Notch Inhibitor

BMS-871 is an orally active pan-Notch inhibitor with IC₅₀ values ​​of 4/1/4/3 nM for Notch1/2/3/4, respectively. BMS-871 significantly inhibited the proliferation of TALL-1 and MDA-MB-157 cells and demonstrated significant antitumor activity in T-acute lymphoblastic leukemia and triple-negative breast cancer xenograft models. BMS-871 can be used to study leukemia and breast cancer.

XRF-1021 is an orally active HIPK2 inhibitor (IC₅₀ = 0.18 μM). XRF-1021 reduces the expression of fibrotic markers in TGF-β1 stimulated NRK-49F and HK-2 cells, including Fibronectin, Collagen I and α-SMA. XRF-1021 blocks TGF-β, NF-κB, p53, Wnt/β-catenin, and Notch signaling. XRF-1021 reduces renal injury and fibrosis in vivo. XRF-1021 can be used for the research of chronic kidney disease.

IMR-1A (Standard) is the analytical standard of IMR-1A. This product is intended for research and analytical applications. IMR-1A, a acid metabolite of IMR-1, is a Notch inhibitor with an IC50 of 0.5 μM. IMR-1A has a 50-fold increase in potency with respect to IMR-1. IMR-1 can metabolize in vivo to IMR-1A[1].

Procyanidin B2, 3,3'-di-O-gallate is an active constituent. Procyanidin B2, 3,3'-di-O-gallate can be isolated from grape seed extract (GSE) procyanidin mix. Procyanidin B2, 3,3' -di-o-gallate target cancer stem cells (CSCs) in prostate cancer (PCa). Procyanidin B2, 3,3'-di-O-gallate targets both unsorted and sorted CSCs at lower doses. Procyanidin B2, 3,3'-di-O-gallate strongly suppresses the constitutive as well as Jagged1 (Notch1 ligand)-induced activated Notch1 pathway.

SAHM1 TFA is a Notch pathway inhibitor. SAHM1 TFA stabilizes hydrocarbon-stapled alpha helical peptide. SAHM1 TFA targets the protein-protein interface and prevents Notch complex assembly.

MRK 003 is an orally active γ-secretase inhibitor. MRK 003 targets the Notch signaling pathway by blocking the proteolytic cleavage of Notch receptors. MRK 003 inhibits tumor cell proliferation, induces apoptosis, downregulates anti-apoptotic proteins, upregulates phosphorylated Akt, suppresses angiogenesis, and overcomes microenvironment-mediated proliferative protection. MRK 003 can be used in research related to lung cancer, multiple myeloma, non-Hodgkin's lymphoma, pancreatic ductal adenocarcinoma, glioblastoma, and breast cancer.

DAPM is a Notch pathway inhibitor with anticancer activity and antiproliferative effects. DAPM effectively inhibits tubular adenoma development by inhibiting cell proliferation and inducing the expression of Krüppel-like factor 4 (KLF4) and p21 in human colon cancer cells.

PF-06650808 Antibody (Anti-NOTCH3 mAb hu28) is an IgG1-kappa Notch3-targeting antibody. PF-06650808 Antibody is the antibody component of the antibody-drug conjugate (ADC) PF-06650808. PF-06650808 Antibody can be used for the research of advanced breast cancer, advanced solid tumors.

GSI-18 is a γ-secretase inhibitor with anticancer activity. GSI-18 inhibits the attachment-free growth of pancreatic cancer cells by inhibiting Notch signaling.

CP-654577 is a selective ErbB2 inhibitor with an IC₅₀ of 11 nM. CP-654577 downregulates the Notch1 signaling pathway. CP-654577 upregulates p27^kip1, reduces the levels of Cyclins D and E, and inhibits G1 phase progression of the cell cycle. CP-654577 induces cell Apoptosis, downregulates activated Akt, and suppresses tumor growth in athymic mice. CP-654577 can be used in breast cancer-related research.

NEURL1B-IN-1 is a molecular glue-like NEURL1B degrader with a Kd value of 46.2 nM. NEURL1B-IN-1 binds to Arg422 within the NHR2 domain of NEURL1B, triggers its autoubiquitination and proteasomal degradation, disrupts its interaction with DLL1, and attenuates the Notch signaling pathway. NEURL1B-IN-1 induces cell cycle arrest and apoptosis, and inhibits migration of hepatocellular carcinoma cells. NEURL1B-IN-1 is applicable to research related to hepatocellular carcinoma.

