| DC74831 |
Normetanephrine HCl |
Normetanephrine is a metabolite of norepinephrine created by action of catechol-O-methyl transferase on norepinephrine. It is excreted in the urine and found in certain tissues. It is a marker for catecholamine-secreting tumors such as pheochromocytoma. |
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| DC74832 |
MAO-B-IN-22 |
MAO-B-IN-22 (compound 6h) is a potent MAO-B inhibitor |
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| DC74833 |
PSB06126 sodium |
PSB-06126 is a NTPDase 3 inhibitor. PSB-06126 inhibits rat NTPDase 3 at low micromolar concentrations and display selectivity over NTPDase 1 and NTPDase 2. |
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| DC74834 |
Omadacycline |
Omadacycline, also known as PTK 0796 and Amadacyclin, is a novel first-in-class aminomethylcycline with potent activity against important skin and pneumonia pathogens, including community-acquired methicillin-resistant Staphylococcus aureus (MRSA), β-hemolytic streptococci, penicillin-resistant Streptococcus pneumoniae, Haemophilus influenzae, and Legionella. Omadacycline is active against strains expressing the two main forms of tetracycline resistance (efflux and ribosomal protection). The primary effect of omadacycline is on bacterial protein synthesis, inhibiting protein synthesis with a potency greater than that of tetracycline. The binding site for omadacycline is similar to that for tetracycline. |
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| DC74835 |
LSD1-IN-23 |
LSD1-IN-23 is a competitive/non-competitive mixed inhibitor of lysine specific demethylase 1 (LSD1) |
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| DC74836 |
ROS-IN-1 |
ROS-IN-1 is a mitochondrial ROS inhibitor. |
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| DC74837 |
Entecavir hydrate |
Entecavir is an oral antiviral drug used in the treatment of hepatitis B virus (HBV) infection. Entecavir is a reverse transcriptase inhibitor. It prevents the hepatitis B virus from multiplying and reduces the amount of virus in the body. More specifically, it is a deoxyguanosine analogue belonging to a class of carbocyclic nucleosides, that inhibits reverse transcription, DNA replication and transcription in the viral replication process. |
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| DC74838 |
LY-344864 free base |
LY-344864 is a potent 5-HT1 receptor agonist. |
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| DC74839 |
Eptapirone free base |
Eptapirone, also known as F11440 and L0068, is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential. The affinity of F 11440 for 5-HT1A binding sites (pKi, 8.33) was higher than that of buspirone (pKi, 7.50), and somewhat lower than that of flesinoxan (pKi, 8.91). In vivo, F 11440 was 4- to 20-fold more potent than flesinoxan, and 30- to 60-fold more potent than buspirone. |
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| DC74840 |
ICG001 |
ICG-001 is a potent and selective Wnt signaling modulator. ICG-001 modulates Wnt signaling and increased the expression of genes beneficial for cardiac regeneration in epicardial cells. ICG-001 binds cAMP-responsive element binding (CREB)-binding protein (CBP) to disrupt its interaction with β-catenin and inhibit CBP function as a coactivator of Wnt/β-catenin-mediated transcription. ICG-001 induces cytotoxicity of multiple myeloma cells in Wnt-independent manner. Note: Chemical structures of ICG-001 and PRI-724 look very close, but they are not the same molecule. Many vendors confused them. |
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| DC74841 |
SKF-96365 HCl |
SKF-96365 is a selective TRPC channel blocker. SKF-96365 activates cytoprotective autophagy to delay apoptosis in colorectal cancer cells through inhibition of the calcium/CaMKIIγ/AKT-mediated pathway. SKF-96365 strongly inhibits voltage-gated sodium current in rat ventricular myocytes. SKF 96365 inhibits glioblastoma cell growth by enhancing reverse mode of the Na(+) /Ca(2+) exchanger and increasing intracellular Ca(2+). SKF-96365 attenuates toxin-induced neuronal injury through opposite regulatory effects on Homer1a and Homer1b/c in cultured rat mesencephalic cells. |
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| DC74842 |
Mozavaptan HCl |
Mozavaptan, also known as OPC 31260, is a vasopressin receptor antagonist marketed by Otsuka. In Japan, it was approved in October 2006 for hyponatremia (low blood sodium levels) caused by syndrome of inappropriate antidiuretic hormone (SIADH) due to ADH producing tumors. |
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| DC74843 |
Rapastinel |
Rapastinel, also known as GLYX 13 and BV 102, is a monoclonal antibody-derived tetrapeptide that acts as a partial agonist at the glycine site of the N-methyl-D-aspartate (NMDA) receptor. |
