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Bleomycin hydrochloride is a DNA synthesis inhibitor. Bleomycin hydrochloride is a DNA damaging agent. Bleomycin hydrochloride is an antitumor antibiotic .
Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
Crocin (Crocin I) is an orally active natural product that can be isolated from the stigma of Crocus sativus. Crocin inhibits tumor cell proliferation and promotes apoptosis through JAK pathway. Crocin has anti-inflammatory, antioxidant and antitumor activities .
Fresolimumab (GC1008) is a human monoclonal antibody against TGF-β that neutralizes all mammalian active subtypes of TGF-β. The binding affinity of Fresolimumab to TGF-β2 is 1.8 nM. Fresolimumab improves Bleomycin (HY-108345)-induced acute lung injury. Fresolimumab radiolabeled with 89Zr can be used for PET analysis of TGF-β expression, antibody uptake and organ distribution. Fresolimumab can be used in the study of cancer, osteogenesis imperfecta, fibrosis and kidney disease .
AR-C118925XX is a selective P2Y2 receptor antagonist. AR-C118925XX inhibits ATP-induced IL-6 production and phosphorylation of p38. AR-C118925XX also inhibits Bleomycin (HY-108345)-induced dermal fibrosis in mice. AR-C118925XX also inhibits ATP-induced tumor growth .
Bleomycin A5 (Pingyangmycin) is a glycopeptide antibiotic with multiple biological activities, which can be isolated from Streptomyces. Bleomycin A5 exerts cytotoxic effects by binding to Fe 2+ to form a complex, inducing single-strand and double-strand DNA breaks, and inhibiting DNA replication. Bleomycin A5 inhibits Drp1-mediated mitochondrial fission and suppresses PINK1/Parkin pathway-mediated mitophagy, ultimately triggering mitochondria-mediated cellular apoptosis. Bleomycin A5 can be used in cancer research .
Dermatan sulphate sodium is an oral active glycosaminoglycan and thrombin inactivator with antithrombotic activity. It selectively catalyzes the heparin cofactor II-mediated inactivation of thrombin without interacting with antithrombin III. Dermatan sulphate sodium promotes stem cell differentiation, exhibits high bioavailability, and alleviates pulmonary fibrosis injury induced by Bleomycin (HY-108345). Dermatan sulphate sodium can be used in research related to cardiovascular diseases, inflammation, and stem cell differentiation .
Bleomycin is a glycopeptide antibiotic. Bleomycin has potent antitumour activities against a range of lymphomas, head and neck cancers and germ-cell tumours. Bleomycin can be used for the research of cancer and chemotherapy .
CCG-232601 (compound 8f) is a potent and orally active Rho/MRTF/SRF transcriptional pathway inhibitor. CCG-232601 inhibits the development of Bleomycin-induced dermal fibrosis in mice. CCG-232601 has the potential for the research of antifibrotic for systemic scleroderma .
AX-202 is a humanized IgG4 monoclonal antibody targeting S100A4. AX-202 neutralizes the activity of S100A4. AX-202 effectively reverses established fibrosis and reduces inflammation and fibrosis-related biomarkers in a mouse model of skin fibrosis. AX-202 is applicable for the research of fibrotic and inflammatory diseases .
Licoricesaponin G2 is an orally active component found in Licorice. Licoricesaponin G2 significantly ameliorates Bleomycin (HY-108345)-induced pulmonary fibrosis by inhibiting the TNF-α signaling pathway, reducing epithelial-mesenchymal transition, and decreasing extracellular matrix deposition. Licoricesaponin G2 inhibits cancer cells proliferation, migration, inhibits PI3K/AKT/mTOR signaling pathway and increases ROS production. Licoricesaponin G2 can be used for the research of lung cancer and pulmonary fibrosis .
Rosmantuzumab (OMP-131R10) is an anti-R-spondin 3 (RSPO3) humanized monoclonal antibody. Rosmantuzumab can be used for the research of advanced telapsed and refractory solid tumors .
Phleomycin D1 (PLM D1), a glycopeptide antibiotic, is a member of the Bleomycin/Phleomycin family. Phleomycin D1 causes cell death by binding and cleaving DNA. Phleomycin D1 induces cell cycle arrest at S phase .
ATUX-1215 is an activator of protein phosphatase 2A (PP2A). ATUX-1215 reduced the phosphorylation of ERK, p38, JNK, and Akt and the secretion of IL-12p70, GM-CSF, and IL1α in Bleomycin hydrochloride (HY-17565A)-treated animals. ATUX-1215 can slow the progression of lung fibrosis .
L-Gulose is a rare L-aldohexose in nature, and serves as a key structural unit for the synthesis of a variety of important active compounds (e.g., vitamin C) .
