kp-1

KP-1 is a selective fluorescent probe for labeling human pluripotent stem cells.

SA1-III(KP1) is a bioactive peptide recognized for its anti-aging properties and is utilized as a cosmetic ingredient [1].

Klotho-derived peptide 1 (KP1) (56-87), a peptide originating from the human Klotho protein, disrupts TGF-β signaling by binding to TGF-β receptor types 1 and 2 (TGFBR1 and TGFBR2; Kds = 1.41 and 14.6 µM, respectively). Preincubation with KP1 at a concentration of 10 µg/ml hinders the TGF-β-induced escalation of fibronectin and α-smooth muscle actin (α-SMA) levels in NRK-49F rat fibroblasts. Furthermore, in vivo studies reveal that KP1, administered at 1 mg/kg per day, preferentially accumulates in damaged kidneys, leading to significant reductions in serum creatinine and blood urea nitrogen levels, indicators of improved kidney function. Additionally, it decreases kidney fibrosis in mouse models of unilateral ureteral obstruction (UUO) and unilateral ischemia-reperfusion injury-induced renal fibrosis.

Klotho-derived peptide 1 (KP1 human) can inhibit the interaction between TGF-β and its receptor TGF-β receptor 2, suppressing the activation of Smad2/3 and mitogen-activated protein kinase (MAPK) induced by TGF-β. It shows anti-fibrotic and renal protective effects in mouse models.

KP-14 is a PROTAC specifically designed to target KRAS.

IKP-104 is a microtubule/tubulin inhibitor (IC50 = 1.31 μM) that halts cells in mitosis and the M phase by inhibiting microtubule assembly and inducing cytoskeleton microtubule depolymerization. It suppresses the growth of both murine and human tumor cell lines, exhibiting antitumor effects in mouse ascites tumor and lung cancer models. IKP-104 is applicable in research on cancers such as leukemia, lung cancer, and melanoma.

KP-1212( SN-1212) is a nucleoside designed for the treatment of HIV by viral mutagenesis.

AKP-11 is a sphingosine-1-phosphate receptor 1 (S1P1) agonist with an EC50 of 0.047 μM for [35S]GTPγS binding to CHO-K1 cell membranes expressing human S1P1. It reduces S1P1 surface expression and enhances Akt and ERK phosphorylation in CHO cells with S1P1-HA at a 100 nM concentration. At doses of 1.3 and 3 mg/kg, AKP-11 lowers IFN-γ and IL-17 protein levels in the spinal cord and mitigates disease severity in a rat experimental autoimmune encephalomyelitis (EAE) model. Additionally, it decreases peripheral total lymphocyte and specific T cell subsets (CD4+, CD8+, and CD26L+ T cells) counts in both EAE rats and healthy controls at a 1.3 mg/kg dosage.

Canine KP-10 is a potent kisspeptin that induces a significant gonadotropin and estradiol response in female dogs during estrus.

NKP-1339 (IT-139) induces G2/M cell cycle arrest, blockage of DNA synthesis, and induction of apoptosis via the mitochondrial pathway.

CX-157 (KP 157) is a novel monoamine oxidase-A (MAO-A) inhibitor for the study of depression-like neurological disorders and cancer.

KP136 (AL136) is an orally active anti-allergic compound that inhibits histamine release and is used in studies of asthma and allergic edema.

Relenopride (YKP 10811) is a selective 5-HT4 receptor agonist that promotes intestinal motility and is used in the study of intestinal disorders.

Efinaconazole (KP-103)(KP-103) is an Azole Antifungal currently under development as a topical treatment for onychomycosis.

Vensobafusp alfa (KP-104) is a fusion protein composed of an IgG4 monoclonal antibody targeting complement protein C5, combined with the domains 1-5 of complement factor H (FH1-5). It exhibits anti-inflammatory and immunomodulatory properties. The isotype control for Vensobafusp alfa can be referred to as human IgG4(S228P) kappa.

SMER3 is an inhibitor of the Skp1-Cullin-F-box (SCF)(Met30) ubiquitin ligase, a member of the SCF E3-ligase family, which regulates diverse cellular processes including transcription, cell-cycle control and immune response.

Relenopride, a 5-HT agonist, is used potentially for the treatment of chronic constipation.

KP1019 is now discontinued.

KP 10614 is a new prostacyclin analog that inhibits platelet-polymorphonuclear leukocyte interaction.

RKS262 is a specific cyclin/CDK inhibitor. RKS262 was identified by structural optimization of Nifurtimox which is currently undergoing phase II clinical trials to treat high-risk neuroblastoma. In a NCI(60) cell-line assay RKS262 exhibited significant cytotoxicity in ovarian cancer cells and a variety of other cell lines exceeding effects of commercial drugs such as cisplatin, 5-FU, cyclophosphamide or sapacitabine. Various leukemia cell-lines were most sensitive (GI(50): ~ 10 nM) while several non-small cell lung cancer cell lines and few cell lines from other tissues were relatively resistant (GI(50) > 1 µM) to RKS262 treatment.

Ravidasvir, also known as PPI-668 and ASC16, is a second-generation, orally active, potent and selective HCV NS5A protein inhibitor.

BOLD-100 free base (NKP-1339; IT-139), a ruthenium-based anticancer agent, inhibits stress-induced GRP78 upregulation, thus disrupting endoplasmic reticulum (ER) homeostasis. This action induces ER stress and unfolded protein response (UPR), interfering with the intricate relationship between ER-stress response, lysosome dynamics, and autophagy execution.

γ-Secretase modulator 12 (Compound 1a) is a selective compound that effectively reduces amyloid-β42 (Aβ42) levels with an IC50 of 0.39 μM, specifically designed for Alzheimer's disease research. Notably, γ-Secretase modulator 12 exhibits a favorable brain/plasma ratio (Kp, brain = 0.72) in mice [1].

ASK1-IN-6 (Compound 32), a selective apoptosis signal-regulating kinase 1 (ASK1) inhibitor, exhibits an IC50 of 25 nM. This compound readily crosses the blood-brain barrier, as evidenced by rat pharmacokinetics showing a clearance/unchanged clearance rate of 1.6/56 L/h/kg and an unbound partition coefficient (Kp,uu) of 0.46. Additionally, ASK1-IN-6 demonstrates anti-inflammatory activity and effectively improves symptoms in the Alzheimer's Disease Tg4510 mouse model.