Dimethyl Sulfoxide
Apexbio Technology LLC ABT-737 852808-04-9 10mM (in 1mL DMSO)
ABT-737 (CAS 852808-04-9) is a small molecule inhibitor targeting the BCL-2 protein family exhibiting high binding affinity toward the anti-apoptotic proteins BCL-2 BCL-X L and BCL-w ABT-737 disrupts BCL-2/BAX protein interactions leading to apoptosis primarily via the BAK-mediated intrinsic pathway independent of BIM In preclinical studies ABT-737 demonstrated single-agent antitumor activity in lymphoma multiple myeloma and small-cell lung cancer models Additionally research indicates activity against acute myeloid leukemia (AML) cells progenitor cells and leukemia stem cells while sparing normal hematopoietic populations highlighting its potential for therapeutic research in hematologic malignancies
Apexbio Technology LLC Pomalidomide (CC-4047) 19171-19-8 10mM (in 1mL DMSO)
Pomalidomide (CC-4047) an immunomodulatory derivative structurally related to Thalidomide exhibits anti-tumor and anti-angiogenic properties Chemically the molecule is distinguished by additional amino substituent at the fourth position of the phthalimide ring and two extra oxy groups Its mechanism of action includes modulation of specific cytokines within the tumor microenvironment (TNF- IL-6 IL-8 VEGF) suppression of tumor cell proliferation and modification of host immune cell activity Pomalidomide is widely studied in biomedical research particularly in therapeutic exploration for hematologic malignancies such as multiple myeloma including relapsed or refractory disease states
Apexbio Technology LLC NU7441 (KU-57788) 503468-95-9 10mM (in 1mL DMSO)
NU7441 (KU-57788 CAS 503468-95-9) is a selective inhibitor targeting DNA-dependent protein kinase (DNA-PK) via competition with ATP exhibiting an IC50 of approximately 13 nM and a Ki of 0 65 nM It demonstrates high specificity showing minimal inhibition of related kinases ATM and ATR at concentrations up to 100 M and substantially weaker activity towards mTOR and PI3K (IC50 values of 1 7 and 5 M respectively) NU7441 sensitizes HeLa cells to etoposide enhancing cytotoxicity and augments tumor growth delay when co-administered in SW620 xenograft mouse models The molecule serves as a tool compound in DNA repair and oncology research
Apexbio Technology LLC Entecavir Hydrate 209216-23-9 10mM (in 1mL DMSO)
Entecavir hydrate is an antiviral compound that acts as a reverse transcriptase (RT) inhibitor specifically targeting hepatitis B virus (HBV) infection It inhibits HBV DNA replication by interacting with the viral reverse transcriptase enzyme thus preventing the synthesis of complementary DNA from the viral RNA template Entecavir hydrate is frequently employed in antiviral studies and clinical research related to hepatitis B treatment regimens In studies involving chronic HBV-infected patients entecavir hydrate combined with peginterferon alpha-2b therapy has shown significant suppression of viral DNA levels and reduced covalently closed circular DNA (cccDNA) within hepatocytes The reported IC50 value of entecavir hydrate against HBV DNA polymerase activity typically ranges below 10 nM in cellular assay systems enabling its utility in both preclinical and clinical antiviral investigations
Apexbio Technology LLC CH5138303 959763-06-5 10mM (in 1mL DMSO)
CH5138303 (CAS 959763-06-5) is a potent inhibitor targeting Heat Shock Protein 90 (HSP90) exhibiting strong binding affinity with a Kd of 0 48 nM HSP90 a molecular chaperone regulates protein folding stability and degradation and maintains oncogenic proteins crucial to tumor cell proliferation CH5138303 effectively reduces protein levels and phosphorylation of HSP90 client proteins including Raf1 AKT EGFR and HER2 in NCI-N87 cancer cells In animal studies using human gastric cancer NCI-N87 xenografts oral administration of CH5138303 demonstrates significant antitumor activity achieving a tumor growth inhibition (TGI) rate of 136% at an ED of 3 9 mg/kg