Bleomycin A5 (Pingyangmycin) hydrochloride is a glycopeptide antibiotic with multiple biological activities, which can be isolated from Streptomyces. Bleomycin A5 hydrochloride exerts cytotoxic effects by binding to Fe 2+ to form a complex, inducing single-strand and double-strand DNA breaks, and inhibiting DNA replication. Bleomycin A5 hydrochloride inhibits Drp1-mediated mitochondrial fission and suppresses PINK1/Parkin pathway-mediated mitophagy, ultimately triggering mitochondria-mediated cellular apoptosis. Bleomycin A5 hydrochloride can be used in cancer research .
Neotuberostemonine, one of the main antitussive alkaloids in the root of Stemona tuberosa Lour, attenuates bleomycin-induced pulmonary fibrosis by suppressing the recruitment and activation of macrophages .
Crocin (Standard) is the analytical standard of Crocin. This product is intended for research and analytical applications. Crocin (Crocin I) is an orally active natural product that can be isolated from the stigma of Crocus sativus. Crocin inhibits tumor cell proliferation and promotes apoptosis through JAK pathway. Crocin has anti-inflammatory, antioxidant and antitumor activities .
IV-255 is a selective small molecule inhibitor of the BRG1 bromodomain. IV-255 increases the extent of DNA damage induced by Temozolomide (HY-17364) and Bleomycin (HY-108345). IV-255 inhibits the invasiveness of GBM cells. IV-255 enhances Temozolomide-induced cell death and the apoptosis-inducing activity of Temozolomide .
NZ-97 is an inhibitor for dipeptidyl peptidase 4 (DPP4) with an IC50 of 18 nM. NZ-97 exhibits a low initial plasma exposure with Cmax of 0.13 µM, which is eliminated in 8 h. NZ-97 ameliorates damage in the Lipopolysaccharides (HY-D1056)-induced lung injury and Bleomycin (HY-108345)-induced lung fibrosis in mice model .
TGFβ-IN-2 is an orally active TGF-β inhibitor. TGFβ-IN-2 suppresses the TGF-β-induced protein expression of COL1A1, α-SMA, and p-Smad3 in vitro. TGFβ-IN-2 demonstrates excellent anti-fibrotic efficacy in Bleomycin (HY-108345)-induced pulmonary fibrosis model. TGFβ-IN-2 can be used for the study of pulmonary fibrosis .
ROCK2-IN-12 (Compound A25) is a selective ROCK2 inhibitor with an IC50 of 7.0 nM for ROCK2 over ROCK1. ROCK2-IN-12 has potent antifibrotic effects via the TGF-β/Smad and ROCK2/STAT3 signaling pathways. ROCK2-IN-12 significantly reduces collagen deposition and reverses fibrotic progression in Bleomycin (HY-108345)-induced pulmonary fibrosis (PF) mouse models. ROCK2-IN-12 can be used for lung diseases like pulmonary fibrosis research .
GK444 (Compound 15a) is a HDAC1/2 inhibitor (IC50: 100 and 92 nM for HDAC1/2 respectively). GK444 inhibits Caco-2 cells with IC50 of 4.1 μM. GK444 also reduces TGF-β1 induced COL1A1 mRNA levels in primary normal human lung fibroblasts. GK444 inhibits Bleomycin (HY-108345)-induced lung fibrosis in mice .
Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC50 values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice .
Peplomycin (Bleomycin PEP) is an analog of Bleomycin (HY-108345) and an antitumor antibiotic. Peplomycin exhibits potent antitumor activity and relatively low pulmonary toxicity. Peplomycin can induce various skin abnormalities and trigger apoptosis in SSCKN cells of oral squamous cell carcinoma. Peplomycin can also induce pulmonary fibrosis. Peplomycin is applicable for the research of tumors, pulmonary fibrosis and other related diseases .
N4Py is a pentadentate ligand, that forms a stable complex with metal ions, such as iron, platinum, and copper. N4py mimics the metal binding domains of iron-dependent antibiotics like Bleomycin(HY-17565), forms the DNA-cleaving FeII-N4Py complexes, generates reactive oxygen species (ROS), and causes oxidative damage in cells. N4py can be used in cancer research .
Aucuparin, a natural product found in Sorbus aucuparia, inhibits pulmonary fibrosis in a bleomycin (HY-108345)-induced lung fibrosis mouse model. Aucuparin has anti-inflammatory activity and can inhibit the activation of inflammatory factors by TGF-β .
Linvemastat (Compound FC-4) is an orally active MMP-12 inhibitor (IC50: < 10 nM) with high selectivity of MMP-1, -2, -3, -7, -9, -10 and -14. Linvemastat significantly attenuates lung fibrosis in Bleomycin (HY-108345) induced unilateral lung fibrosis mice model and potently reduces kidney damage, interstitial inflammation or fibrosis in kidney fibrosis model of unilateral ureteral occlusion. Linvemastat can be used for inflammatory diseases research, such as idiopathie pulmonary fibrosis (IPF), inflammatory bowel disease (IBD) and asthma .
