p27

p27 is a CDK inhibitor and a substrate of SCFSkp2/Cks1, useful for cancer research.

SJ572403 is an inhibitor of disordered protein p27 with Kd of 2.2 mM for specific regions within the D2 subdomain of p27-KID. SJ572403 can be used in studies about diseases with intrinsically disordered proteins.

Pralatrexate (10-Propargyl-10-deazaaminopterin) is a folate analogue inhibitor of dihydrofolate reductase (DHFR) exhibiting high affinity for reduced folate carrier-1 (RFC-1) with antineoplastic and immunosuppressive activities.

p27 Analogue CP2 is a macrocyclic peptide inhibitor that targets the SCFSkp2/Cks1 E3 ubiquitin ligase complex (Kd=32 nM). By preventing the ubiquitination and subsequent degradation of the p27 protein mediated by SCFSkp2/Cks1, it helps restore p27 levels and inhibits cell proliferation. This compound shows potential for research on cancers that rely on Skp2 overexpression, such as breast cancer.

HSP27 inhibitor J2 (J2) (J2) is a HSP27 inhibitor, inhibits a production of HSP27 giant polymers, thereby having an effect of inhibiting a chaperone function of the HSP27 and reducing a cell protection function.

SP27, a selective PROTAC, degrades PLK4 with a DC50 of 19.5 nM and may be utilized in breast cancer research [1].

DiaPep277, a 24 amino acid peptide sourced from HSP60 positions 437-460, impedes β-cell destruction in NOD mice and modulates diabetogenic T-cell activity in animal diabetes models [1] [2].

Connexin mimetic peptide 40GAP27, corresponding to the GAP27 domain of the second extracellular loop of the dominant vascular connexin (Cx40), designated as 40Gap27, is a biologically active peptide utilized to study the pathways by which oxidant stress hinders gap junction communication. Administered 40Gap27 attenuates endothelium-dependent subintimal smooth muscle hyperpolarization.

Talmapimod (SCIO-469) is a selective, orally active, ATP-competitive p38α inhibitor with IC50 values of 9 nM for p38α and 90 nM for p38β. Talmapimod exhibits at least 2000-fold selectivity over a panel of 20 kinases, including other MAPKs.

CYM50260 is a potent and highly selective agonist of the sphingosine-1-phosphate 4 receptor (S1P4-R, EC50= nM), exhibiting no activity against S1P1-R, S1P2-R, S1P3-R, and S1P5-R.

Tolnaftate (NP-27) is a synthetic antifungal agent used to treat skin infections caused by fungi.

Orphenadrine hydrochloride (Mephenamin) is a muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm.

CC0651 is a highly selective allosteric inhibitor of human Cdc34 ubiquitin-conjugating enzyme (UCE), inhibiting p27 Kip1 ubiquitination (IC50=1.72 μM) by blocking ubiquitin transfer to substrates, for use in cancer research.

Riviciclib is a potent inhibitor of cyclin-dependent kinase (CDK)(CDK9-cyclinT1, CDK4-cyclin D1, and CDK1-cyclinB with IC50s of 20 nM, 63 nM, and 79 nM, respectively),with antitumor activity on cisplatin-resistant cells.

Doxorubicinol is the major circulating metabolite of doxorubicin with antineoplastic acitivity.

R-PEP 27 is an inhibitor of potent renin, decreased plasma angiotensin II, and blood pressure in normal volunteers.

TP-271, a tetracyclines antibiotic, is used potentially for the treatment of community-acquired bacterial pneumonia (CABP).

VTP-27999, an alkyl amine Renin inhibitor, has been utilized in trials studying the basic science of Renal Function.

3-Aminopropylphosphinic acid (3-APPA), a phosphonic analog of gamma-aminobutyric acid (GABA), acts as a potent and selective agonist of the GABA B receptor.

VTP-27999 HCl is an alkyl amine renin inhibitor, useful for treating hypertension and end-organ diseases. IC50 value: Target: Renin.

TCS-PIM-1-4a (SMI-4a), a Pim inhibitor, blocks mTORC1 activity through activation of AMPK and kills a wide range of both myeloid and lymphoid cell lines (IC50=0.8-40 μM).

Orphenadrine Citrate (Flexon) is a skeletal muscle relaxant, it acts in the central nervous system to produce its muscle relaxant effects.

NSC-87877 disodium (NSC87877) is a cell-permeable inhibitor of both SHP-1 and SHP-2 with IC50 values of 355 and 318 nM respectively. It also inhibits EGF-induced Erk1/2 activation in HEK293 cells and significantly reduces MDA-MB-468 cell viability/proliferation.

Riviciclib hydrochloride (P276-00) is a novel inhibitor of CDK1, CDK4, and CDK9, with IC50 values of 79 nM, 63 nM, and 20 nM, respectively, currently in Phase 2/3.