Rucaparib (AG014699) hydrochloride is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib hydrochloride is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib hydrochloride has the potential for castration-resistant prostate cancer (CRPC) research[1][2][3][4].
Aurora Kinases-IN-3 (Compound 15a) is an orally active AURKB inhibitor that elicits an AURKB-suppressive activity by disrupting the mitotic localization of AURKB, rather than inhibiting its phosphorylation of H3 at Ser10[1].
J22352 is a PROTAC (proteolysis-targeting chimeras)-like and highly selective HDAC6 inhibitor with an IC50 value of 4.7 nM. J22352 promotes HDAC6 degradation and induces anticancer effects by inhibiting autophagy and eliciting the antitumor immune response in glioblastoma cancers, and leading to the restoration of host antitumor activity by reducing the immunosuppressive activity of PD-L1[1].
Enzastaurin is a potent and selective PKCβ inhibitor with an IC50 of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε.
Spisulosine (ES-285) is an antiproliferative (antitumoral) compound of marine origin. Spisulosine inhibits the growth of the prostate PC-3 and LNCaP cells through intracellular ceramide accumulation and PKCζ activation[1].
JMJD6-IN-1 (Compound 1-3) is a JMJD6 inhibitor, with an inhibition rate of 82% at 10 μM. JMJD6-IN-1 inhibits MCF-7 and HCC4006 cell proliferation with IC50s of 19.2 μM and 25.2 μM. JMJD6-IN-1 can be used for research of cancers[1].
Amredobresib is a potent inhibitor of BET. Amredobresib inhibits the binding of bromodomains to acetylated lysines on histone H3 and H4 and thus acts as important regulators of gene transcription. Amredobresib is useful for the research of acute myeloid leukemia (AML) and cancer (extracted from patent WO2019145410A1 and WO2021175824A1)[1].
Romidepsin is a potent HDAC1 and HDAC2 inhibitor with IC50s of 36 and 47 nM, respectively.
PRMT5-IN-32 is an inhibitor of PRMT5. PRMT5-IN-32 inhibits HCT116 cell proliferation with an IC 50 of 0.13 μM[1].
Lademirsen (SAR339375; RG-012) is a highly specific antisense oligonucleotide (ASO) targeting miR-21. Lademirsen has the potential for Alport nephropathy research[1][2].
PF-06726304 is a potent and selective EZH2 inhibitor with a Ki of 0.7 nM.
PROTAC BRD4 Degrader-21 (Comp 74) is a PROTAC degrader of BRD4. PROTAC BRD4 Degrader-21 displays significant tumor growth inhibition in tumor -bearing xenograft models in mice and can be used for anticancer research[1].
BRM/BRG1 ATP Inhibitor-3 is a BRG1/BRM inhibitor. BRM/BRG1 ATP Inhibitor-3 inhibits BRM and BRG1 with IC50 values of 10.4 nM and 19.3 nM, respectively. BRM/BRG1 ATP Inhibitor-3 can be used for the research of cancers and BAF complex-related disorders[1].
EX229, a Benzimidazole derivative, is a potent and allosteric activator of AMP-activated protein kinase (AMPK), with Kds of 0.06 μM, 0.06 μM and 0.51 μM for α1β1γ1, α2β1γ1 and α1β2γ1 in biolayer interferometry, respectively.
EcoRI Methyltransferase is a bacterial sequence-specific S-adenosyl-L-methionine-dependent DNA methyltransferase. EcoRI Methyltransferase relies on a complex conformational mechanism to achieve its remarkable specificity, including DNA bending, base flipping and intercalation into the DNA[1].
SMYD2-IN-1 is a SMYD2 inhibitor extracted from patent WO2016166186A1, compound example 1.1, has an IC50 of 4.45 nM[1].
