157 Results for "

human DOR

" in MedChemExpress (MCE) Product Catalog:
Products (157)

157 Results for "human DOR" in MCE Product Catalog:

5
5 Cited Publications
Cat. No.: HY-14521
CAS No.: 106400-81-1
Purity:  98.96%
Synonyms: DDATHF
Research Areas:  

Cancer

Lometrexol (DDATHF), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol has anticancer activity. Lometrexol also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor .
loading...
    loading...
5
5 Cited Publications
Cat. No.: HY-14521B
CAS No.: 1435784-14-7
Synonyms: DDATHF hydrate
Research Areas:  

Cancer

Lometrexol (DDATHF) hydrate, an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol hydrate can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol hydrate has anticancer activity. Lometrexol hydrate also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor .
loading...
    loading...
5
5 Cited Publications
Cat. No.: HY-14521A
CAS No.: 120408-07-3
Purity:  ≥98.0%
Synonyms: DDATHF disodium
Research Areas:  

Cancer

Lometrexol (DDATHF) disodium, an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol disodium can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol disodium has anticancer activity. Lometrexol disodium also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor .
loading...
    loading...
3
3 Cited Publications
Cat. No.: HY-106005
CAS No.: 1314883-11-8
Purity:  99.17%
Target:  

Parasite PI4K

Research Areas:  

Infection

MMV390048 is a representative of a new chemical class of Plasmodium PI4K inhibitor (Kd app=0.3 µM). MMV390048 binds to the ATP binding site of Plasmodium PI4K and does not bind to other P. falciparum and human kinases apart from human PIP4K2C, thus alleviating potential kinase-mediated safety concerns. MMV390048 is an antimalarial agent .
loading...
    loading...
3
3 Cited Publications
Cat. No.: HY-123981
CAS No.: 47208-82-2
Purity:  99.72%
Target:  

Phosphatase

Research Areas:  

Cancer

5MPN is a first-in-class, potent, orally active and selective 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 4 (PFKFB4) inhibitor. 5MPN appears to be a competitive inhibitor of the F6P binding site (Ki=8.6 μM). 5MPN does not inhibit PFK-1 or PFKFB3. 5MPN targets the sugar metabolism of tumors and suppresses proliferation of multiple human cancer cell lines .
loading...
    loading...
3
3 Cited Publications
Cat. No.: HY-125913
CAS No.: 618-39-3
Target:  

Ser/Thr Protease

Research Areas:  

Inflammation/Immunology

Benzamidine is a competitive protease inhibitor that blocks the hydrolytic cleavage of glucagon by plasmin, trypsin and thrombin. Benzamidine effectively inhibits the degradation of glucagon by relevant proteases during the collection, storage and analysis of human plasma and blood samples. During in vivo metabolism, Benzamidine undergoes N-hydroxylation and produces multiple metabolites, exhibiting characteristics of delayed excretion or biphasic elimination. Benzamidine only induces slight single-strand DNA breaks at high concentrations and shows no significant genotoxic potential overall. Benzamidine may interfere with the detection of some glucagon antisera, but does not affect key antigen-antibody affinity at specific concentrations. Benzamidine can be used as a stabilizer in glucagon radioimmunoassays to ensure the accuracy and recovery rate of detection results .
loading...
    loading...
3
3 Cited Publications
Cat. No.: HY-W018781
CAS No.: 1670-14-0
Target:  

Ser/Thr Protease

Research Areas:  