Bleomycin B2 (Phleomycin D2) is an anti-cancer agent that targets DNA. Bleomycin B2 causes DNA strand breaks, thereby inhibiting the growth and proliferation of cancer cells. Bleomycin B2 is promising for research of cancers .
Demethyl bleomycin A2 is a Bleomycin (HY-108345) congener. The DNA cleavage of demethyl bleomycin A2 is insensitive to the presence of 5-Methylcytidine (HY-113135) .
Antifibrotic agent 1 is an orally active anti-idiopathic pulmonary fibrosis (IPF) agent. Antifibrotic agent 1 effectively attenuates IPF-related processes, including TGF-β induced EMT and FMT processes, as well as pro-fibrotic M2 polarization. Antifibrotic agent 1 selectively inhibits CSF-1R, PDGFR-α and Src family kinases (SFKs), while sparing VEGFRs, FGFRs and Abl to minimize off-target toxicity. Antifibrotic agent 1 has potent anti-fibrotic activity in Bleomycin (BLM) (HY-108345)-induced pulmonary fibrosis mice model .
Antiflammin-1 is an anti-inflammatory peptide 1 (MQMKKVLDS). Antiflammin-1 is a derivative of uteroglobin. Antiflammin-1 has anti-inflammatory and antifibrotic actions in bleomycin (HY-108345)-induced lung injury .
Entrectinib (Standard) is the analytical standard of Entrectinib. This product is intended for research and analytical applications. Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
Entrectinib-d4 (NMS-E628-d4; RXDX-101-d4) is the deuterium labeled Entrectinib (HY-12678). Entrectinib is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
ATX inhibitor 26 is an Autotaxin (ATX) inhibitor with an IC50 of 57 nM in human plasma. ATX inhibitor 26 inhibits cell migration and collagen gel contraction. ATX inhibitor 26 has significant anti-fibrotic effects, reducing collagen deposition in a Bleomycin (BLM) (HY-108345)-induced pulmonary fibrosis model .
dual FXR/PPARδ agonist-2 is a FXR/PPARδ dual agonist through hybridation of FXR agonist GW-4064 and PPARδ agonist GW-0742.dual FXR/PPARδ agonist-2 displays potent dual-target activities with a FXR agonistic EC50 of 12.28 nM and 69 % PPARδ activation at 100 nM. dual FXR/PPARδ agonist-2 shows anti-fibrotic effects in pulmonary fibrosis mouse model .
TM5007 is a poent and orally active inhibitor of plasminogen activator inhibitor-1 (PAI-1) with an IC50 of 29 μM. TM5007 enhance fibrinolysis activity and inhibits coagulation. TM5007 also prevents the fibrotic process initiated by bleomycin in mouse lung .
NK3201 is an orally active chymase inhibitor (IC50: 2.5, 1.2, and 28 nM for human, dog and hamster chymase). NK3201 inhibits Bleomycin (HY-17565)-induced pulmonary fibrosis. NK3201 inhibits vascular proliferation in grafted vein .
TP0556351 is a potent and selective matrix metalloproteinase-2 (MMP2) inhibitor with an IC50 value of 0.2 nM. TP0556351 reduces the amount of collagen in the lungs of a Bleomycin-induced pulmonary fibrosis mouse model. TP0556351 can be used for researching idiopathic pulmonary fibrosis (IPF) .
ATX inhibitor 15 (compound 30), a indole-based carbamate derivative, is a potent autotaxin (ATX) inhibitor with an IC50 of 2.17 nM. ATX inhibitor 15 inhibits in vivo ATX and the gene expression of pro-fibrotic factors. ATX inhibitor 15 has lung protection effects in Bleomycin challenged mice lung fibrosis model .
PDE1-IN-8 (Compound 3f) is the inhibitor for PDE1 with an IC50 of 11 nM. PDE1-IN-8 inhibits cAMP and cGMP signaling pathway, inhibits the differentiation and proliferation of cells into myofibroblast, and exhibits anti-fibrotic efficacy in Bleomycin (HY-17565)-induced rat pulmonary fibrosis model .
IV-275 is an inhibitor of both BRG1 and BRM bromodomains. IV-275 increases the extent of DNA damage induced by Temozolomide (HY-17364) and Bleomycin (HY-108345). IV-275 inhibits the invasiveness of GBM cells. IV-275 enhances Temozolomide-induced cell death and the apoptosis-inducing activity of Temozolomide .
