CK-666 is a cell-permeable inhibitor of actin-related protein Arp2/3 complex, and binds to Arp2/3 complex, stabilizes the inactive state of the complex, blocking movement of the Arp2 and Arp3 subunits into the activated filament-like (short pitch) conformation[1].
(Lys(Ac)5,8,12,16)-Histone H4 (1-25)-Gly-Ser-Gly-Ser-Lys(biotinyl) is a biologically active peptide.
Ac-PAL-AMC is a fluorogenic substrate specific for 20S proteasome LMP2/β1i activity[1].
MET kinase-IN-2 is a potent, selective, orally bioavailable MET kinase inhibitor with an IC50 of 7.4 nM. MET kinase-IN-2 has antitumor activity[1].
12-Hydroxyisobakuchiol, meroterpene derivative, is a natural product. 12-Hydroxyisobakuchiol can be isolated from the leaves of Psoralea glandulosa[1].
SRT 2183 is a selective Sirtuin-1 (SIRT1) activator with an EC1.5 value of 0.36 μM[1]. SRT 2183 induces growth arrest and apoptosis, concomitant with deacetylation of STAT3 and NF-κB, and reduction of c-Myc protein levels[2].
ARV-766 is an orally active and potent proteolysis targeting chimera (PROTAC) protein degrader. ARV-766 degrades wild-type androgen receptor (AR) but also relevant AR LBD mutants, including the most prevalent AR L702H, H875Y, and T878A mutations[1].
KU-60019 is an improved ATM kinase-specific inhibitor with IC50 of 6.3 nM.
4-Fluorobenzonitrile-d2 is the deuterium labeled 4-Fluorobenzonitrile[1].
Hematein is a oxidation product of hematoxylin acted as a dye[1]. Hematein is an allosteric casein kinase II inhibitor with an IC50 of 0.74 μM. Hematein inhibits Akt/PKB Ser129 phosphorylation, the Wnt/TCF pathway and increases apoptosis in lung cancer cells[2].
Naloxegol oxalate (NKTR-118 oxalate; AZ-13337019 oxalate) is an opioid-receptor antagonist[1].
KRAS inhibitor-6 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound A[1].
Melperone, a butyrophenone, is an antipsychotic drug used for sleep induction which is frequently prescribed in psychiatric setting[1]. Melperone has been used for a variety of indications, including the treatment of schizophrenia, but also for agitation in the elderly[2].
Pyridin-4-ol-d5 is the deuterium labeled Pyridin-4-ol[1].
LGD-4033 is a novel nonsteroidal, oral SARM that binds to androgen receptor with high affinity (Ki of 1 nM) and selectivity.IC50 value: 1 nM (Ki, for androgen receptor) Target: androgen receptorin vitro: LGD-4033, a novel nonsteroidal oral, selective androgen receptor modulator, binds androgen receptor with high affinity and selectivity.in vivo: LGD-4033 has demonstrated anabolic activity in the muscle, anti-resorptive and anabolic activity in bone, and robust selectivity for muscle versus prostate In animal models. LGD-4033 is well tolerated, has a long elimination half-life and dose-proportional accumulation upon multiple dosing. LGD-4033 is safe, has favorable pharmacokinetic profile, and increases lean body mass even during this short period without change in prostate-specific antigen.
Coniferyl alcohol is an intermediate in biosynthesis of eugenol and of stilbenoids and coumarin[1]. Coniferyl alcohol specifically inhibits fungal growth[1].
Propargyl-PEG6-SH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
MK2-IN-3 is a potent and selective inhibitor of MAPKAP-K2 (MK-2), with an IC50 of 8.5 nM. MK2-IN-3 shows selectivity for MK-2 over MK-3, MK-5, ERK2, MNK1, p38a (IC50s=0.21, 0.081, 3.44, 5.7, and >100 μM, respectively) and MSK1, MSK2, CDK2, JNK2, IKK2 (IC50s>200 μM). MK2-IN-3 can reduce TNFα production in both U937 cells and in vivo[1].
Mexiletine D6 hydrochloride (KOE-1173 D6 hydrochloride) is a deuterium labeled Mexiletine hydrochloride (KOE-1173 hydrochloride). Mexiletine hydrochloride, a Class IB antianhythmic, is a non-selective voltage-gated sodium channel blocker[1].
Zimberelimab is a fully human IgG4 anti-PD-1 monoclonal antibody with high affinity and selectivity. Zimberelimab shows antitumor activities and can be used for various cancers research including cervical cancer, non-small cell lung cancer and classical Hodgkin’s lymphoma[1].
N-Pyrazinylcarbonylphenylalanine-d8 is the deuterium labeled Deruxtecan. Deruxtecan is an ADC drug-linker conjugate composed of a derivative of DX-8951 (DXd) and amaleimide-GGFG peptide linker, used for synthesizing DS-8201 and U3-1402.
Gigantol is a bibenzyl compound derived from several medicinal orchids. Giganto shows promising therapeutic potential against cancer cells. Gigantol is a novel inhibitor of the Wnt/β-catenin pathway.
1-O-Acetyl-2-O-benzoyl-3-O-tert-butyldiphenylsilyl-L-threofuranose is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
TriDAP (L-Ala-γ-D-Glu-meso-diaminopimelic acid) is a biological active peptide. (specific Nod1 activator)
SB-332235 is a potent, orally active nonpeptide CXCR2 antagonist, with an IC50 of 7.7 nM. SB-332235 displays 285-fold selectivity for CXCR2 over CXCR1. SB-332235 inhibits acute and chronic models of arthritis in the rabbit. SB-332235 inhibits viability of AML cells[1][2].
Corydaline is an acetylcholinesterase inhibitor isolated from Corydalis yanhusuo.
Berteroin, a naturally occurring Sulforaphane analog, ia an antimetastatic agent. Berteroin has anti-inflammatory, antitumor and bactericidal effects[1][2].
CID 2011756 is an ATP competitive PKD inhibitor, with an IC50 of 3.2 µM for PKD1 in cell free assay, and also shows cellular pan-PKD inhibitory activity against PKD2 and PKD3 (IC50, 0.6 and 0.7 µM, respectively). CID 2011756 also has antitumor activity.
Boc-Leucinol is a leucine derivative[1].
Abz-Gly-p-nitro-Phe-Pro-OH is the fluorescent substrate angiotensin I converting enzyme (ACE-I) with 355 nm excitation and 405 nm emission wavelengths[1].