Apexbio Technology LLC TAK-242 243984-11-4 10mM (in 1mL DMSO)
TAK-242 (CAS 243984-11-4) also known as resatorvid is a cyclohexene derivative that functions as a selective inhibitor of Toll-like receptor 4 (TLR4) signaling Mechanistically TAK-242 binds specifically to the intracellular domain of TLR4 disrupting its interaction with downstream adaptor proteins and thus suppressing activation of inflammatory signal pathways triggered by lipopolysaccharide (LPS) In vitro TAK-242 inhibits LPS-induced production of nitric oxide TNF- and interleukin-6 in macrophages (IC50 1 1 11 nM) Preclinical animal models indicate its potential usefulness in mitigating inflammatory responses associated with neuropsychiatric conditions triggered by stress
Apexbio Technology LLC CEP-18770 847499-27-8 10mM (in 1mL DMSO)
CEP-18770 (CAS 847499-27-8) is a reversible boronic acid-based inhibitor of proteasome chymotrypsin-like activity It specifically targets the proteasome s P2 threonine protease subunit reducing NF- B signaling and the expression of downstream effectors With a reported IC50 of 3 8 nM CEP-18770 induces apoptosis in multiple myeloma cell lines and inhibits osteoclastogenesis and angiogenesis via suppression of RANKL signaling Research supports its potential use in oncology particularly for multiple myeloma showing selective cytotoxicity sparing normal epithelial and bone marrow-derived cells
Apexbio Technology LLC Riociguat 625115-55-1 10mM (in 1mL DMSO)
Riociguat (CAS 625115-55-1) chemically known as BAY 63-2521 is a small-molecule stimulator of soluble guanylate cyclase (sGC) It directly activates sGC independently and also enhances the enzyme s sensitivity to nitric oxide (NO) leading to elevated cyclic guanosine monophosphate (cGMP) levels Elevated cGMP induces smooth muscle relaxation and vasodilation Riociguat has been examined clinically for potential therapeutic roles in chronic thromboembolic pulmonary hypertension (CTEPH) and pulmonary arterial hypertension (PAH)
Apexbio Technology LLC Belinostat (PXD101) 414864-00-9 10mM (in 1mL DMSO)
Belinostat (PXD101) is a hydroxamic acid-based inhibitor targeting histone deacetylase (HDAC) enzymes Its mechanism involves the suppression of HDAC enzymatic activity leading to increased acetylation of histone proteins H3 and H4 within cells In biochemical assays using Hela cell extracts belinostat exhibits inhibitory activity against HDAC with an IC50 value of approximately 27 nM In tumor cell culture models belinostat induces cytotoxicity and represses cellular proliferation with reported IC50 values ranging roughly from 0 5 M to 10 M varying by cell type and origin making it suitable for research on epigenetic modulation in oncology specifically in studies of bladder prostate and related cancer cell lines
Apexbio Technology LLC D4476 301836-43-1 10mM (in 1mL DMSO)
D4476 (CAS 301836-43-1) is a selective cell-permeable inhibitor of casein kinase 1 (CK1) and ALK5 exhibiting IC50 values of 0 3 M for CK1 and 0 5 M for ALK5 (at 0 1 mM ATP in vitro) It likely acts via ATP-competitive inhibition of CK1 showing minimal to no significant inhibitory activity against SAPK2a/p38 PKB or SGK Treatment with D4476 inhibits CK1-mediated phosphorylation of FOXO1a (Ser322 and Ser325) and RhoB (Ser185) in H4IIE and HeLa cells respectively impacting downstream processes such as nuclear export dynamics and actin cytoskeleton regulation Additionally it induces partial p53-dependent growth arrest in HCT116 cells
Apexbio Technology LLC RG2833 1215493-56-3 10mM (in 1mL DMSO)
