About 31 results found for searched term "INI-43" (0.111 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M1744 | ARRY-162 (Binimetinib) | MEK |
| MEK-162; Binimetinib; ARRY-438162 | ||
| ARRY-162 (MEK-162; Binimetinib) is a selective, potent inhibitor of MEK and cellular pERK with IC50 of 12 nM and 11 nM, respectively. | ||
| M8730 | INI-43 | Others |
| INI-43 is a cell penetrant and potent inhibitor of Kpnb1-mediated nuclear import that cancer cell death via a G2–M cell cycle arrest followed by apoptosis. | ||
| M1749 | Gefitinib | EGFR/HER2 |
| ZD-1839, Iressa | ||
| Gefitinib (ZD1839) is an EGFR tyrosine kinase and Akt phosphorylation inhibitor. Gefitinib significantly down-regulates CD47 expression and increases DC phagocytosis in non-small cell lung cancer cells such as PC9, H1437 and H1573. Gefitinib combined with CD47 antibody can enhance the phagocytosis of macrophages. | ||
| M1784 | Icotinib | EGFR/HER2 |
| BPI-2009H | ||
| Icotinib (BPI-2009H) is a potent and novel epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) with an IC50 of 5 nM. Iconitib inhibits the proliferation of A431 and BGC-823 A549, H460 and KB cell lines with IC50s of 1, 4.06, 12.16, 16.08, 40.71 μM. | ||
| M1956 | Apatinib mesylate | VEGFR/PDGFR |
| Rivoceranib mesylate; YN968D1 | ||
| Apatinib is a small-molecule multitargeted tyrosine kinase inhibitor of VEGFR2 with an IC50 of 2.43 nM. | ||
| M2800 | KY02111 | Others |
| KY02111 is a widely used small molecule that boosts cardiomyogenesis. Chemical genetics of KY02111 identified squalene synthase (SQS) as a molecular target of KY02111. By disrupting the interaction of SQS with cardiac ER-membrane protein TMEM43, KY02111 impairs TGFβ/SMAD signaling and recapitulates the clinical mutation of TMEM43 that causes an inherited heart disease. | ||
| M2945 | Pimozide | Dopamine Receptor |
| R6238 | ||
| Pimozide is an antagonist of 6-hydroxyapatide against 6-hydroxyapatide, with Ki values of 1.4 nM, 2.5 nM and 588 nM for 6-hydroxyapatide, D3 and D1 receptors, respectively. Pimozide also has a high affinity for α1-adrenoceptor. Ki value is 39 nM. Pimozide is also an inhibitor of STAT3 and STAT5, and piperimidate triggers ADCD in glioblastoma cell lines (LN-229, MZ-54, GOS-3 and U343) by inducing dephosphorylation and inactivation of mTORC1. | ||
| M5048 | Presatovir | RSV |
| GS-5806 | ||
| Presatovir is a novel, orally bioavailable RSV fusion inhibitor, against a wide range of RSV A and B clinical isolates (mean EC50 = 0.43 nM). | ||
| M6219 | Rituximab | CD20 |
| IDEC-C2B8 | ||
| Rituximab is a chimeric anti-CD20 mAb that binds the CD20 antigen on B cells with a binding affinity of 5 nM, MW: 143.86 KD. | ||
| M6297 | Upadacitinib | JAK |
| ABT-494 | ||
| Upadacitinib (ABT-494) is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib (ABT-494) displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib (ABT-494) can be used for several autoimmune disorders research. | ||
| M13660 | eIF4A3-IN-1 | Others |
| eIF4A3-IN-1 (compound 53a) is a selective eukaryotic initiation factor 4A3 (eIF4A3) inhibitor (IC50=0.26 μM; Kd=0.043 μM), which binds to a non-ATP binding site of eIF4A3 and shows significant cellular nonsense-mediated RNA decay (NMD) inhibition at 10 and 3 μM and can be as a probe for further study of eIF4A3, the exon junction complex (EJC), and NMD. | ||
| M20515 | Emedastine | Histamine Receptor |
| Emedastine is a potent, high affinity histamine H1-receptor-selective antagonist with Ki of 1.3 ±0.1 nM for H1-receptors while considerably weaker at H2- (K1 = 49,067 ± 11,113 nM) and H3-receptors (Ki = 12,430 ± 1,282 nM). | ||
