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MMP-7-IN-3 is a potent and selective inhibitor of MMP-7. MMP-7-IN-3 suppresses kidney fibrosis progression in a mouse model with unilateral ureteral obstruction .
Endo CNTinh-03 is inhibitor for the elevation of cAMP and cGMP induced by agonist, such as G protein-coupled receptors, adenylate cyclase, and guanylate cyclase (IC50 is 4 μM). Endo CNTinh-03 inhibits cholera toxin- and Escherichia coli (STa) toxin- induced CFTR chloride current, ameliorates secretory diarrhea in mouse models, and prevents cyst growth in polycystic kidney disease model .
Telaglenastat (CB-839) is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mousekidney and brain, respectively. Telaglenastat inuduces autophagy and has antitumor activity .
N-methyl-N-dithiocarboxyglucamine (MDCG) sodium mobilizes and promotes excretion of metallothionein-bound 109Cd in mouse model. N-methyl-N-dithiocarboxyglucamine significantly lowers the Cd content of both the liver and kidney, which is organs most susceptible to Cd-induced toxicity .
Saccharic acid is a competitive inhibitor of β-glucuronidase. Saccharic acid considerably retards hydrolysis of the glucuronide of 'l-ortho-hydroxyphenylazo-2-naph-thol' by frozen mousekidney sections, but has no effect on liver regeneration following damage and on growth in infant mice .
(R)-Levrazoxane ((R)-ICRF 186) is enzymatically hydrolysed to one-ring open intermediates by dihydropyrimidine amidohydrolase (DPHase), which is present in the liver and kidney. The radiosensitizing efficiency of (R)-Levrazoxane towards EMT6 mouse mammary tumour cells is greater than that of Dexrazoxane (HY-B0581). (R)-Levrazoxane is promising for research of liver and kidney related diseases .
Ferroptosis-IN-12 (Cpd-A1) is a ferroptosis inhibitor. Ferroptosis-IN-12 exhibits effective ferroptosis inhibition in Erastin (HY-15763)-treated mouse tubular epithelial cells (mTECs) and improves kidney function, alleviates renal tubular damage, and reduces inflammation in a dose-dependent manner in acute kidney injury (AKI) mouse models induced by ischemia/reperfusion (I/R) or cecal ligation and puncture (CLP). Ferroptosis-IN-12 demonstrates good plasma stability and high distribution in kidney tissues in pharmacokinetic studies in mice. Ferroptosis-IN-12 holds promise for research in the field of acute kidney injury (AKI) .
Telaglenastat (CB-839) hydrochloride is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat hydrochloride selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mousekidney and brain, respectively. Telaglenastat hydrochloride inudces autophagy and has antitumor activity .
C-Type Natriuretic Peptide (1-53), Porcine, Rat, mouse is an activator of particulate guanylate cyclase B (pGC-B), which is highly expressed in endothelial cells, kidneys, and the heart. C-Type Natriuretic Peptide (1-53), Porcine, Rat, mouse can mediate a potent anti-fibrotic effect in human cardiac and renal fibroblasts by generating the second messenger cGMP .
3-OH-Kynurenamine dihydroiodide is the dihydroiodide form of 3-OH-Kynurenamine (HY-156908). 3-OH-Kynurenamine dihydroiodide is an activator for aryl hydrocarbon receptor (AhR), and thus regulates the immune response. 3-OH-Kynurenamine dihydroiodide upregulates the expressions of Ido1 and Tgfb1, ameliorates the skin inflammation in psoriasis mouse model and kidney damage in nephrotoxic lupus mouse model .
Klotho-derived peptide 1 (KP1 human) blocks TGF-β/TGF-β receptor 2 interaction, inhibits TGF-β-induced activation of Smad2/3 and mitogen-activated protein kinase (MAPK), and exhibits anti-fibrotic and kidney protective effects in mouse model .
Klotho-derived peptide 1 (KP1 human) hydrochloride blocks TGF-β/TGF-β receptor 2 interaction, inhibits TGF-β-induced activation of Smad2/3 and mitogen-activated protein kinase (MAPK), and exhibits anti-fibrotic and kidney protective effects in mouse model .
SIRT5 inhibitor 7 (compound 58) is a substrate-competitive and selective SIRT5 inhibitor with anti-inflammatory activity. SIRT5 inhibitor 7 has renal protective effects and regulates protein succinylation and the release of pro-inflammatory cytokines. SIRT5 inhibitor 7 has in vivo activity in AKI mouse models of lipopolysaccharide (LPS) and cecal ligation/perforation (CLP)-induced sepsis-related acute kidney injury .