Cancer

Benzamidine hydrochloride is a competitive protease inhibitor that blocks the hydrolytic cleavage of glucagon by plasmin, trypsin and thrombin. Benzamidine hydrochloride effectively inhibits the degradation of glucagon by relevant proteases during the collection, storage and analysis of human plasma and blood samples. During in vivo metabolism, Benzamidine hydrochloride undergoes N-hydroxylation and produces multiple metabolites, exhibiting characteristics of delayed excretion or biphasic elimination. Benzamidine hydrochloride only induces slight single-strand DNA breaks at high concentrations and shows no significant genotoxic potential overall. Benzamidine hydrochloride may interfere with the detection of some glucagon antisera, but does not affect key antigen-antibody affinity at specific concentrations. Benzamidine hydrochloride can be used as a stabilizer in glucagon radioimmunoassays to ensure the accuracy and recovery rate of detection results .
loading...
    loading...
3
3 Cited Publications
Cat. No.: HY-W087937
CAS No.: 206752-36-5
Synonyms: Benzenecarboximidamide hydrochloride hydrate
Benzamidine (Benzenecarboximidamide) hydrochloride hydrate is a competitive protease inhibitor that blocks the hydrolytic cleavage of glucagon by plasmin, trypsin and thrombin. Benzamidine hydrochloride hydrate effectively inhibits the degradation of glucagon by relevant proteases during the collection, storage and analysis of human plasma and blood samples. During in vivo metabolism, Benzamidine hydrochloride hydrate undergoes N-hydroxylation and produces multiple metabolites, exhibiting characteristics of delayed excretion or biphasic elimination. Benzamidine hydrochloride hydrate only induces slight single-strand DNA breaks at high concentrations and shows no significant genotoxic potential overall. Benzamidine hydrochloride hydrate may interfere with the detection of some glucagon antisera, but does not affect key antigen-antibody affinity at specific concentrations. Benzamidine hydrochloride hydrate can be used as a stabilizer in glucagon radioimmunoassays to ensure the accuracy and recovery rate of detection results .
loading...
    loading...
3
3 Cited Publications
Cat. No.: HY-18719A
CAS No.: 1032008-74-4
Endoxifen Z-isomer hydrochloride is an orally active selective PKCβ1 inhibitor with an IC50 of 360 nM against human PKCβ1. It also acts as an estrogen receptor modulator and antiestrogen. Endoxifen Z-isomer hydrochloride binds to and blocks ERα, ERβ and PKCβ1, inhibits estrogen and PI3K/AKT/mTORC1 signaling pathways, suppresses the expression of genes associated with cell cycle, cell proliferation and extracellular matrix remodeling, and induces apoptosis, reactive oxygen species (ROS) production and hypoxic features. Endoxifen Z-isomer hydrochloride inhibits tumor growth in breast tumor and glioblastoma models, reduces bone turnover and blood lipid levels, and does not require metabolism via CYP2D6. It can be used in research related to ER + breast cancer, invasive breast cancer, glioblastoma multiforme, type I bipolar disorder, desmoid tumor, gynecological malignancies, melanoma and hormone receptor-positive solid tumors .
loading...
    loading...
3
3 Cited Publications
Cat. No.: HY-18719
CAS No.: 112093-28-4
Endoxifen Z-isomer is an orally active selective PKCβ1 inhibitor with an IC50 of 360 nM against human PKCβ1. Endoxifen Z-isomer also acts as an estrogen receptor modulator and antiestrogen. Endoxifen Z-isomer binds to and blocks ERα, ERβ and PKCβ1, inhibits estrogen and PI3K/AKT/mTORC1 signaling pathways, suppresses the expression of genes associated with cell cycle, cell proliferation and extracellular matrix remodeling, and induces apoptosis, reactive oxygen species (ROS) production and hypoxic features. Endoxifen Z-isomer inhibits tumor growth in breast tumor and glioblastoma models, reduces bone turnover and blood lipid levels, and does not require metabolism via CYP2D6. Endoxifen Z-isomer can be used in research related to ER + breast cancer, invasive breast cancer, glioblastoma multiforme, type I bipolar disorder, desmoid tumor, gynecological malignancies, melanoma and hormone receptor-positive solid tumors .
loading...
    loading...
2
2 Cited Publications
Cat. No.: HY-N2574
CAS No.: 511-96-6
Gitogenin is a natural steroid isolated from the whole plant of Tribulus longipetalus. Gitogenin is a selective inhibitor of UDP-glucuronosyltransferase 1A4 (UGT1A4) and enzyme α-glucosidase with IC50 values of 0.69 μM (use trifluoperazine as a substrate) and 37.2 μM, respectively, and does not inhibit the activities of major human cytochrome P450 isoforms .
loading...
    loading...
2
2 Cited Publications
Cat. No.: HY-15451
CAS No.: 1048973-47-2
Purity:  99.26%
Synonyms: BZO-HEXOXIZID
Target:  