ATX-IN-3 is an orally active autotaxin (ATX) inhibitor with an IC50 of 46 nM. ATX-IN-3 certainly reduces collagen deposition and ameliorates lung fibrosis in the pulmonary fibrosis mouse model. ATX-IN-3 has good metabolic stability and drug-like properties. ATX-IN-3 can used for the study of idiopathic pulmonary fibrosis (IFP) .
ATX inhibitor 25 (Compound 29) is an orally active Autotaxin inhibitor with an IC50 of 1.08 nM. ATX inhibitor 25 exhibits excellent in vitro metabolic stability, with a t1/2 of more than 170 minutes. In the bleomycin (HY-108345)-induced pulmonary fibrosis mouse model, orally administered ATX inhibitor 25 shows anti-fibrotic effects .
ATX-1905 is a positron emission tomography (PET) tracer that demonstrates good autotaxin (ATX) binding specificity and achieves semiquantification of lung ATX expression levels, which are elevated in fibrotic lungs. ATX-1905 exhibits elevated uptake in Bleomycin (HY-108345)-induced pulmonary fibrosis (BPF) lungs. ATX-1905 is promising for research of idiopathic pulmonary fibrosis (IPF) .
ATX-IN-1 (compound 35) is an inhibitor of ATX (IC50=0.7 nM) with anti-inflammatory activity. ATX-IN-1 can inhibit TGF-β/Smad pathway and reduce collagen deposition to alleviate Bleomycin (HY-108345)-induced fibrosis in mice. ATX-IN-1 has good oral bioavailability (F=69.5%) and particle stability .
AAF-CMK TFA (Ala-ala-phe-chloromethylketone tfa; N-Ala-Ala-Phe-CMK) is a subtilisin-type serine peptidase that removes tripeptides from the free NH2 termini of oligopeptides. AAF-CMK TFA is an irreversible inhibitor of TPPII and is typically used at concentrations of 10-100 μM. It does not significantly interfere with the chymotrypsin-like activity of the proteasome. AAF-CMK also inhibits bleomycin hydrolase and puromycin-sensitive aminopeptidase when used at a concentration of 50 μM.
HDAC6-IN-44 (compound H10) is a selective HDAC6 inhibitor with an IC50 value of 8.97 nM. HDAC6-IN-44 can inhibit the idiopathic pulmonary fibrosis (IPF) phenotype and exhibits antifibrotic activity. Additionally, HDAC6-IN-44 reduces fibrogenesis in a bleomycin-induced pulmonary fibrosis mouse model and demonstrates good metabolic stability. HDAC6-IN-44 holds promise for research in the field of idiopathic pulmonary fibrosis .
PIM1-IN-8 is a PIM1/p65 pathway inhibitor. PIM1-IN-8 suppresses the expression of α-SMA and collagen I in activated fibroblasts and blocks TGF-β induced migration. PIM1-IN-8 alleviates pulmonary fibrosis in a Bleomycin (BLM) (HY-17565A)-induced pulmonary fibrosis mice model. PIM1-IN-8 can be used for the study of idiopathic pulmonary fibrosis (IPF) .
PDE1-IN-10 is a potent and sekective Phosphodiesterase 1 (PDE1) inhibitor with an IC50 of 5 nM. PDE1-IN-10 can suppress TGF-β/Smad-MAPK signaling and exhibit antifibrotic effects. PDE1-IN-10 can be used for the research of idiopathic pulmonary fibrosis .
HDAC6-IN-53 (Compound W28) is an inhibitor targeting histone deacetylase 6 (HDAC6) with an IC50 of 19.65 nM. HDAC6-IN-53 exerts the activity of inhibiting the phenotype of idiopathic pulmonary fibrosis (IPF) by suppressing the collagen expression induced by TGF-β1, and it has demonstrated a good therapeutic effect in a mouse model of pulmonary fibrosis induced by Bleomycin (HY-17565A). HDAC6-IN-53 can be used in the research of idiopathic pulmonary fibrosis and other related pulmonary fibrosis diseases.
Lactoquinomycin A is a quinone antibiotic. Lactoquinomycin A has the activity of anti-Gram-positive bacteria and some Gram-negative bacteria, but the effect of anti-Gram-negative bacteria is weak and has no effect on fungi. Lactoquinomycin A inhibits a variety of cell lines including lymphoma L5178Y progenitor, Adriamycin resistant, Bleomycin-resistant, human leukemia K562, mouse leukemia L-1210 and mouse leukemia P 388 with ID50 (μg/mL) of 0.02, 0.006, 0.008, 0.033, 0.013 and 0.03, respectively .
