MI-1 inhibits Menin-MLL interaction with an IC50 of 1.9 μM[1].
Mitoxantrone dihydrochloride is a topoisomerase II inhibitor; also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM.
LSD1-IN-6 (Compound 4m) is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 123 nM. LSD1-IN-6 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1[1].
LSD1-IN-27 (Compound 5ac) is a LSD1 inhibitor (IC50: 13 nM). LSD1-IN-27 inhibits the stemness and migration of gastric cancer cells. LSD1-IN-27 also reduces the expression of PD-L1 in BGC-823 and MFC cells. LSD1-IN-27 can enhance T cell immune response in gastric cancer[1].
SIRT5 Inhibitor 6 is a potent, substrate-competitive and selective SIRT5 inhibitor with an IC50 of 3.0 μM. SIRT5 Inhibitor6 has a therapeutic potential against septic AKI in vivo[1].
EML425 is a potent and selective CREB binding protein (CBP)/p300 inhibitor with IC50s of 2.9 and 1.1 μM, respectively.
Veliparib is a potent PARP inhibitor, inhibiting PARP1 and PARP2 with Kis of 5.2 and 2.9 nM, respectively.
KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC50 of 15.1 nM.
Fisetin is a natural flavonol found in many fruits and vegetables with various benefits, such as antioxidant, anticancer, neuroprotection effects.
G007-LK is a potent and selective inhibitor of TNKS1 and TNKS2, with IC50s of 46 nM and 25 nM, respectively.
AluI Methyltransferase (AluI) is a methyltransferase used as the interference enzymes to investigate the selectivity[1].
Gardenia yellow is an active member of crocin, increases mRNA expression of SIRT3, and acts as an orally active antidepressant agent[1].
Laccaic acid A is a orally active and DNA-competitive inhibitor of DNA methyltransferase 1 (Dnmt1) (Ki=310 nM; IC50=650 nM). Laccaic acid A has stronger Dnmt1 inhibitory effect than SG-1027 (HY-13962). Laccaic acid A combined with Phenethyl isothiocyanate has a strong synergistic effect on colorectal cancer[1][2].
Upadacitinib (ABT-494) tartrate tetrahydrate is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib tartrate tetrahydrate displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib tartrate tetrahydrate can be used for several autoimmune disorders research[1][2].
Valproic acid (VPA) sodium (2:1) is an orally active HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium (2:1) activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium (2:1) is used in the treatment of epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches[1][2][3][4][5][6][7].
Selisistat (EX-527) is a potent and selective SIRT1 inhibitor with IC50 of 98 nM.
PRMT5-IN-27 (compound 481) is an inhibitor of PRMT5. PRMT5-IN-27 inhibits HCT116 cell proliferation with an IC 50 of 0.13 μM[1].
Bisindolylmaleimide I (GF109203X) is a highly selective, cell-permeable, and reversible protein kinase C (PKC) inhibitor with a Ki of 14 nM.
JAK-2/3-IN-2 (Compound 3h) is a JAK2 and JAK3 inhibitor with IC50s of 23.85 nM and 18.9 nM, respectively[1].
BET BD2-IN-1 (compound 45) is a potent and selective inhibitor of BET BD2 (IC50=1.6 nM). BET BD2-IN-1 inhibits the differentiation of Th17 cells by decreasing the activation of STAT3 and NF-κB. BET BD2-IN-1 is used in psoriasis and inflammatory bowel disease (IBD) research[1].
Rencofilstat (CRV431) is a non-immunosuppressive analogue of cyclosporine A and pan-cyclophilin inhibitor, potently inhibits cyclophilin isoforms A, B, D, and G with IC50 of 1-7 nM.Rencofilstat (CRV431) is more than 13 times more potent than the parent compound, cyclosporine A (CsA).Rencofilstat (CRV431) inhibits liver HBV DNA and HBsAg, reduces liver HBV DNA levels and moderately decreased serum HBsAg levels in HBV transgenic mouse model.Rencofilstat (CRV431) shows potential as a drug candidate for chronic liver diseases.
DC-BPi-03 is a potent BPTF-BRD inhibitor with an IC50 of 698.3 nM and a Kd of 2.81 μM[1].
Itacnosertib (TP-0184) is both inhibitor to JAK2, ACVR1 (ALK2) and ALK5 as described in WO2014151871[1].
LIN28 inhibitor LI71 is a potent and cell-permeable LIN28 inhibitor, which abolishes LIN28-mediated oligouridylation with an IC50 of 7 uM. LIN28 inhibitor LI71 directly binds the cold shock domain (CSD) to suppress LIN28’s activity against let-7 in leukemia cells and embryonic stem cells[1].
O-304 is a small molecule AMPK activator.
Galegine hydrochloride, a guanidine derivative, contributes to weight loss in mice. Guanidine hydrochloride is the compound derived from G. officinalis, which gave rise to the biguanides, metformin and phenformin. Galegine hydrochloride activates AMPK in 3T3-L1 adipocytes and L6 myotubes, as well as in the H4IIE rat hepatoma and HEK293 human kidney cell lines. Galegine hydrochloride has antibacterial activity, with minimum inhibitory concentration of 4 mg/L against Staphylococcus aureus strains[1][2].
SGC-CBP30 is a potent CREBBP/EP300 bromodomain inhibitor with IC50 of 21-69 and 38 nM for CREBBP and EP300 bromodomains, respectively.IC50 Value: 21-69 nM(for CREBBP); 38 nM(for EP300)Target: Othersin vivo: SGC-CBP30 is a highly potent and selective p300/CBP bromodomain inhibitor (IC50 ~0.021-0.069 uM for CBP and ~0.038 uM for p300). It has 40-fold selectivity for CBP over BRD4. It accelerated FRAP recovery at 1 uM. in vivo: N/A
Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative isolated from plants of the Genus Daphne, is a protein kinase inhibitor, with IC50s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively[1][2]. Daphnetin (7,8-dihydroxycoumarin) is a secondary metabolite of plants used in folk medicine to counter inflammatory and allergic diseases, also has been clinically used in the treatment of coagulation disorders, rheumatoid arthritis with anti-malarian and anti-pyretic properties[3].
Tyk2-IN-4 is a selective, potent, allosteric inhibitor of tyrosine kinase 2 (Tyk2).
Rovadicitinib is a Janus kinase (JAK) inhibitor with an IC50 value <20 nM. Rovadicitinib also exhibits anti-inflammatory activity[1][2].