HMGB1-IN-2 (compound 15) is an inhibitor of highly conserved nuclear protein (HMGB1), showing NO inhibitory effect with IC50 value of 20.2 μM in RAW264.7 cells. HMGB1-IN-2 (30 μM) decreases the level of IL-1 β, TNF-α, caspase-1 p20, inhibits the phosphorylation of NF-κB p65, exhibits anti-apoptotic activity. HMGB1-IN-2 (15 mg/kg; ip) relives kidney injury in septic acute kidney injury mouse. HMGB1-IN-2 inhibits Huh7 cells and A549 cells with IC50s of 77.0 μM, and 82.0 μM, respectively .
TNF-α-IN-18 (Compound 61) is an inhibitor for TNF-α (IC50 of 1.8 μM), that inhibits TNF signaling pathway through block of NF-kB migration from cytoplasm to nucleus. TNF-α-IN-18 exhibits slight cytotoxicity to mouse fibroblast LM cell, with a CC50 >50 μM. TNF-α-IN-18 ameliorates the TNF- or Lipopolysaccharide (HY-D1056)-induced sepsis in mouse models. TNF-α-IN-18 protects mice from rheumatoid arthritis .
Reveromycin C is a polyketide originally isolated from Streptomyces that has antifungal activity against C. albicans (MICs=2.0 and >500 μg/mL at pH 3 and 7.4, respectively). Reveromycin C inhibits EGF-induced mitogenic activity in the Balb/MK mouse epidermal cell line. It also reverses the morphology of sarcoma-virus-transformed NRK rat kidney cells (EC50=1.58 μg/mL) and inhibits proliferation of KB cells and K562 human chronic myelogenous leukemia cells (IC50=2.0 μg/mL for both).
GFB-8438 is a potent and subtype selective TRPC5 inhibitor, with IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. GFB-8438 shows excellent selectivity against TRPC6, other TRP family members, NaV 1.5, as well as limited activity against the hERG channel. GFB-8438 protects mouse podocytes from injury induced by protamine sulfate model .
DCFBC is a prostate-specific membrane antigen (PSMA) inhibitor for small animal positron emission tomography (PET) imaging. [18F]DCFBC was prepared by reacting fluorine-18 labeled phenyl bromide with the precursor (S)-2-[3-[(R)-1-carboxy-2-thiolethyl]urea]-glutaric acid in ammonia-saturated methanol at 60°C for 10 min and then purified by C-18 reversed-phase HPLC. [18F]DCFBC was injected via the tail vein in severe combined immunodeficient mice for in vitro biodistribution or imaging. For in vitro biodistribution studies, mice were sacrificed at 5, 15, 30, 60, and 120 min after injection, and tumors, blood, and major organs were collected, weighed, and radioactivity was counted. Imaging was performed using a GE eXploreVista small animal PET scanner, collecting 12 consecutive 10-min frames. Results showed that the radiochemical yield of [18F]DCFBC averaged 16±6% (n=8) from 4-[18F]fluorophenyl bromide. Specific radioactivity ranged from 13 to 133 GBq/Amol (350-3600 Curie/mmol) with an average of 52 GBq/Amol (1392 Curie/mmol; n=6). Biodistribution and imaging studies showed high uptake of [18F]DCFBC in PIP tumors and almost no uptake in FLU tumors. High radiopharmaceutical uptake was also seen in the kidney and bladder; however, radioactivity washout from these organs was faster than from the PIP tumors. Maximum PIP tumor uptake was reached at 60 min post-injection at 8.16±2.55% injected dose/g and decreased to 4.69±0.89 at 120 min post-injection. The PIP tumor-to-muscle ratio was 20 at 120 min post-injection. Based on mouse biodistribution, the dose-limiting organ was the kidney (estimated human absorbed dose: 0.05 mGy/MBq; 0.2 rad/mCi). Conclusions: [18F]DCFBC localizes specifically to PSMA+ expressing tumors in mice and is suitable for small animal PET imaging. This novel radiopharmaceutical is an attractive candidate for further study in PET imaging of prostate cancer.
MMP-7-IN-3 is a potent and selective inhibitor of MMP-7. MMP-7-IN-3 suppresses kidney fibrosis progression in a mouse model with unilateral ureteral obstruction .