Lactoquinomycin B is a quinone antibiotic. Lactoquinomycin B has the activity of anti-Gram-positive bacteria and some Gram-negative bacteria, but the effect of anti-Gram-negative bacteria is weak and has no effect on fungi. Lactoquinomycin B inhibits a variety of cell lines including lymphoma L5178Y progenitor, Adriamycin resistant, Bleomycin-resistant, human leukemia K562, mouse leukemia L-1210 and mouse leukemia P 388 with ID50 (μg/mL) of 0.43, 0.21, 0.19, 0.16, 0.2 and 0.12, respectively .
TRPV1-IN-3 (compound 14) is a TRPV1 inhibitor that can be used for the research of idiopathic pulmonary fibrosis. TRPV1-IN-3 affects the expression of fibrosis markers collagen I and α-SMA by inhibiting the TGF-β/Smads and MAPK pathways, thereby exerting antifibrotic activity in vitro (IC50=0.51 μM). TRPV1-IN-3 significantly inhibits collagen deposition in lung tissue, improves the alveolar structure, and also increases the survival rate of mice with pulmonary fibrosis induced by Bleomycin (HY-108345) .
NCX 466 is an orally active COX-1 and COX-2 inhibitor that exhibits anti-inflammatory and analgesic effects. Additionally, NCX 466 acts as a NO donor, exerting anti-inflammatory and antioxidant effects by improving microcirculation. NCX 466 significantly reduces the levels of transforming growth factor-β (TGF-β) and oxidative stress markers (such as thiobarbituric acid reactive substances (TBARS) and 8-hydroxy-2'-deoxyguanosine (8-OHdG)), and it decreases leukocyte recruitment during inflammation by reducing myeloperoxidase (MPO) activity, thereby preventing bleomycin (HY-108345)-induced pulmonary fibrosis in mice .
JNK-1-IN-4 (Compound E1) is an inhibitor for JNK, that inhibits JNK-1, JNK-2 and JNK-3 with IC50s of 2.7, 19.0 and 9.0 nM, respectively. JNK-1-IN-4 inhibits the phosphorylation of c-Jun, and reduces the expression of TGF-β1-induced EMT marker proteins, such as fibronectin and α-SMA. JNK-1-IN-4 exhibits good pharmacokinetic characteristics with a bioavailability of 69%. JNK-1-IN-4 exhibits anti-fibrotic effect in Bleomycin (HY-17565)-induced mice idiopathic pulmonary fibrosis models .
FGFRs-IN-1 (Compound A16) is the orally active inhibitor for FGFR, that inhibits FGFR1/2/3/4 with IC50s of 2.3, 7, 11, and 163 nM, respectively. FGFRs-IN-1 also inhibits VEGFR1/2/3, Abl, and Flt3 with IC50s of 61, 176, 112, 26, and 353 nM, respectively. FGFRs-IN-1 exhibits weak inhibitory efficacy against CYP enzymes. FGFRs-IN-1 reduces the expression of α-SMA and collagen I, and inhibits epithelial-mesenchymal transition (EMT) in TGF-β1 stimulated A549 cell. FGFRs-IN-1 exhibits anti-inflammatory activity in Bleomycin (HY-17565)-induced mouse pulmonary fibrosis model and CCl4 (HY-Y0298)-induced mouse liver fibrosis model .
Curdione (Standard) is the analytical standard of Curdione. This product is intended for research and analytical applications. Curdione ((+)-Curdione) is an orally active sesquiterpenoid. Curdione inhibits platelet aggregation. Curdione induces ferroptosis in colorectal cancer via m6A methylation mediated by METTL14 and YTHDF2. Curdione inhibits ferroptosis in Isoproterenol (HY-B0468)-induced myocardial infarction by regulating the Keap1/Trx1/GPX4 signaling pathway, suppressing oxidative stress (ROS) and apoptosis. Curdione ameliorates Doxorubicin (HY-15142)-induced cardiotoxicity by inhibiting oxidative stress (ROS) and activating the Nrf2/HO-1 pathway. Curdione ameliorates sepsis-induced lung injury by inhibiting platelet-mediated neutrophil extracellular trap formation. Curdione ameliorates Bleomycin (HY-17565A)-induced pulmonary fibrosis by inhibiting TGF-β-induced fibroblast-to-myofibroblast differentiation. Curdione exhibits neuroprotective effects against focal cerebral ischemia-reperfusion injury in rats. Curdione exerts antiproliferative effects against human uterine leiomyosarcoma by targeting IDO1. Curdione protects vascular endothelial cells and atherosclerosis by regulating DNMT1-mediated ERBB4 promoter methylation. Curdione inhibits inducible prostaglandin E2 production (IC50 = 1.1 μM) and cyclooxygenase 2 expression .
