lines with potency similar to classic chemotherapeutic agents.
- Demonstrates subnanomolar potency in a TTK enzyme assay.
- Inhibits tumor growth in a mouse xenograft model of human triple-negative breast cancer (TNBC).
Medchemexpress LLC GNE-207 | 2158266-58-9 | 99.9% | 1 ML
GNE-207 is a potent, selective small-molecule inhibitor of the CBP/p300 bromodomain supplied as a ready-to-use 10 mM solution in DMSO (1 mL). It is intended for biochemical and epigenetic research applications, including in vitro bromodomain binding and selectivity studies.
- Ready-to-use 10 mM solution in DMSO, 1 mL
- High purity, approximately 99.9%
- Molecular formula C29H30N6O3 and molecular weight 510.59 g/mol
- Suitable for in vitro biochemical and epigenetic assays
- Store in solvent at -80°C for long-term stability
Medchemexpress LLC Triciribine (API-2) | 35943-35-2 | C13H16N6O4 | 1 ML
Triciribine is a nucleoside analog and purine analog that acts as a DNA synthesis inhibitor. It also selectively inhibits the phosphorylation and activation of all three Akt isoforms, with IC50 values of 130 nM for Akt and 0.02-0.46 μM for HIV-1/2. This product is for research use only.
- Inhibits DNA synthesis
- Inhibits Akt with an IC50 of 130 nM (cell assay)
- Inhibits HIV-1 and HIV-2 with IC50 values of 0.02-0.46 μM
- Selectively inhibits phosphorylation and activation of all three Akt isoforms
- Inhibits Akt phosphorylation at Thr308 and Ser473 at 10 μM concentration
- Effectively inhibits phosphorylation and catalytic activity of Akt in PC-3 cells
Medchemexpress LLC Deiodoamiodarone 5mg | 23551-25-9 | 5 MG
Deiodoamiodarone (L 3937 Dideiodo Amiodarone) is an intermediate of amiodarone Amiodarone is a potent calmodulin antagonist[1]
Medchemexpress LLC Collagen I alpha 2 Antibody (YA3695) | 10 UL
Collagen I alpha 2 Antibody (YA3695) is a Mouse-derived, non-conjugated IgG1 monoclonal antibody targeting Collagen I alpha 2. Intended for research use only, this antibody is supplied in PBS with 0.05% sodium azide and exhibits reactivity with human, mouse, rat, and monkey species.
- Mouse-derived IgG1 monoclonal antibody
- Targets Collagen I alpha 2
- For research use only
- Supplied in PBS with 0.05% sodium azide
- Reacts with human, mouse, rat, and monkey species
Medchemexpress LLC IHMT-MST1-58 | 2414484-25-4 | C21H22N6O3S | 5 MG
IHMT-MST1-58 is a potent, selective mammalian and orally active STE20-like protein 1 kinase (MST1) inhibitor with an IC50 value of 23 nM. It can be utilized for research related to Type 1/2 diabetes.
- Potent, selective mammalian and orally active STE20-like protein 1 kinase (MST1) inhibitor.
- IC50 value of 23 nM against MST1.
- Used for research of Type 1/2 diabetes.
- Strong inhibitory activity against MST1 (IC50 = 23 nM) and weak activity against MST2 (IC50 = 652 nM).
- Inhibits phosphorylation of MST1 in vitro.
- Protective effect on β cells from inflammatory cytokines.
- Combined with metformin, it decreased fasting blood glucose and hemoglobin A1c levels in STZ-induced T1D/T2D mouse models.
Medchemexpress LLC SB-423562 | 351490-27-2 | C26H32N2O4 | 10 MM * 1 ML
SB-423562 is a short-acting calcium-sensing receptor (CaR) antagonist. It has potential for osteoporosis research.
- Short-acting calcium-sensing receptor (CaR) antagonist
- Supports osteoporosis research
- Purity of 99.66%
- Supplied as 10 MM solution in 1 ML of DMSO
- Powder storage: -20°C for 3 years; 4°C for 2 years
- Solution storage: -80°C for 2 years; -20°C for 1 year
Medchemexpress LLC NIC-0102 | 2806031-94-5 | C21H25BF2N2O4 | 1 ML
NIC-0102 is an orally active proteasome inhibitor that specifically inhibits NLRP3 inflammatory vesicle activation. It demonstrates potent anti-inflammatory effects in a model of dextran sulfate sodium (DSS)-induced ulcerative colitis.
- Inhibits proteasome with a pIC50 of 7.55
- Specifically inhibits NLRP3 inflammatory vesicle activation
- Shows potent anti-inflammatory effects
- Inhibits production of pro-IL-1β
Medchemexpress LLC IHMT-MST1-58 | 2414484-25-4 | C21H22N6O3S | 1 ML
IHMT-MST1-58 is a potent, selective, mammalian, and orally active STE20-like protein 1 kinase (MST1) inhibitor with an IC50 value of 23 nM. It is utilized in research for type 1/2 diabetes.
- Potent MST1 inhibitor with an IC50 of 23 nM.
- Weak activity against MST2 and no activity against NEK3.
- Strong binding affinity to MST1.
- Inhibits phosphorylation of MST1 and downstream MOB1 autophosphorylation.
- Provides protective effect for β cells against inflammatory cytokine damage.
- Oral administration decreased fasting blood glucose and HbA1c levels in STZ-induced T1D/T2D mouse models.
- Acceptable pharmacokinetic properties across species.
- Purity: 99.05%.
Medchemexpress LLC FTO-IN-8 | 2640366-38-5 | C19H23ClN2O2 | 50 MG
FTO-IN-8 is an N6-methyladenosine demethylase (FTO) inhibitor with an IC50 value of 5.5 μM. This compound exhibits anti-cancer cell proliferative activity, making it suitable for research into cancer targeted therapy and metabolism.
- Inhibits proliferation of cancer cells (AGS, SNU-16, KATOIII)
- Shows no cytotoxicity to normal colonic cells (CCD-841CoN)
- Increases m6A and m6Am levels
- Inhibits Wnt/PI3K-Akt signaling in gastric cancer AGS cells
Selleck Chemical LLC STX-478-E1815-25MG
STX-478 is a highly potent mutant-selective allosteric inhibitor of PI3K that selectively targets prevalent mutant forms of PI3K It demonstrates strong efficacy against common PI3K helical- and kinase-domain mutations including the H1047R variant with an IC50 value of 9 4 nmol/L STX-478 exhibits 14-fold greater selectivity for mutant PI3K over the wild-type form It spares metabolic dysfunction and improves therapeutic response in PI3K -Mutant Xenografts
Selleck Chemical LLC Raf inhibitor 2-E0934-5MG
Raf inhibitor 2 is a potent Raf kinase inhibitor with an IC50 of 1 0 M
Medchemexpress LLC BMS-911543 | 1271022-90-2 | C23H28N8O | 2 MG
BMS-911543 is a highly selective JAK2 inhibitor with an IC50 of 1.1 nM. It demonstrates potent antiproliferative effects on JAK2-dependent SET-2 and BaF3-V617F engineered cell lines. This compound also selectively reduces pSTAT5 expression in pancreatic tumors and decreases intratumoral FoxP3+ T regulatory cells in mice, making it a relevant tool for research into myeloproliferative neoplasms and pancreatic cancer.
- Selective JAK2 inhibitor (IC50 1.1 nM)
- Potent antiproliferative effects on SET-2 and BaF3-V617F cells
- Reduces pSTAT5 expression in pancreatic tumors
- Decreases intratumoral FoxP3+ T regulatory cells
- Blocks T regulatory cell differentiation in vitro