p12

Nelarabine (GW 506U78) is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells.

GPR110 peptide agonist P12 is a peptide that acts as an agonist for GPR110. This compound markedly enhances the initial rate of G protein GTPγS binding stimulated by GPR110. It mimics the action of the natural ligand, causing the extracellular domain (ECD) of GPR110 to dissociate from the seven-transmembrane domain (7TM) and exposing the N-terminal β-strand-13 stalk region of the 7TM domain, which acts as the agonist activating G protein signaling. GPR110 peptide agonist P12 is applicable in research related to developmental disorders and cancers associated with GPR110.

GPR110 peptide agonist P12 acetate is an acetate form of GPR110 peptide agonist P12 and acts as a potent agonist for GPR110. This peptide significantly enhances the initial rate of G protein GTPγS binding stimulated by GPR110. By mimicking the action of natural ligands, GPR110 peptide agonist P12 acetate causes the extracellular domain (ECD) of GPR110 to dissociate from the seven transmembrane domain (7TM), revealing the N-terminal β-strand-13 stalk region of the 7TM domain, which facilitates the activation of G protein signaling. This compound is utilized in research related to developmental disorders and cancers associated with GPR110.

FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional compound that selectively degrades the BET bromodomain transcriptional co-activator BRD4 by linking BET bromodomains to the E3 ubiquitin ligase CRBN. It also functions as a degrader of FKBP12F36V when FKBP12F36V is expressed in-frame with a targeted protein.

PP-121 is a multi-targeted inhibitor of PDGFR (IC50: 2 nM), Hck (IC50: 8 nM), mTOR (IC50: 10 nM), VEGFR2(IC50: 12 nM), Src (IC50: 14 nM) and Abl (IC50: 18 nM) , also inhibits DNA-PK (IC50: 60 nM).

gp120-α4β7 binding inhibitor 11 is an anti-HIV agent. gp120-α4β7 binding inhibitor 11 interferes the binding of HIV associated glycoprotein gp12G with the integrin α4β7 (IC50=1.64nM).

FKBP12 PROTAC dTAG-13 is a PROTAC and selective degrader that can be used for target validation during drug discovery by splicing FKBP12 F36V with CRBN and thereby degrading FKBP12 F36V.

FKBP12 PROTAC RC32 is a PROTAC-like degrader targeting FKBP12. It can degrade FKBP12 in organs after intraperitoneal administration.

Fructo-oligosaccharide DP12 GF11 is a member of fructooligosaccharides (FOS) characterized by a degree of polymerization (DP) of 12. FOS compounds consist of 11 fructose units connected by (2→1)-β-glycosidic bonds, with a lone D-glucosyl unit located at the non-reducing end.

UP12 enhances ATPase activity by activating valosin-containing protein (VCP), with an EC50 of 2.57 μM.

FKBP12 Ligand-Linker Conjugate 1 is a complex comprising a target protein ligand for FKBP12 and a linker, which is utilized in the synthesis of the PROTAC degrader MC-25B.

FKBP12 ligand-1 is the target protein ligand for MC-25B, which is a PROTAC targeting FKBP12.

TOP1210, a narrow spectrum kinase inhibitor, potently inhibits P38α, Src, and Syk kinase activities.

gp120-IN-2 (compound 4i) is a potent inhibitor of HIV-1 gp120, demonstrating anti-HIV-1 activity with an IC50 of 7.5 μM and a CC50 of 112.93 μM. It shows dose-dependent cytotoxicity in SUP-T1 cells [1].

gp120-IN-1 (compound 4e) is a potent HIV-1 gp120 inhibitor with a CC50 of 100.90 μM and IC50 of 2.2 μM, inhibiting gp120-mediated virus entry into cells and exhibiting anti-HIV-1 activity with dose-dependent cytotoxicity in SUP-T1 cells [1].

CYP121A1-IN-1 is a potent inhibitor of CYP121A1, demonstrating favorable activity against Mycobacterium tuberculosis (H37Rv MIC 90 ~6.25 μM, ~2.2 μg mL). It significantly reduces mycocyclosin production by blocking the CYP121A1-mediated conversion of cyclo(l-tyrosyl-l-tyrosyl) to mycocyclosin [1].

TP-1287 is an oral phosphate prodrug of the CDK9 inhibitor, alvocidib.

SLP120701 is a potent and selective sphingosine kinase 2 inhibitor. Sphingosine-1-phosphate (S1P) is a ubiquitous, endogenous small molecule that is synthesized by two isoforms of sphingosine kinase (SphK1 and 2). Intervention of the S1P signaling pathway has attracted significant attention because alteration of S1P levels is linked to several disease states including cancer, fibrosis, and sickle cell disease.

FKBP12-IN-Q2 is an inhibitor of FKBP12.

GP120, HIV-1 MN, a peptide, is utilized in researching HIV infection [1] [2].

(Asn10,Leu11,D-Trp12)-pTH-Related Protein (7-34) amide (human, mouse, rat) is a potent antagonist of the PTH-1R [1][2].

EP12, a c-Myc inhibitor and G4 stabilizer, induces apoptosis and DNA damage in multiple myeloma cells while obstructing P65 P50 nuclear translocation by disrupting the NF-κB signaling pathway, effectively inhibiting multiple myeloma growth [1].

Pap12-6, an antibacterial peptide originating from the first twelve N-terminal amino acids of papiliocin found in P. xuthus larvae, exhibits activity against a range of eight Gram-negative bacteria (e.g., E. coli, P. aeruginosa, S. syphimurium with MIC50s=4-8 µM) and Gram-positive bacteria (e.g., S. aureus, methicillin-resistant S. aureus 3126, B. subtilis, and S. epidermidis with MIC50s=4-8 µM), without compromising the viability of human erythrocytes, mouse RAW 264.7 macrophages, human HaCaT keratinocytes, or human HEK293 kidney cells at 25 µM. It causes membrane depolarization in E. coli at 4 and 8 µM and, upon preincubation at 10 µM, decreases nitrite (NO2-), Tnf-α, and Il-6 secretion in LPS-stimulated RAW 264.7 macrophages. In a murine model, Pap12-6 enhances survival rates and diminishes colony forming units (CFUs) in several organs upon E. coli infection at 10 mg/kg and 1 mg/kg doses, respectively. Additionally, at a 1 mg/kg dose, it lowers serum aspartate aminotransferase (AST) and alanine transaminase (ALT) levels, as well as blood urea nitrogen levels in E. coli-induced sepsis, indicating its therapeutic potential for bacterial infections without affecting host cell viability.

Tat-QFNP12 is a peptide that combines a transcriptional transactivator (Tat) transmembrane domain with an inhibitor targeting the interaction between N-Myc downstream regulated gene 2 (NDRG2) and protein phosphatase Mg2+/Mn2+ dependent 1A (PPM1A). This compound effectively mitigates blood-brain barrier endothelial tight junction disruption caused by elevated levels of matrix metalloproteinase-9 (MMP-9), alleviates cerebral edema, and promotes spontaneous activity along with symmetric limb movement in a mouse model of subarachnoid hemorrhage induced by endovascular puncture. These benefits are observed at a dosage of 20 mg/kg.