Bleomycin B2 (Phleomycin D2) sulfate is a selective antitumor and antibacterial agent that induces DNA strand breaks and inhibits DNA ligase activity. The optimal pH for the activity of Bleomycin B2 sulfate is 9.1, and its efficacy is enhanced by thiol compounds or hydrogen peroxide. Bleomycin B2 sulfate undergoes enzymatic inactivation via bleomycin-inactivating enzymes, exhibits selective retention in squamous cell carcinoma, and is inactivated most rapidly in liver and kidney homogenates. Bleomycin B2 sulfate can be applied in research related to squamous cell carcinoma and other relevant studies .
Peplomycin (Bleomycin PEP) sulfate is an analog of Bleomycin (HY-108345) and an antitumor antibiotic. Peplomycin sulfate exhibits potent antitumor activity and relatively low pulmonary toxicity. Peplomycin sulfate can induce various skin abnormalities and trigger apoptosis in SSCKN cells of oral squamous cell carcinoma. Peplomycin sulfate can also induce pulmonary fibrosis. Peplomycin sulfate is applicable for the research of tumors, pulmonary fibrosis and other related diseases .
Phosphodiesterase-IN-5 is a potent, orally active and selective phosphodiesterase 10A (PDE10A) inhibitor with an IC50 of 6.2 nM. Phosphodiesterase-IN-5 shows >1612-fold selectivity over other PDEs. Phosphodiesterase-IN-5 exhibits potent antifibrotic efficacy in a Bleomycin (BLM) (HY-108345)-induced murine model of pulmonary fibrosis (PF) by blocking myofibroblast differentiation via the cAMP/PKA/CREB signaling pathway. Phosphodiesterase-IN-5 can be used for the research of PF .
SHR-1906 is a selective fully humanized monoclonal IgG1 inhibitory antibody targeting CTGF. SHR-1906 specifically binds to CTGF, thereby blocking the interaction between CTGF and TGF-B1 with an inhibition rate of 55%. SHR-1906increases the survival rate in a pulmonary fibrosis model by reducing TGF-β1 levels and inhibiting fibrotic lesions in lung tissue in Bleomycin (HY-108345)-induced pulmonary fibrosis.SHR-1906 can be used for pulmonary fibrosis (IPF) research. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001) .
Anti-Mouse DDR2 Antibody (DAB0065) is a mAb that specifically targets mouse discoidin domain receptor DDR2 without cross-reacting with DDR1. Anti-Mouse DDR2 Antibody (DAB0065) binds to the extracellular domain of native mouse DDR2, induces endocytosis and lysosomal degradation of DDR2, and this process is independent of collagen binding. Anti-Mouse DDR2 Antibody (DAB0065) exhibits significant therapeutic effects in both the unilateral ureteral obstruction (UUO) mouse model of renal fibrosis and the bleomycin (HY-108345)-induced mouse model of pulmonary fibrosis, effectively downregulating the mRNA expression of type I collagen Col1a1 and fibronectin Fn1. Anti-Mouse DDR2 Antibody (DAB0065) can be humanized and has the potential to be developed as a targeted agent for diseases such as idiopathic pulmonary fibrosis and renal fibrosis .
PI3K/mTOR-IN-20 is a selective dual PI3K/mTOR inhibitor. PI3K/mTOR-IN-20 demonstrates nanomolar antiproliferative effects with IC50s of 0.380 and 0.090 μM for MRC-5 and Mlg2908 cells. PI3K/mTOR-IN-20 reduces Ashcroft scores, hydroxyproline content, collagen deposition, and downregulates fibrosis-related proteins, while restoring lung architecture in a Bleomycin-induced pulmonary fibrosis model. PI3K/mTOR-IN-20 shows a favorable safety profile with steady weight recovery and no distinct liver or kidney toxicity. PI3K/mTOR-IN-20 can be used for fetal lung fibroblasts research .
Antiflammin-1 is an anti-inflammatory peptide 1 (MQMKKVLDS). Antiflammin-1 is a derivative of uteroglobin. Antiflammin-1 has anti-inflammatory and antifibrotic actions in bleomycin (HY-108345)-induced lung injury .
Fresolimumab (GC1008) is a human monoclonal antibody against TGF-β that neutralizes all mammalian active subtypes of TGF-β. The binding affinity of Fresolimumab to TGF-β2 is 1.8 nM. Fresolimumab improves Bleomycin (HY-108345)-induced acute lung injury. Fresolimumab radiolabeled with 89Zr can be used for PET analysis of TGF-β expression, antibody uptake and organ distribution. Fresolimumab can be used in the study of cancer, osteogenesis imperfecta, fibrosis and kidney disease .
AX-202 is a humanized IgG4 monoclonal antibody targeting S100A4. AX-202 neutralizes the activity of S100A4. AX-202 effectively reverses established fibrosis and reduces inflammation and fibrosis-related biomarkers in a mouse model of skin fibrosis. AX-202 is applicable for the research of fibrotic and inflammatory diseases .