| M20730 | KGA-2727 | SGLT |
| KGA-2727 is a potent, selective, high-affinity inhibitor of sodium glucose cotransporter 1 (SGLT1) with Ki of 97.4 nM and 43.5 nM for human SGLT1 and rat SGLT1, respectively. The selectivity ratios (Ki for SGLT2/Ki for SGLT1) of KGA-2727 are 140 (human) and 390 (rat). KGA-2727 exhibits antidiabetic efficacy in rodent models. | ||
| M20997 | Remogliflozin etabonate (GSK189075) | SGLT |
| Remogliflozin etabonate (GSK189075) is an orally active, selective and low-affinity inhibitor of sodium glucose cotransporter (SGLT2) with Ki of 1950 nM, 2140 nM, 43100 nM, 8570 nM for hSGLT2, rSGLT2, hSGLT1, rSGLT1, respectively. Remogliflozin etabonate exhibits antidiabetic efficacy in rodent models. | ||
| M21063 | LEO 134310 | Others |
| LEO 134310 is a non-steroidal, selective glucocorticoid receptor (GR) agonist that is being studied in the first phase of plaque psoriasis.LEO 134310 has shown high affinity (EC50 of 14 nM) in GR binding assays.LEO 134310 can be used in dermatological conditions. | ||
| M22527 | Cinchonidine | Alkaloids |
| α-Quinidine | ||
| Cinchonidine (α-Quinidine) is a cinchona alkaloid found in Cinchona officinalis and Gongronema latifolium. Cinchonidine (α-Quinidine) is a weak inhibitor of serotonin transporter (SERT) with Ki values of 330, 4.2, 36, 196, 15 μM for dSERT, hSERT, hSERT I172M, hSERT S438T, hSERT Y95F, respectively. | ||
| M24827 | Talacotuzumab | IL Receptor/Related |
| JNJ 56022473; CSL 362 | ||
| Talacotuzumab (JNJ 56022473; CSL 362) is an IgG1-type fully humanized, CD123-neutralizing monoclonal antibody containing a modified Fc structure. Talacotuzumab has KDs of 0.43 nM, 188 nM, 46 nM, 16.8 nM for CD123, CD32b/c, CD16-158F, CD16-158V, respectively. Talacotuzumab inhibits IL-3 binding to CD123, antagonizing IL-3 signaling in target cells. Talacotuzumab has mutated the Fc region to increase affinity for CD16 (FcγRIIIa), thereby enhancing antibody-dependent cell-mediated cytotoxicity (ADCC). Talacotuzumab is highly effective in vivo reducing leukemic cell growth in acute myeloid leukemia (AML) xenograft mouse models. | ||
| M25580 | PPTN hydrochloride | P2 Receptor |
| PPTN hydrochloride is a potent, high-affinity, competitive and highly selective P2Y14 receptor antagonist with a KB value of 434 pM. | ||
| M28208 | Naldemedine tosylate | Opioid Receptor |
| S-297995 tosylate | ||
| Naldemedine (S-297995) tosylate is an orally active μ-opioid receptor antagonist (PAMORA). Naldemedine tosylate shows potent binding affinities (Ki=0.34, 0.43, 0.94 nM, respectively) and antagonist activities (IC50=25.57, 7.09, 16.1 nM, respectively) for recombinant human μ-, δ-, and κ- opioid receptors. Naldemedine can be used in opioid-induced constipation (OIC) research. | ||
| M28575 | AB-MECA | Adenosine Receptor |
| AB-MECA is a high affinity A3 adenosine receptor agonist with a binding Ki of 430.5 nM for human A3 receptors in CHO cells. AB-MECA can enhance plasma histamine level. | ||
| M28611 | Benzomalvin A | Neurokinin Receptor |
| Benzomalvin A is a potent antagonist of neurokinin receptor isolated from Penicillium sp. Benzomalvin A shows inhibitory activity against substance P with Ki values of 12, 42 and 43 μM at the guinea pig, rat and human neurokinin NK1 receptors, respectively. | ||
| M29485 | Tuspetinib | FLT3 |
| HM43239 | ||
| Tuspetinib (HM43239) is an orally active and selective FLT3 inhibitor with IC50s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. Tuspetinib inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib inhibits the proliferation and induces the apoptosis of leukemic cells. | ||