RG2833 (CAS 1215493-56-3) is a small-molecule inhibitor targeting histone deacetylase (HDAC) In neuronal cell models RG2833 elevates frataxin (FXN) mRNA and protein expression by modifying epigenetic regulation at the FXN locus Studies conducted on peripheral blood mononuclear cells (PBMCs) from patients demonstrated reduced HDAC activity enhanced histone H3 lysine 9 acetylation and elevated FXN mRNA levels upon RG2833 treatment Research utilizing induced pluripotent stem cell (iPSC)-derived neuronal cultures further supports HDAC inhibition as the mechanism underlying RG2833-mediated FXN upregulation This molecule is primarily explored for epigenetic studies in Friedreich s ataxia research
Apexbio Technology LLC RO5126766(CH5126766) 946128-88-7 10mM (in 1mL DMSO)
RO5126766 (CH5126766 CAS 946128-88-7) is a dual Raf/MEK inhibitor that targets the RAS/RAF/MEK/ERK signaling pathway involved in cellular proliferation survival and differentiation By inhibiting RAF-dependent MEK1 phosphorylation and subsequent MEK-mediated ERK activation RO5126766 suppresses downstream signaling In vitro kinase assays show IC50 values of 0 0082 0 056 M for MEK1 phosphorylation and 0 16 M for MEK1-induced ERK2 activation Studies in KRAS-mutant cancer cell lines such as HCT116 and NCI-H460 demonstrate that RO5126766 blocks MEK and ERK phosphorylation effectively inducing cell cycle arrest at the G1 stage Thus RO5126766 serves as a valuable research tool for investigating tumor biology driven by MAPK signaling dysregulation
Apexbio Technology LLC PF-04449913 1095173-27-5 10mM (in 1mL DMSO)
PF-04449913 (CAS 1095173-27-5) is an orally bioavailable small molecule inhibitor targeting smoothened (SMO) a critical component of the Hedgehog (Hh) signaling pathway Activation of SMO by Hh ligands typically initiates signaling cascades involving Gli transcription factors influencing cellular proliferation and oncogenesis PF-04449913 inhibits SMO activity with an IC50 of 5 nM thereby suppressing downstream Gli-mediated signaling Preclinical pharmacokinetic studies demonstrated favorable properties including a half-life of approximately 30 hours 55% oral bioavailability low plasma clearance (1 03 mL/min/kg) and moderate distribution (2 7 L/kg) PF-04449913 is actively explored in cancer research contexts
Apexbio Technology LLC SB202190 (FHPI) 152121-30-7 10mM (in 1mL DMSO)
SB202190 (FHPI CAS 152121-30-7) is a selective MAPK inhibitor targeting specifically the p38 isoforms and with reported IC50 values of approximately 50 nM and 100 nM respectively Through inhibition of p38 signaling SB202190 has been observed to stimulate the proliferation of leukemia cell lines including THP-1 and MV4-11 via activation of ERK and C-Raf phosphorylation pathways Additionally SB202190 modulates cellular responses to genotoxic stress such as hydroxyurea-induced premature chromosome condensation and influences histone acetylation status (Lys5 of histone H4) in plant systems Such activities render SB202190 useful for investigating MAP kinase-dependent pathways in cell proliferation and stress responses
Apexbio Technology LLC Pirfenidone 53179-13-8 10mM (in 1mL DMSO)
Pirfenidone (CAS 53179-13-8) is a small molecule antifibrotic agent exhibiting anti-inflammatory properties Mechanistically pirfenidone reduces levels of pro-inflammatory mediators notably TNF- via translational regulation independent of MAPK pathway activation It suppresses TGF- -mediated signaling and extracellular matrix protein production contributing to decreased fibrotic responses in cellular and animal models In vivo pirfenidone administration mitigates fibrosis and inflammatory cytokine expression in tissues such as lung liver and kidney Clinically pirfenidone is investigated primarily for idiopathic pulmonary fibrosis demonstrating reductions in fibrosis progression and improved functional parameters