Tangeretin (Standard) is the analytical standard of Tangeretin. This product is intended for research and analytical applications. Tangeretin (Tangeritin), a flavonoid from citrus fruit peels, has been proven to play an important role in anti-inflammatory responses and neuroprotective effects in several disease models, and is a Notch-1 inhibitor.

Anti-Mouse Delta-like protein 1/DLL1 Antibody (HMD1-5) is an anti-mouse Delta-like protein 1/DLL1 IgG monoclonal antibody. Anti-Mouse Delta-like protein 1/DLL1 Antibody (HMD1-5) can reverse the inhibition of Treg cells. Anti-Mouse Delta-like protein 1/DLL1 Antibody (HMD1-5) can inhibit the upregulation of GLT-1 expression induced by endothelial cells. Anti-Mouse Delta-like protein 1/DLL1 Antibody (HMD1-5) reduces autoimmune response by reducing B cell activation. Anti-Mouse Delta-like protein 1/DLL1 Antibody (HMD1-5) can be used for research on inflammation conditions such as lupus nephritis.

Narvesiran is a notch-regulated ankyrin repeat protein (NRARP) synthesis reducer, angiogenesis inhibitor.

MEDI0639 (21H3RK) is a human monoclonal antibody (mAb) targeting DLL4. MEDI0639 inhibits Notch1 binding to Dll4. MEDI0639 reverses Notch1-mediated growth inhibition of human umbilical vein endothelial cells in vitro. MEDI0639 promotes human angiogenesis and reduces the number of vessels covered by smooth muscle actin-positive mural cells. MEDI0639 can be used in Small cell lung cancer and solid tumors research.

Avagacestat (Standard) is the analytical standard of Avagacestat. This product is intended for research and analytical applications. Avagacestat (BMS-708163) is a potent inhibitor of γ-secretase, with IC50s of 0.27 nM and 0.30 nM for Aβ42 and Aβ40 inhibition; Avagacestat (BMS-708163) also inhibits NICD (Notch IntraCellular Domain) with IC50 of 0.84 nM and shows weak inhibition of CYP2C19, with IC50 of 20 μM. Avagacestat can be used for Alzheimer disease research.

AMG-119 is a humanized IgG1 monoclonal antibody that targets delta-like ligand 3 (DLL3). AMG-119 can be used for the study of relapsed/refractory (R/R) small cell lung cancer (SCLC). Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001).

Rhodojaponin VI is an orally active diterpenoid compound found in hododendron molle G. Don
(Ericaceae) (RM). Rhodojaponin VI binds rat N-Ethylmaleimide-sensitive fusion (NSF) with a Kd of 1.03 μM. Rhodojaponin VI blocks the MDM2-Notch1 signalling pathway by reducing MDM2 and Notch1 expression. Rhodojaponin VI indirectly reduces Cav_2.2 current intensity by inhibiting NSF-mediated Cav2.2 trafficking. Rhodojaponin VI alleviates glomerulonephritis progression and podocyte injury in passive heymann nephritis rats. Rhodojaponin VI also has antinociceptive effects. Rhodojaponin VI can be used for the researches of heymann nephritis and pain.

RO4929097 (Standard) is the analytical standard of RO4929097 (HY-11102). This product is intended for research and analytical applications. RO4929097 (RG-4733) is an orally active γ secretase inhibitor with an IC₅₀ of 4 nM, inhibiting cellular processing of Aβ40 and Notch with EC₅₀ of 14 nM and 5 nM, respectively.

Anti-Mouse Delta-like protein 4/DLL4 Antibody (HMD4-2) is an anti-mouse Delta-like protein 4/DLL4 IgG monoclonal antibody. Anti-Mouse Delta-like protein 4/DLL4 Antibody (HMD4-2) can reduce angiogenesis and density by blocking the DLL4-Notch signaling pathway. Anti-Mouse Delta-like protein 4/DLL4 Antibody (HMD4-2) reduces inflammatory response by decreasing NF-κB activity and pro-inflammatory factors (IL-1β, iNOS, IL-6) levels. Anti-Mouse Delta-like protein 4/DLL4 Antibody (HMD4-2) can inhibit Th17 cell differentiation and IL-17A production. Anti-Mouse Delta-like protein 4/DLL4 Antibody (HMD4-2) can reduce macrophage infiltration and alleviate insulin resistance. Anti-Mouse Delta-like protein 4/DLL4 Antibody (HMD4-2) can be used for researches on inflammation, metabolic conditions and cancer such as atherosclerosis, pancreatic cancer and asthma.