Cannabinoid Receptor

Research Areas:  

Neurological Disease

MDA 19 is a potent and selective agonist of human cannabinoid receptor 2 (CB2), with a Ki of 43.3 nM. MDA 19 has antiallodynic effects in a rat model of neuropathic pain and does not affect rat locomotor activity .
loading...
    loading...
1
1 Cited Publications
Cat. No.: HY-P3463
CAS No.: 123475-27-4
Synonyms: GLP-1 (human)
Target:  

GCGR

Beinaglutide is a human GLP-1 polypeptide that shares almost 100% homology with human GLP-1 (7–36). Beinaglutide displays does-dependent effects in glycemic control, inhibiting food intake and gastric empty and promoting weight loss. Beinaglutide has the potential for the research of overweight/obesity and nonalcoholic steatohepatitis (NASH) .
loading...
    loading...
1
1 Cited Publications
Cat. No.: HY-W179181
CAS No.: 852702-51-3
Target:  

GLUT

Research Areas:  

Metabolic Disease Cancer

MSNBA is a potent and selective GLUT5 fructose transport inhibitor with an IC50 of 0.10 mM. MSNBA does not affect the transport activity of human GLUT1, GLUT2, GLUT3, GLUT4 or bacterial GlcPSe. MSNBA competitively inhibits GLUT5 fructose uptake with a Ki of 3.2 μM in MCF7 cells. MSNBA can be used for the study of cancer or diabetes .
loading...
    loading...
1
1 Cited Publications
Cat. No.: HY-120951
CAS No.: 1310744-67-2
Purity:  99.01%
Target:  

Endonuclease

Research Areas:  

Cancer

PFM39, a Mirin analog, is a potent and selective MRE11 exonuclease inhibitor. PFM39 inhibits phosphate rotation for dsDNA exonuclease activity. PFM39 does not inhibit TmMre11 or human MRE11/MRN endonuclease activity .
loading...
    loading...
1
1 Cited Publications
Cat. No.: HY-111759
CAS No.: 22242-96-2
Purity:  98.60%
Synonyms: 7-CN-7-C-Ino
Jaspamycin (7-CN-7-C-Ino) is a potent activator of PKA, binding to the R site (PKAR), with an EC50 of 6.5 nM and Kd of 8 nM in Trypanosoma brucei. Jaspamycin (7-CN-7-C-Ino) does not bind with purified human PKARIα. Anti-parasite activity .
loading...
    loading...
1
1 Cited Publications
Cat. No.: HY-126972A
Purity:  98.02%
Target:  

RAD51

Research Areas:  

Cancer

RI(dl)-2 TFA is a potent and selective RAD51-mediated D-loop formation inhibitor with an IC50 of 11.1 μM. RI(dl)-2 TFA does not influence RAD51 binding to ssDNA and inhibits homologous recombination (HR) activity in human cells (IC50 of 3.0 μM) .
loading...
    loading...
1
1 Cited Publications
Cat. No.: HY-P2294A
Target:  

TGF-β Receptor

Research Areas:  

Inflammation/Immunology

pm26TGF-β1 TFA peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide TFA shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide TFA displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction .
loading...
    loading...
1
1 Cited Publications
Cat. No.: HY-149208
CAS No.: 2921948-27-6
Target:  

HDAC Apoptosis

Research Areas:  

Cancer

HDAC-IN-53 is an orally active, and selective HDAC1-3 inhibitor with IC50 values of 47 nM, 125 nM, and 450 nM, respectively. HDAC-IN-53 does not inhibit class II HDACs (HDAC4, 5, 6, 7, 9; IC50>10 μM). HDAC-IN-53 induces caspase-dependent apoptosis. HDAC-IN-53 significantly inhibits the growth of human tumor xenografts in nude mice and murine tumor growth in immune-competent mice bearing MC38 colon cancer .
loading...
    loading...
Cat. No.: HY-P4385
CAS No.: 129622-68-0
Target:  

PTHR

Research Areas:  

Metabolic Disease

(Asn10,Leu11,D-Trp12)-pTH-Related Protein (7-34) amide (human, mouse, rat) is a potent PTH-1R antagonist and does not display any partial agonist activity .
loading...
    loading...