ZL0580, a structurally close analog of ZL0590, induces epigenetic suppression of HIV via selectively binding to BD1 domain of BRD4. ZL0580 induces HIV suppression by inhibiting Tat transactivation and transcription elongation as well as by inducing repressive chromatin structure at the HIV promoter[1][2][3].
CPI-203 is a novel potent, selective and cell permeable inhibitor of BET bromodomain, with an IC50 value of appr 37 nM (BRD4 α-screen assay).
Dot1L-IN-2 is a potent, selective and orally bioavailable inhibitor of Dot1L (a histone methyltransferase), with an IC50 and Ki of 0.4 nM and 0.08 nM, respectively.
Protein Kinase C (beta) Peptide is a peptide fragment of Protein Kinase Cβ. Protein Kinase Cβ is related with hyperglycemia decreases endothelium-derived nitric oxide. Inhibition of Protein kinase Cβ prevents the reduction in endothelium-dependent vasodilation induced by acute hyperglycemia[1].
Tz-Thalidomide is a tetrazine tagged Thalidomide (HY-14658) (Ligands for E3 Ligase). Tz-Thalidomide has binding affinity for BRD4, with IC50s of 46.25 μM (BRD4-1) and 62.55 μM (BRD4-2)[1].
AMDE-1 is a potent autophagy inducer. AMDE-1 induces autophagy by the AMPK-mTORC1-ULK1 pathway and at the same time inhibited autophagy-mediated degradation by causing lysosome dysfunction. AMDE-1 can be used in research of cancer[1].
Remlarsen (MRG-201), a miR-29b mimic, acts a miR-29b agonist. Remlarsen has the potential for preventiong formation of a fibrotic scar or cutaneous fibrosis[1].
Ganoderic acid D, a highly oxygenated tetracyclic triterpenoid, is the major active component of Ganoderma lucidum. Ganoderic acid D upregulates the protein expression of SIRT3 and induces the deacetylated cyclophilin D (CypD) by SIRT3. Ganoderic acid D inhibits the energy reprogramming of colon cancer cells including glucose uptake, lactate production, pyruvate and acetyl-coenzyme production in colon cancer cells[1]. Ganoderic acid D can inhibit the growth of numerous cancer cell lines and it inhibits HeLa human cervical carcinoma cells with an IC50 of 17.3 mM[2].
TTK21 (CBP-p300 activator TTK21) is a small molecule activator of CBP/p300 histone acetyltransferase activity with a maximal effect at a concentration of 275 uM; induces acetylation of histones H3 and H4 in vitro but not H2B and H2A; promotes neurogenesis and extends memory duration in adult mice, promotes regeneration and sprouting of sensory and motor axons, as well as recovery of sensory and motor functions in both the mouse and rat model of spinal cord injury.
Bizine, a Phenelzine analogue, is a potent and selective LSD1 inhibitor, with a b>Ki of 59 nM. Bizine can modulate bulk histone methylation in cancer cells. Bizine shows neuroprotective effects[1].
Hypocrellin A, a naturally occurring PKC inhibitor, has many biological and pharmacological properties, such as antitumour, antiviral, antibacterial, and antileishmanial activities. Hypocrellin A is a promising photosensitizer for anticancer photodynamic therapy (PDT)[1][2][3][4].
Y06036 is a potent and selective BET inhibitor, which binds to the BRD4(1) bromodomain with Kd value of 82 nM[1]. Antitumor activity[1].
JQ1-TCO (JQ1-trans-cyclooctene) is a derivative of JQ1 (HY-13030), an inhibitor of BET. JQ1-TCO is suitable for click chemistry and can be used as molecular probes in vitro and in vivo[1][2].
RO8191 (RO4948191), an imidazonaphthyridine compound, is an orally active and potent interferon (IFN) receptor agonist. RO8191 activates IFN-stimulated genes (ISGs) expression and JAK/STAT phosphorylation. RO8191 shows antiviral activity against both HCV and EMCV with an IC50 of 200 nM for HCV replicon[1].