Rosmantuzumab (OMP-131R10) is an anti-R-spondin 3 (RSPO3) humanized monoclonal antibody. Rosmantuzumab can be used for the research of advanced telapsed and refractory solid tumors .
SHR-1906 is a selective fully humanized monoclonal IgG1 inhibitory antibody targeting CTGF. SHR-1906 specifically binds to CTGF, thereby blocking the interaction between CTGF and TGF-B1 with an inhibition rate of 55%. SHR-1906increases the survival rate in a pulmonary fibrosis model by reducing TGF-β1 levels and inhibiting fibrotic lesions in lung tissue in Bleomycin (HY-108345)-induced pulmonary fibrosis.SHR-1906 can be used for pulmonary fibrosis (IPF) research. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001) .
Anti-Mouse DDR2 Antibody (DAB0065) is a mAb that specifically targets mouse discoidin domain receptor DDR2 without cross-reacting with DDR1. Anti-Mouse DDR2 Antibody (DAB0065) binds to the extracellular domain of native mouse DDR2, induces endocytosis and lysosomal degradation of DDR2, and this process is independent of collagen binding. Anti-Mouse DDR2 Antibody (DAB0065) exhibits significant therapeutic effects in both the unilateral ureteral obstruction (UUO) mouse model of renal fibrosis and the bleomycin (HY-108345)-induced mouse model of pulmonary fibrosis, effectively downregulating the mRNA expression of type I collagen Col1a1 and fibronectin Fn1. Anti-Mouse DDR2 Antibody (DAB0065) can be humanized and has the potential to be developed as a targeted agent for diseases such as idiopathic pulmonary fibrosis and renal fibrosis .
Crocin (Crocin I) is an orally active natural product that can be isolated from the stigma of Crocus sativus. Crocin inhibits tumor cell proliferation and promotes apoptosis through JAK pathway. Crocin has anti-inflammatory, antioxidant and antitumor activities .
Bleomycin A5 (Pingyangmycin) is a glycopeptide antibiotic with multiple biological activities, which can be isolated from Streptomyces. Bleomycin A5 exerts cytotoxic effects by binding to Fe 2+ to form a complex, inducing single-strand and double-strand DNA breaks, and inhibiting DNA replication. Bleomycin A5 inhibits Drp1-mediated mitochondrial fission and suppresses PINK1/Parkin pathway-mediated mitophagy, ultimately triggering mitochondria-mediated cellular apoptosis. Bleomycin A5 can be used in cancer research .
Dermatan sulphate sodium is an oral active glycosaminoglycan and thrombin inactivator with antithrombotic activity. It selectively catalyzes the heparin cofactor II-mediated inactivation of thrombin without interacting with antithrombin III. Dermatan sulphate sodium promotes stem cell differentiation, exhibits high bioavailability, and alleviates pulmonary fibrosis injury induced by Bleomycin (HY-108345). Dermatan sulphate sodium can be used in research related to cardiovascular diseases, inflammation, and stem cell differentiation .
Licoricesaponin G2 is an orally active component found in Licorice. Licoricesaponin G2 significantly ameliorates Bleomycin (HY-108345)-induced pulmonary fibrosis by inhibiting the TNF-α signaling pathway, reducing epithelial-mesenchymal transition, and decreasing extracellular matrix deposition. Licoricesaponin G2 inhibits cancer cells proliferation, migration, inhibits PI3K/AKT/mTOR signaling pathway and increases ROS production. Licoricesaponin G2 can be used for the research of lung cancer and pulmonary fibrosis .
L-Gulose is a rare L-aldohexose in nature, and serves as a key structural unit for the synthesis of a variety of important active compounds (e.g., vitamin C) .
Bleomycin A5 (Pingyangmycin) hydrochloride is a glycopeptide antibiotic with multiple biological activities, which can be isolated from Streptomyces. Bleomycin A5 hydrochloride exerts cytotoxic effects by binding to Fe 2+ to form a complex, inducing single-strand and double-strand DNA breaks, and inhibiting DNA replication. Bleomycin A5 hydrochloride inhibits Drp1-mediated mitochondrial fission and suppresses PINK1/Parkin pathway-mediated mitophagy, ultimately triggering mitochondria-mediated cellular apoptosis. Bleomycin A5 hydrochloride can be used in cancer research .
Neotuberostemonine, one of the main antitussive alkaloids in the root of Stemona tuberosa Lour, attenuates bleomycin-induced pulmonary fibrosis by suppressing the recruitment and activation of macrophages .
Crocin (Standard) is the analytical standard of Crocin. This product is intended for research and analytical applications. Crocin (Crocin I) is an orally active natural product that can be isolated from the stigma of Crocus sativus. Crocin inhibits tumor cell proliferation and promotes apoptosis through JAK pathway. Crocin has anti-inflammatory, antioxidant and antitumor activities .