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| DC74844 |
JPH203 free base |
JPH203, also known as KYT-0353, is a potent and selective LAT1 selective ( L-type amino acid transporter 1) inhibitor. JPH203 can very potently inhibit l-leucine uptake. JPH203 inhibits YD-38 cell growth. JPH203 up-regulated the population of apoptotic YD-38 cells through the activation of apoptotic factors, including caspases and PARP. |
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| DC74845 |
Zunsemetinib M-atropisomer |
Zunsemetinib M-atropisomer is the inactive isomer of Zunsemetinib. Zunsemetinib, also known as ATI-450 and CDD450, is the P-atropisomer and is a potent MK2 Inhibitor. ATI-450 binds with high affinity to the interface of the p38MAPK-MK2 complex and selectively inhibits p38MAPK-catalysed phosphorylation of MK2 which stabilises the inactive conformation of MK2, and subsequently reduces inflammatory cytokine levels. ATI-450 specifically blocks the downstream MK2-mediated inflammatory drive on the p38 pathway and may therefore avoid the tachyphylaxis associated with p38 inhibitors. Note CAS#1640282-42-3 is the active P-atropisomer. CAS# 1640282-44-5 is the inactive M-astropisomer. |
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| DC74846 |
BU-224 HCl |
BU-224 is a Putative I2 antagonist; and a high affinity ligand for the imidazoline I2 binding site (Ki = 2.1 nM). BU224 reverses cognitive deficits, reduces microgliosis and enhances synaptic connectivity in a mouse model of Alzheimer's disease. |
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| DC74847 |
Limaprost |
Limaprost, also known as ONO 1206 and OP1206, is an analog of PGE1 with structural modifications intended to give it a prolonged half-life and greater potency. Limaprost is orally active. Limaprost reduces motor disturbances by increasing the production of insulin-like growth factor I in rats subjected to spinal cord injury. |
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| DC74848 |
BMS193885 free base |
BMS-193885 is a potent, competitive neuropeptide (NPY) Y1 antagonist (Ki = 3.3 nM, IC50 = 5.9 nM) that displays > 47, > 100, > 160, > 160 and > 160-fold selectivity over σ1, α1, Y2, Y4 and Y5 receptors respectively. It reduces food intake and body weight via central Y1 inhibition and is brain penetrant. BMS-193885 has 3.3 nM affinity at the neuropeptide Y(1) receptor, acting competitively at the neuropeptide Y binding site. BMS-193885 increased the K(d) of [(125)I]PeptideYY from 0.35 nM to 0.65 nM without changing the B(max) (0.16 pmol/mg of protein) in SK-N-MC cells that endogenously express the neuropeptide Y(1) receptor. It is also found to be a full antagonist with an apparent K(b) of 4.5 nM measured by reversal of forskolin (FK)-stimulated inhibition of cAMP production by neuropeptide Y. |
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| DC74849 |
TAS-115 free base |
TAS-115, also known as Pamufetinib, is a c-MET Inhibitor. TAS-115 inhibited the kinase activity of both VEGFR2 and MET and their signal-dependent cell growth as strongly as other known VEGFR or MET inhibitors. TAS-115 is extremely selective and specific, at least in vitro. In in vivo studies, TAS-115 completely suppressed the progression of MET-inactivated tumor by blocking angiogenesis without toxicity when given every day for 6 weeks, even at a serum-saturating dose of TAS-115. TAS-115 induced marked tumor shrinkage and prolonged survival in MET-amplified human cancer-bearing mice. TAS-115 is a unique VEGFR/MET-targeted inhibitor with improved antitumor efficacy and decreased toxicity. |
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| DC74850 |
DeBio-1143 (AT-406) |
DeBio-1143, also known as AT-406, ARRY-334543and SM-406, is an orally bioavailable inhibitor of IAP (Inhibitor of Apoptosis Protein) family of proteins with potential apoptotic inducing and antineoplastic activity. AT-406 selectively inhibits the biological activity of IAP proteins, including X chromosome-linked IAP (XIAP), the cellular IAPs 1 (c-IAP1) and 2 (c-IAP2) and melanoma inhibitor of apoptosis protein (ML-IAP). This may restore and promote the induction of apoptosis through apoptotic signaling pathways. AT-406 may work synergistically with cytotoxic drugs to overcome tumor cell resistance to apoptosis. |
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| DC74851 |
CO101244 HCl |
CO-101244, also known as RO-63-1908 and PD-174494, is a novel, potent and selective antagonist of NR2B-containing NMDA receptors (IC50 values are 0.043, > 100 and > 100 μM for NR1A/2B, NR1A/2A and NR1A/2C subunit combinations respectively). CO-101244 displays neuroprotective effects in vivo and in vitro. |
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| DC74852 |
