p42

Zibotentan (ZD4054) (ZD4054) is a specific Endothelin (ET)A antagonist with IC50 of 21 nM, exhibiting no activity at ETB. Phase 3.

CYM5442 is an S1P agonist, targeting to Sphingosine.

Albofungin is a xanthone isolated from A. tumemacerans.

NTP42 is an antagonist of thromboxane A2 (TXA2) receptor(IC50 of 3.278 nM)

SP4206 is an interaction inhibitor of IL-2/IL-2Rα (IL-2 and IL-2Rα with Kd of 70 nM and 10 nM,respectively)

AMP423 is a naphthyl derivative of 2-cyanoaziridine-1-carboxamide with structural similarity to the pro-oxidant anti-tumor agent imexon. AMP423 was active in SCID mice bearing 8226/S myeloma and SU-DHL-6 B-cell lymphoma tumors, with a median tumor growth delay (T-C) of 21 days (P = 0.0002) and 5 days (P = 0.004), respectively, and a median tumor growth inhibition (T/C) of 33.3% (P = 0.03) and 82% (P = 0.01), respectively. In non-tumor-bearing mice, AMP423 was not myelosuppressive.

Pep42 TFA, a cyclic peptide ligand of GPR78, selectively internalizes into highly metastatic human melanoma cells through a receptor-mediated process.

Zoledronic acid monohydrate (CGP 42446) is a synthetic imidazole bisphosphonate analog with anti-bone-resorption activity.

Zoledronic Acid (ZOL 446) is a bisphosphonate. Zoledronic Acid (ZOL 446) is used to prevent skeletal fractures in patients with cancers such as multiple myeloma and prostate cancer. It can also be used to treat hypercalcemia of malignancy and can be helpful for treating pain from bone metastases. An annual dose of Zoledronate may also prevent recurring fractures in patients with a previous hip fracture. Zoledronic Acid (ZOL 446) is a single 5 mg infusion for the treatment of Paget's disease of bone. In 2007, the FDA also approved Reclast for the treatment of postmenopausal osteoporosis.

LSP4-2022 is a selective, blood-brain barrier-permeable mGlu4 orthosteric agonist (EC50 = 0.11 μM) capable of inhibiting neurotransmission in wild-type mouse cerebellar slices, exhibiting pro-depressive activity.

USP7-IN-4(USP7 inhibitor ALM4) is a non-competitive, potent and selective inhibitor of USP7 (ubiquitin-specific protease 7) with an IC50 = 6 nM, up-regulates p53 and p21, down-regulates MDM2, increases the level of ubiquitination of MDM2, and exhibits anti-proliferative activity in a variety of cancer cell lines, with an EC50 = 2.0 nM in RS4;11 (acute lymphoblastic leukemia cell line) .

CGP-42112 acetate is a potent angiotensin receptor AT2 agonist that inhibits the increase in protein kinase A activity produced by LPS.

AG126 (Tyrphostin AG126) selectively inhibits the phosphorylation of ERK1 (p44) and ERK2 (p42) at 25-50 μM. It blocks the production of TNF-α in vitro2 and in vivo, attenuating signaling through NF-κB, the induced expression of COX-2 and iNOS, and the inflammatory response in diverse animal models. AG-126 weakly inhibits epidermal GFRK (IC50: 450 μM) and platelet-derived GFRK (IC50 > 100 μM).

CGP-42112 is an agonist of the Angiotensin-II subtype 2 receptor (AT2 R).

VKT-17-P4-23 is a blood-brain barrier-permeable DksA inhibitor targeting the highly conserved transcriptional regulator DksA in Gram-negative bacteria, with a Kd value of 124 μM. Through modulation of the DksA-regulated SPI-2-dependent survival pathway, VKT-17-P4-23 exhibits antibacterial activity against planktonic and intracellular pathogens including Salmonella and additionally demonstrates activity against persistent bacterial populations that are difficult to eradicate. VKT-17-P4-23 is applicable to investigations involving Salmonella infection, bacterial persistence mechanisms, and transcriptional regulation in pathogenic bacteria.

LMP-420 is a selective inhibitor of tumor necrosis factor-α (TNF-α). It reduces the release of pro-inflammatory cytokines, such as IL-1β and IL-2, while inducing the expression of anti-inflammatory cytokine IL-10, and anti-apoptotic molecules SOCS-1 and Mn-SOD. LMP-420 also downregulates chemokines like IP-10 and MCP-1, which decreases immune cell infiltration. This compound shows potential for research into type 1 diabetes, inflammatory diseases such as colitis, and HIV-mycobacterium tuberculosis co-infection.

Capromorelin, a member of the growth hormone secretagogue (GHS) class of drugs, is a ghrelin receptor agonist and a novel therapy for stimulation of appetite in dogs with Ki value of 7 nM for hGHS-R1a and EC50 value of 3 nM for rat pituicyte. Capromorelin

TP-0427736 is a novel potent and selective ALK5 inhibitor (IC50: 2.72 nM). P0427736 was 300-fold higher than the inhibitory effect on ALK3. TP0427736 reduces TGF-β induced growth inhibition in human outer root sheath cells and elongates the anagen phase i

Albonoursin is used as an antibacterial cyclic dipeptide.

CGP-42454A is a bio-active chemical.

TP-422 is a negative control for TP-238.

SP-420 is a novel orally active iron chelator.

Telaprevir (Incivek) (VX-950) is an effective inhibitor of HCV NS3-4A serine protease (IC50: 0.35 μM).

NVP018, also known as BC 556, is a potent inhibitor of hepatitis B virus, hepatitis C virus (HCV), and HIV-1 replication, shows minimal inhibition of major drug transporters, and has a high barrier to generation of both HCV and HIV-1 resistance..