p21

BIX-01294 is an G9a Histone Methyltransferase inhibitor(IC50 : 1.9 μM).

BRK inhibitor P21d hydrochloride is a highly potent inhibitor of breast tumor kinase (BRK PTK6), displaying an IC50 of 30 nM, and effectively suppresses p-SAM68 with an IC50 of 52 nM. This compound serves as a valuable tool for evaluating BRK inhibitors' efficacy in xenograft breast tumor models, enabling in vivo activity assessment.

NP213 TFA is a rapidly acting and first-in-class synthetic antimicrobial peptide (AMP) with anti-fungal activity. It targets the fungal cytoplasmic membrane via membrane perturbation and disruption.

CP21 is an iron chelator that binds to iron in a 3:1 (ligand:iron) ratio. It is active against P. falciparum when used at concentrations of 10 and 100 µM. CP21 inhibits production of prostaglandin I2 induced by epinephrine, arachidonic acid, or A23187 in isolated rat aortic rings with IC50 values of 1.3, 1.3, and 1.4 mM, respectively. It inhibits glutamate-induced oxytosis, as well as decreases iodoacetic acid-induced cytotoxicity in an in vitro model of ischemia, in HT22 mouse hippocampal cells (EC50s = 13 and 9.5 µM, respectively). CP21 (200 mg kg) increases the excretion of iron, but not copper, zinc, calcium, or magnesium, in rabbits.

p21PBP, a peptide composed of 20 amino acids, serves as an inhibitor of DNA replication. It specifically binds to the purified proliferating cell nuclear antigen (PCNA) found in extracts from tumor cells. p21PBP holds potential for use in cancer research.

R-HP210 inhibits LPS-induced transcription of several pro-inflammatory genes (IL-1β, IL-6 and COX-2). r-HP210 has an IC50 value of 3.80 μM for NF-κB-mediated bolus trans-suppression. r-HP210 does not induce trans-activation of glucocorticoids (GCs).

HP211206 is a PROTAC degrader of the SARS-CoV-2 main protease (Mpro). It effectively degrades both the SARS-CoV-2 Mpro and its resistant mutants. The IC50 for HP211206 against Mpro is 181.9 nM, and the DC50 is 621 nM. HP211206 also exhibits antiviral activity.

NP213 is a rapidly acting synthetic antimicrobial peptide (AMP). NP213 is effective and well-tolerated in resolving nail fungal infections. NP213 has anti-fungal activities. NP213 targets the fungal cytoplasmic membrane and plays its role via membrane perturbation and disruption.

AP39 is a compound used to increase hydrogen sulfide (H2S) levels within mitochondria; it consists of a mitochondria-targeting motif (triphenylphosphonium) coupled to an H2S-donating moiety (dithiolethione) by an aliphatic linker. AP219, as a control compound for AP39, contains the triphenylphosphonium scaffold but lacks the H2S-releasing portion.

HP210, a selective glucocorticoid receptor modulator (SGRM), can suppress IL-1β and IL-6 mRNA expression, suggesting its utility in investigating inflammation-related diseases [1].

CP21R7 (CP21) is an effective and specific GSK3β inhibitor. It is used as an activator of stem cells prior to the induction of differentiation of stem cells to smooth muscle and endothelial cells. CP21R7 can be combined with BMP4 to commit human pluripotent stem cells to a mesodermal fate.

P21d hydrochloride is a potent and selective breast tumor Ki nase (Brk) inhibitor (IC50 = 30 nM). Exhibits >650-fold selectively for Brk over Aurora B Ki nase and Lck. Downregulates SNAIL protein, restores E-cadherin expression and suppresses migration in breast cancer cells. Also activein vivoand orally bioavailable.

S-HP210 is a selective and potent glucocorticoid receptor (GR) modulator that inhibits NF-κB transcription (IC50: 1.92 μM). S-HP210 is not toxic to mouse fibroblasts at effective doses of 3T3.

Anti-Mesothelin Antibody (YP218) is a chimeric rabbit IgG antibody that targets human Mesothelin.

5-Aminosalicylic Acid (5-ASA) is an anti-inflammatory agent, structurally related to the SALICYLATES, which is active in INFLAMMATORY BOWEL DISEASE. It is considered to be the active moiety of SULPHASALAZINE.

G-5555 is a potent inhibitor of p21-activated kinase 1 (PAK1) (Kis: 3.7 nM and 11 nM for PAK1 and PAK2, respectively).

Vesnarinone (Arkin) (INN) is a mixed phosphodiesterase 3 inhibitor and ion-channel modifier that has modest, dose-dependent, positive inotropic activity, but minimal negative chronotropic activity. It also suppresses cell proliferation and induces apoptosis by inducing the expression of p21, an inhibitor of cyclin-dependent kinase activity in p53-mediated cell cycle arrest.

Perillyl Alcohol is a naturally occurring monoterpene related to limonene with antineoplastic activity. Perillyl alcohol (Isocarveol) inhibits farnesyl transferase and geranylgeranyl transferase, thereby preventing post-translational protein farnesylation and isoprenylation and activation of oncoproteins such as p21-ras, and arresting tumor cells in the G1 phase of the cell cycle.

O6-Benzylguanine is a guanine analog with antineoplastic activity,and is a potent O6-alkylguanine DNA alkyltransferase (AGT) inactivator.

Fingolimod hydrochloride (FTY720) , a novel immune modulator, is a sphingosine 1-phosphate (S1P) antagonist (IC50: 0.033 nM in K562 and NK cells).

Fingolimod (FTY-720A) is an antagonist of sphingosine 1-phosphate (S1P) (IC50 of 0.033 nM in K562 and NK cells).

Aspirin (Acetylsalicylic Acid) is a COX inhibitor that inhibits COX1 and COX2 (IC50=5 210 μg mL) with selective, irreversible, and oral activity. Aspirin is also a histone deacetylase inhibitor that up-regulates the cell cycle blocking protein, p21. Aspirin has a variety of activities. Aspirin has anti-inflammatory, antipyretic and analgesic, and antiplatelet aggregation activities.

β-Carotene (Provitamin A) is a naturally-occurring retinol (vitamin A) precursor obtained from certain fruits and vegetables with potential antineoplastic and chemopreventive activities. As an anti-oxidant, beta carotene inhibits free-radical damage to DNA.

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) .