Dov-Val-Dil-OH TFA |
Dov-Val-Dil-OH is a useful chemical intermediate for synthesis of auristatin-related compounds, such as Monomethyl auristatin E (MMAE), Auristatins are antimitotic agents which inhibits cell division by blocking the polymerisation of tubulin. |
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| DC74853 |
CZC-54252 HCl |
CZC-54252 is a potent inhibitor of leucine-rich repeat kinase 2 (LRRK2) with IC50 values 1.28 nM and 1.85 nM for wild-type and G2019S mutant forms of LRRK2 respectively. CZC-54252 attenuates neuronal injury induced by LRRK2-G2019S mutant activity in primary human neurons (EC50 = 1 nM). Activating mutations in leucine-rich repeat kinase 2 (LRRK2) are present in a subset of Parkinson's disease (PD) patients and may represent an attractive therapeutic target. |
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| DC74854 |
HLCL-61 HCl |
HLCL-61 is a potent and selective PRMT5 inhibitor for treatment of acute myeloid leukemia. HLCL-61 resulted in significantly increased expression of miR-29b and consequent suppression of Sp1 and FLT3 in AML (acute myeloid leukemia) cells. As a result, significant antileukemic activity was achieved. The increased PRMT5 activity enhanced AML growth in vitro and in vivo while PRMT5 downregulation reduced it. In AML cells, PRMT5 interacted with Sp1 in a transcription repressor complex and silenced miR-29b preferentially via dimethylation of histone 4 arginine residue H4R3. |
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| DC74855 |
GSK269962 |
GSK269962 is a selective ROCK inhibitor with IC50 values of 1.6 and 6 nM for ROCK-I and ROCK-II, respectively. GSK269962 can become an alternative worth considering in OAB treatment. |
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| DC74856 |
AZD6482 (S-isomer) |
AZD6482 (S-isomer), CAS#1173900-37-2, is an isomer of AZD6482 (MedKoo Cat#406268) with S-configuration. AZD6482 is a potent, selective and ATP competitive PI3Kβ inhibitor (IC(50) 0.01 μm). AZD6482 inhibited insulin-induced human adipocyte glucose uptake in vitro (IC(50) of 4.4 μm). This is the first human target validation for PI3Kβ inhibition as anti-platelet therapy showing a mild and generalized antiplatelet effect attenuating but not completely inhibiting multiple signaling pathways with an impressive separation towards primary hemostasis. AZD6482 at 'supratherapeutic' plasma concentrations may attenuate insulin signaling, most likely through PI3Kα inhibition. |
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| DC74857 |
XI-011 HCl |
XI-011 (NSC146109), a small-molecule inhibitor of MDMX, showed robust anti-proliferation activity against several cervical cancer cell lines. XI-011 promoted apoptosis of cervical cancer cells via stabilizing p53 and activating its transcription activity. Moreover, XI-011 inhibited the growth of xenograft tumor in HeLa tumor-bearing mice, as well as enhanced the cytotoxic activity of cisplatin both in vitro and in vivo. |
|
| DC74858 |
SRI-37330 free base |
SRI-37330 is an orally bioavailable, non-toxic small molecule TXNIP inhibitor. SRI-37330 effectively rescued mice from streptozotocin- and obesity-induced (db/db) diabetes. SRI-37330 inhibited expression and signaling of thioredoxin-interacting protein, SRI-37330 treatment inhibited glucagon secretion and function, reduced hepatic glucose production, and reversed hepatic steatosis. Rescue assays confirmed that the impact of FTO on the TXNIP/NLRP3 pathway was significantly reversed by the TXNIP inhibitor SRI-37330. |
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| DC74859 |
BMS-345541 HCl |
BMS 345541 is a selective allosteric inhibitor of IKK (IC50 values are 0.3 and 4.0 μM for IKKβ and IKKα respectively). It attenuates LPS-induced cytokine production in vitro and blocks NFκB dependent transcription in mice. BMS 345541 also suppresses joint destruction in a mouse model of arthritis. |
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| DC74860 |
PXS-5505 free base |
PXS-5505 is a Pan-Lysyl Oxidase Inhibitor that has been found to ameliorate multiple-organ fibrosis by inhibiting collagen crosslinks in rodent models in systemic sclerosis. PXS-5505 inhibited lysyl oxidase activity in the skin and LOXL2 activity in the lung. PXS-5505 exhibited anti-fibrotic effects in the SSc skin mouse model, reducing dermal thickness and α-smooth muscle actin. Similarly, in the bleomycin-induced mouse lung model, PXS-5505 reduced pulmonary fibrosis toward normal levels, mediated by its ability to normalise collagen/elastin crosslink formation. PXS-5505 also reduced fibrotic extent in models of the ischaemia-reperfusion heart, the unilateral ureteral obstruction kidney, and the CCl4-induced fibrotic liver. |
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