Search results for: 'leu31-pro34-neuropeptide-y-human-rat'
- A-740003Catalog No. :A3136P2X7 receptor antagonistA-740003 is a novel competitive antagonist of P2X7 receptors with IC50 values of 40 nM for human and 18 nM for rat. .
- Ki16425Catalog No. :A1987LPA receptor antagonist
Ki16425 is a subtype-selective antagonist of lysophosphatidic acid receptor (LPA) with Ki values of 0.34 μM for LPA1, 6.5μM for LPA2, and 0.93μM for LPA3 .
- AprepitantCatalog No. :A1684Substance P (SP) inhibitorAprepitant (also known as MK-0869) is a novel and highly selective Neurokinin-1 (NK-1) receptors that inhibits the activity of substance P (SP), an undecapeptide belonging to the tachykinin family of peptides, on the NK-1 receptor with the dissociation constant Kd of 86 pM for human NK-1 receptor and the half maximal inhibition concentration IC50 of 0.1 nM, 4 nM and 0.7 nM for human, rat and ferret NK-1 receptors respectively [1,2].
- LDE225 (NVP-LDE225,Erismodegib)Catalog No. :B2266Smoothened inhibitor,potent and selective
LDE225 is a potent and selective inhibitor of smoothened with IC50 values of 1.3nM in mouse and 2.5nM in human, respectively .
- 2,3-DCPE hydrochlorideCatalog No. :A4447Bcl-XL protein expression downregulatorSelectively induces apoptosis and downregulates Bcl-XL protein expression in various human cancer cells versus normal cells in vitro. IC50 values are 0.89 and 12.6 μM for LoVo human colon cancer cell line and normal human fibroblasts respectively. Induces p21 expression and S-phase arrest in cancer cells via ERK-mediated pathways.
- AZD-5438Catalog No. :A8326Potent CDK1/2/9 inhibitor
AZD5438 is a potent small molecule inhibitor of cyclin-dependent kinase (CDK) 1, 2 and 9 with half maximal inhibitory concentration IC50 of 16 nmol/L, 6 nmol/L and 20 nmol/L respectively. AZD5438 has also been found to potently inhibit the human cyclin E/CDK2 complex, the cyclin B1/CDK1 complex and the cyclin A/CDK2 complex with IC50 of 0.006 μM, 0.016 μM and 0.045 μM respectively. In previous studies, AZD5438 has exhibited significant anti-proliferative activity in a few human tumor cell lines with IC50 ranging from 0.2 μmol/L to 1.7 μmol/L, in which the phosphorylation of a few proteins, including CDK substrates pRb, nucleolin, protein phosphatase 1a and RNA polymerase II COOH-terminal domain, and cell cycling at G2-M, S and G1 phases were inhibited.
- AM966Catalog No. :A3170LPA1 antagonist, oral active, high affinity, selective,
AM966 is a selective, potent and orally bioavailable antagonist of lysophosphatidic acid type 1 receptor (LPA1) with IC50 values of 17 and 19 nM for human or mouse LPA1, respectively . Relative to LPA2, 3, 4, 5 receptors, AM966 shows 10-fold and 100-fold more selective in mouse and human cell lines for LPA1, respectively .
- Paclitaxel (Taxol)Catalog No. :A4393Antineoplastic agent
Paclitaxel is a novel antineoplastic agent, which was discovered in a screen of extracts of thousands of plants and natural products for antineoplastic activity by a National Cancer Institute program.
- GW9662Catalog No. :A4300PPARγ antagonistGW9662 is a potent antagonist of PPARγ with IC50 value of 3.3nM .
- NSC 405020Catalog No. :A4051MT1-MMP inhibitorNSC-405020 is a novel small molecule inhibitor of membrane type-I matrix metalloproteinase (MT1-MMP) that specifically targets the hemopexin (PEX) domain rather than the catalytic domain of MT1-MMP with 50% inhibition concentration IC50 value larger than 100 μmol/L and does not inhibit the catalytic activity of MT1-MMP or MMP-2.