Bleomycin B2 (Phleomycin D2) is an anti-cancer agent that targets DNA. Bleomycin B2 causes DNA strand breaks, thereby inhibiting the growth and proliferation of cancer cells. Bleomycin B2 is promising for research of cancers .
Lactoquinomycin A is a quinone antibiotic. Lactoquinomycin A has the activity of anti-Gram-positive bacteria and some Gram-negative bacteria, but the effect of anti-Gram-negative bacteria is weak and has no effect on fungi. Lactoquinomycin A inhibits a variety of cell lines including lymphoma L5178Y progenitor, Adriamycin resistant, Bleomycin-resistant, human leukemia K562, mouse leukemia L-1210 and mouse leukemia P 388 with ID50 (μg/mL) of 0.02, 0.006, 0.008, 0.033, 0.013 and 0.03, respectively .
Lactoquinomycin B is a quinone antibiotic. Lactoquinomycin B has the activity of anti-Gram-positive bacteria and some Gram-negative bacteria, but the effect of anti-Gram-negative bacteria is weak and has no effect on fungi. Lactoquinomycin B inhibits a variety of cell lines including lymphoma L5178Y progenitor, Adriamycin resistant, Bleomycin-resistant, human leukemia K562, mouse leukemia L-1210 and mouse leukemia P 388 with ID50 (μg/mL) of 0.43, 0.21, 0.19, 0.16, 0.2 and 0.12, respectively .
Curdione (Standard) is the analytical standard of Curdione. This product is intended for research and analytical applications. Curdione ((+)-Curdione) is an orally active sesquiterpenoid. Curdione inhibits platelet aggregation. Curdione induces ferroptosis in colorectal cancer via m6A methylation mediated by METTL14 and YTHDF2. Curdione inhibits ferroptosis in Isoproterenol (HY-B0468)-induced myocardial infarction by regulating the Keap1/Trx1/GPX4 signaling pathway, suppressing oxidative stress (ROS) and apoptosis. Curdione ameliorates Doxorubicin (HY-15142)-induced cardiotoxicity by inhibiting oxidative stress (ROS) and activating the Nrf2/HO-1 pathway. Curdione ameliorates sepsis-induced lung injury by inhibiting platelet-mediated neutrophil extracellular trap formation. Curdione ameliorates Bleomycin (HY-17565A)-induced pulmonary fibrosis by inhibiting TGF-β-induced fibroblast-to-myofibroblast differentiation. Curdione exhibits neuroprotective effects against focal cerebral ischemia-reperfusion injury in rats. Curdione exerts antiproliferative effects against human uterine leiomyosarcoma by targeting IDO1. Curdione protects vascular endothelial cells and atherosclerosis by regulating DNMT1-mediated ERBB4 promoter methylation. Curdione inhibits inducible prostaglandin E2 production (IC50 = 1.1 μM) and cyclooxygenase 2 expression .
Bleomycin Hydrolase Protein (BLMH) is crucial for cellular defense, inactivating the antitumor drug Bleomycin (BLM) by hydrolyzing its carboxamide bond. This neutralizes BLM's cytotoxic effects, protecting normal and malignant cells. BLMH's exact physiological function is unknown, but its significance in maintaining cellular balance and defending against harmful agents is evident. BLMH/Bleomycin Hydrolase Protein, Mouse (His) is the recombinant mouse-derived BLMH/Bleomycin Hydrolase Protein, expressed by E. coli , with N-His labeled tag.
Bleomycin Hydrolase Protein (BLMH) is crucial for cellular defense, inactivating the antitumor drug Bleomycin (BLM) by hydrolyzing its carboxamide bond. This neutralizes BLM's cytotoxic effects, protecting normal and malignant cells. BLMH's exact physiological function is unknown, but its significance in maintaining cellular balance and defending against harmful agents is evident. BLMH/Bleomycin Hydrolase Protein, Mouse (P. pastoris, His) is the recombinant mouse-derived BLMH/Bleomycin Hydrolase Protein, expressed by P. pastoris , with N-6*His labeled tag.
Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC50 values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice .
Entrectinib-d4 (NMS-E628-d4; RXDX-101-d4) is the deuterium labeled Entrectinib (HY-12678). Entrectinib is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
ATX-1905 is a positron emission tomography (PET) tracer that demonstrates good autotaxin (ATX) binding specificity and achieves semiquantification of lung ATX expression levels, which are elevated in fibrotic lungs. ATX-1905 exhibits elevated uptake in Bleomycin (HY-108345)-induced pulmonary fibrosis (BPF) lungs. ATX-1905 is promising for research of idiopathic pulmonary fibrosis (IPF) .
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Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
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