Z86 (Z6466689386) is a novel small molecule enhancer of the CUL3/LZTR1 E3 ligase KRAS complex.

A novel small molecule that inhibits GATA4/NKX2-5 transcriptional synergy with IC50 of 3 uM, with no activity on the protein kinases involved in the regulation of GATA4 phosphorylation.

Etalocib (LY293111), an orally active leukotriene B4 receptor antagonist, inhibits the binding of [3H]LTB4, with a Ki of 25 nM. Etalocib (LY293111) prevents LTB4-induced calcium mobilization with an lC50 of 20 nM. Etalocib (LY293111) induces apoptosis.

PD-166793 is a cell-permeable biphenylsulfonylvaline compound that acts as a potent inhibitor against MMP-2, -3, and -13 (IC50 = 47, 12, and 8 nM, respectively) and a weaker inhibitor against AMP deaminase (20% inhibition at 0.1 μM), MMP-1, -7, -9, and -14 (IC50 = 6.1, 7.2, 7.9, and 0.24 μM, respectively). Shown to offer therapeutic benefits in vivo in various animal models of heart failure and diabetes.

TC KHNS 11 is a potent and selective PI 3-kinase δ inhibitor that is orally bioavailable.

Novel Integrin very late antigen-4 (VLA-4; α4β1) antagonist, blocking the activation of inflammatory cells.

FK-888 is a selective, high affinity tachykinin NK1 receptor antagonist (Ki = 0.69 nM) that displays 320-fold selectivity for human over rat NK1 receptors. FK-888 inhibits substance P-induced contraction of isolated guinea pig trachea (IC50 = 32 nM) and inhibits substance P-induced airway constriction in vivo.

ML354 (VU0099704) is a novel potent and selective PAR4 antagonist with IC50 of 140 nM, displays 71-fold selectivity versus PAR-1.

Carbodenafil is a Sildenafil (UK-92480) related compound found in health foods. Sildenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM.

CDK9 inhibitor HH1 is a novel potent, highly selective CDK9 inhibitor..

CHDI-390576 (CHDI390576) is a potent, cell permeable and CNS penetrant class IIa HDAC inhibitor with IC50 of 54/60/31/50 nM for HDAC4/5/7/9, respectively.

Floctafenine, also known as R-4318 and Idarac, is a cyclooxygenase inhibitor that inhibits prostaglandin synthesis.

Novel TRPM8 channel blocker

CCT129202 is a potent, selective, ATP-competitive pan-Aurora kinase inhibitor with IC50 of 42, 198 and 227 nM for Aurora A, Aurora B and Aurora C, respectively.

YTHDC1 inhibitor 40 is a potent, selective m6A reader YTHDC1 inhibitor with ITC Kd of 49 nM, HTRF IC50 of 0.35 uM. Compound 40 shows antiproliferative activity against the acute myeloid leukemia (AML) cell lines THP-1, MOLM-13, and NOMO-1.YTHDC1 inhibitor 40 exhibits antiproliferative activity against THP-1 (GI50 = 3.2 μM), MOLM-13 (5.6 μM) and NOMO-1 (8.2 μM), respectively. YTHDC1 inhibitor 40 displays IC50 values of 89, 60, and 83 μM against YTHDF1, YTHDF2, and YTHDF3, respectively, indicating a 200-fold selectivity.YTHDC1 inhibitor 40 does not display significant inhibition of a panel of 58 protein kinases.YTHDC1 inhibitor 40 (2.5-10 uM) induces apoptosis in THP-1 cell line after 24 h treatment.YTHDC1 inhibitor 40 is a tool compound for studying the role of YTHDC1 in AML.

NS-018 maleate (NS018, Ilginatinib) is a potent and highly selective JAK2 inhibitor (IC50=0.72 nM).

AZ12216052 is a mGluR II and III activator.

TFC-007, a selective hematopoietic prostaglandin D synthase (H-PGDS) inhibitor, show high inhibitory activity against H-PGDS enzyme (IC50 value of 83 nM). TFC-007 can be used for composing H-PGDS degradation inducer PROTAC(H-PGDS)-1 (TFC-007 binds to H-PGDS, and Pomalidomide binds to cereblon).

ML 351 is a selective 12/15 LOX inhibitor that is active in vivo.

VU0469650 is a potent, selective and CNS-penetrated negative allosteric modulator of mGlu1 receptor, with an IC50 of 99 nM.

MJ-15 is a potent and selective antagonist of cannabinoid CB1 receptor.

ML241 Hcl is a potent, selective and reversible AAA ATPase p97 inhibitor (IC50=100 nM).

Arcyriaflavin A is an inhibitor of cdk4/cyclin D1 and CaM kinase II.

NSC 625987 is a potent, selective CDK4 inhibitor with IC50 of 0.2 uM, displays >500-fold selectivity over CDK2 (IC50 >100 uM for cdc2/cyclin A, cdk2/cyclin A and cdk2/cyclin E). .

VU0155069 is a potent, selective phospholipase D1 (PLD1) inhibitor with IC50 of 46 nM, 20-fold selectivity over PLD2 (IC50=933 nM).

TL02-59 is a potent, selective, orally available inhibitor of Src-family kinase Fgr IC50 of 0.03 nM, also inhibits Lyn and Hck with IC50 of 0.1 and 160 nM, respectively.

CXCR7 antagonist-1 is an inhibitor of the binding of the SDF-1 chemokine (also known as the CXCL12 chemokine) or I-TAC (also known as CXCL11) to the chemokine receptor CXCR. CXCR7 antagonist-1 prevents tumor cell proliferation, tumor formation, inflammatory diseases, and many other diseases (extracted from patent WO2014085490A1, compound 1.128).

STING agonist-7 is a non-nucleotide STING agonist. STING agonist-7 binds selectively to mouse STING but not human STING. STING agonist-7 penetrates cell membrane poorly.

HIF-2α-IN-4 is a potent inhibitor of hypoxia inducible factor-2α (HIF-2α) translation, with an IC50 of 5 μM. HIF-2α-IN-4 decreases both constitutive and hypoxia-induced HIF-2α protein expression. HIF-2α-IN-4 links its 5'UTR iron-responsive element to oxygen sensing.

Chlorantraniliprole is an insecticide that potently and selectively activates insect ryanodine receptor, with EC50s of 40 nM and 50 nM for Drosophila melanogaster and H. virescens ryanodine receptor, and ∼300-fold more potent than that in the mouse myobla