| M29543 | MS31 | Epigenetic Reader Domain |
| MS31 is a potent, highly affinity and selective fragment-like methyllysine reader protein spindlin 1 (SPIN1) inhibitor. MS31 potently inhibits the interactions between SPIN1 and H3K4me3 (IC50=77 nM, AlphaLISA; 243 nM, FP). MS31 selectively binds Tudor domain II of SPIN1 (Kd=91 nM). MS31 potently inhibits binding of trimethyllysine-containing peptides to SPIN1. MS31 is not toxic to nontumorigenic cells. | ||
| M30192 | Org 43553 | Others |
| Org 43553 is an orally active and low molecular weight (LMW) luteinizing hormone receptor (LH-R) agonist. Org 43553 shows agonistic activity to human LH and FSH receptors with EC50 values of 3.7 and 110 nM, respectively. Org 43553 can be used for the research of endocrine. | ||
| M30336 | Integrin Antagonists 27 | Integrin |
| Integrin Antagonists 27 is a small molecule integrin αvβ3 antagonist with binding affinity of 18 nM, as s novel anticancer agent. Target: Integrin in vitro: Integrin Antagonists 27 is treated with a panel of cancer cell-lines (breast cancer cell line MDA-MB-435, breast cancer cell lines MCF-7, mouse fibroblast NIH3T3, ovarian cancer cell line HEY, lung cancer cell line NCI-H1975) with all IC50 of >20 uM. | ||
| M30642 | 1,8-Dihydroxy-4,5-dinitroanthraquinone | Anti-infection |
| ARDP0006; DHDNE | ||
| 1,8-Dihydroxy-4,5-dinitroanthraquinone (ARDP0006; DHDNE) is a potent inhibitor of serine proteinase NS2B/3, the dengue viral protein. 1,8-Dihydroxy-4,5-dinitroanthraquinone has intermolecular proteinase activity and viral inhibition ability with IC50s of 432 μM and 4.2 μM, respectively. Meanwhile 1,8-Dihydroxy-4,5-dinitroanthraquinone inhibits NS2B/3 cleavage in BHK-21 cells at a dose ranging from 4.2 μM to 432 μM. | ||
| M30819 | Isogambogenic acid | Others |
| Isogambogenic acid is a natural product that can be isolated from Resina Garciniae. Isogambogenic acid has cytotoxicity to cancer cell lines with IC50 values of 0.4327-5.942 μmol/L. | ||
| M30898 | Naldemedine | Opioid Receptor |
| S-297995 | ||
| Naldemedine (S-297995) is an orally active μ-opioid receptor antagonist (PAMORA). Naldemedine shows potent binding affinities (Ki=0.34, 0.43, 0.94 nM, respectively) and antagonist activities (IC50=25.57, 7.09, 16.1 nM, respectively) for recombinant human μ-, δ-, and κ- opioid receptors. Naldemedine can be used in opioid-induced constipation (OIC) research. Naldemedine is predicted to bind to 3CLpro encoded by SARS-CoV2 genome. | ||
| M31013 | MS31 trihydrochloride | Epigenetic Reader Domain |
| MS31 trihydrochloride is a potent, highly affinity and selective fragment-like methyllysine reader protein spindlin 1 (SPIN1) inhibitor. MS31 trihydrochloride potently inhibits the interactions between SPIN1 and H3K4me3 (IC50=77 nM, AlphaLISA; 243 nM, FP). MS31 trihydrochloride selectively binds Tudor domain II of SPIN1 (Kd=91 nM). MS31 trihydrochloride potently inhibits binding of trimethyllysine-containing peptides to SPIN1, and is not toxic to nontumorigenic cells. | ||
| M31166 | Lunasin TFA | Peptides |
| Lunasin TFA is a bioactive peptide isolated from soybeans containing 43 amino acids that inhibits the FAK/ERK/NF-κB signaling pathway through direct binding to α5β1 integrins, resulting in antioxidant, anti-inflammatory, and anti-cancer activities. | ||
| M31316 | DiaPep277 | Immunology/Inflammation |
| DiaPep 277 | ||
| DiaPep277 is a peptide containing 24 amino acids based on residues 437 to 460 of Heat Shock Protein 60 (HSP60) for studies related to the immune system in type 1 diabetes. | ||
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