C-Type Natriuretic Peptide (1-53), Porcine, Rat, mouse is an activator of particulate guanylate cyclase B (pGC-B), which is highly expressed in endothelial cells, kidneys, and the heart. C-Type Natriuretic Peptide (1-53), Porcine, Rat, mouse can mediate a potent anti-fibrotic effect in human cardiac and renal fibroblasts by generating the second messenger cGMP .
Klotho-derived peptide 1 (KP1 human) blocks TGF-β/TGF-β receptor 2 interaction, inhibits TGF-β-induced activation of Smad2/3 and mitogen-activated protein kinase (MAPK), and exhibits anti-fibrotic and kidney protective effects in mouse model .
Klotho-derived peptide 1 (KP1 human) hydrochloride blocks TGF-β/TGF-β receptor 2 interaction, inhibits TGF-β-induced activation of Smad2/3 and mitogen-activated protein kinase (MAPK), and exhibits anti-fibrotic and kidney protective effects in mouse model .
N-methyl-N-dithiocarboxyglucamine (MDCG) sodium mobilizes and promotes excretion of metallothionein-bound 109Cd in mouse model. N-methyl-N-dithiocarboxyglucamine significantly lowers the Cd content of both the liver and kidney, which is organs most susceptible to Cd-induced toxicity .
Saccharic acid is a competitive inhibitor of β-glucuronidase. Saccharic acid considerably retards hydrolysis of the glucuronide of 'l-ortho-hydroxyphenylazo-2-naph-thol' by frozen mousekidney sections, but has no effect on liver regeneration following damage and on growth in infant mice .
Renin Protein, a highly specific endopeptidase, generates angiotensin I from angiotensinogen, initiating a cascade that elevates blood pressure and enhances kidney sodium retention.Renin Protein, Mouse (HEK293, His) is the recombinant mouse-derived Renin protein, expressed by HEK293 , with C-10*His labeled tag.
Collectin-11/CL-K1 Protein is a secreted protein that activates tyrosine kinase receptors (EGFR, HER3) and ERK, JNK, and AKT signaling pathways to promote cell proliferation. Collectin-11/CL-K1 Protein plays an important role in innate immunity and apoptosis. Collectin-11/CL-K1 Protein, Mouse (HEK293, His) is the recombinant mouse-derived Collectin-11/CL-K1 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of Collectin-11/CL-K1 Protein, Mouse (HEK293, His) is 246 a.a., with molecular weight of 30-35 kDa.
Arginase-2 (ARG2) is a multifunctional regulator central to the regulation of arginine metabolism and nitric oxide synthesis outside the urea cycle. In addition to its hepatic effects, ARG2 affects innate and adaptive immune responses, negatively affecting the survival of activated CD4(+) and CD8(+) T cells. Arginase-2/ARG2 Protein, Mouse (His-SUMO) is the recombinant mouse-derived Arginase-2/ARG2 protein, expressed by E. coli , with N-6*His, N-SUMO labeled tag. The total length of Arginase-2/ARG2 Protein, Mouse (His-SUMO) is 332 a.a., with molecular weight of ~52.4 kDa.
The TIM-1/KIM-1/HAVCR protein is a phosphatidylserine receptor that is critical for B cell homeostasis, affecting generation, expansion, and inhibitory functions. As a P-selectin/SELPLG ligand, it facilitates trafficking of activated T cells during inflammation and controls T cell accumulation in the inflamed central nervous system. TIM-1/KIM-1/HAVCR Protein, Mouse (HEK293, C-His) is the recombinant mouse-derived TIM-1/KIM-1/HAVCR protein, expressed by HEK293 , with C-6*His labeled tag.
CXCL14/BRAK protein selectively attracts CESS B cells and THP-1 monocytes without affecting T cells. Its specific chemical attraction emphasizes its role in mediating B cell and monocyte migration, contributing to immune responses within the microenvironment. CXCL14/BRAK Protein, Mouse (His) is the recombinant mouse-derived CXCL14/BRAK protein, expressed by E. coli , with N-6*His labeled tag. The total length of CXCL14/BRAK Protein, Mouse (His) is 77 a.a., with molecular weight of ~13 kDa.
Cadherin-6/KCAD protein acts as a calcium-dependent cell adhesion protein and mediates cell-cell interactions. They preferentially interact in the same way with other cadherin molecules of the same type, promoting adhesion between cells. Cadherin-6/KCAD Protein, Mouse (HEK293, His) is the recombinant mouse-derived Cadherin-6/KCAD protein, expressed by HEK293 , with C-His labeled tag. The total length of Cadherin-6/KCAD Protein, Mouse (HEK293, His) is 597 a.a., with molecular weight of ~98 kDa.
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