subfamily

PF-05105679 is a selective TRPM8 antagonist (IC50 = 103 nM). PF-05105679 can be used in research on cold-related pain.

Daminozide (Succinic Acid) is a plant growth regulator, selectively inhibits the KDM2 7 JmjC subfamily.

1,1'-Methylenedi-2-naphthol target CYP2C19 - cytochrome P450 family 2 subfamily C member 19 (human).

A-803467 is a selective NaV1.8 channel blocker.

RN-1747 is a selective transient receptor potential cation channel subfamily V member 4 agonist (EC50: hTRPV4 of 0.77 μM, mTRPV4 of 4.0 μM, and rTRPV4 of 4.1 μM) and also acts as an antagonist for TRPM8 (IC50: 4 μM).

BRM/BRG1 ATP Inhibitor-1 is an allosteric dual Brahma homolog (BRM)/SWI/SNF related matrix-associated actin-dependent regulator of chromatin subfamily A member 2 (SMARCA2) and BRG1/SMARCA4 ATPase activity inhibitor (IC50s<0.005 μM).

Rhosin hydrochloride is a specific inhibitor of the RhoA subfamily Rho GTPases and inhibits the RhoA-GEF interaction. Rhosin hydrochloride can significantly induce cell apoptosis without affecting cell cycle progression. [1]

Rhosin is an effective and specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction (Kd: ~ 0.4 uM). Rhosin does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin causes cell apoptosis.

Compound BPP (HDGFRP2 PSIP1-IN-1) is a dual inhibitor targeting the PWWP domains of Hepatoma-derived Growth Factor Related Protein 2 (HDGFRP2) and its homologue PSIP1. This compound effectively hinders the occurrence and progression of Diffuse Intrinsic Pontine Glioma (DIPG). It demonstrates binding affinity with a Kd value of 7 μM for HDGFRP2, indicative of its efficient ligand efficacy at 0.47. Additionally, Compound BPP exhibits a Kd value of 27 μM when binding to the PSIP1 PWWP domain, and a Kd value of 14 μM against HDGFRP3, confirming its potency as an inhibitor within the HDGFRP2 PWWP subfamily.

PKCTheta-IN-2 (compound 14) is a potent and selective inhibitor of PKCθ, with an IC50 value of 0.25 nM. It demonstrates good selectivity across a broad range of kinases, including the PKC subfamily (30 kinases). Additionally, PKCTheta-IN-2 effectively inhibits the production of IL-2 in mice, where it exhibits an IC50 of 682 nM.

Apiole (NSC 9070), a phenylpropane volatile compound isolated from parsley, is a calcium channel inhibitor, a mixed-type inhibitor of the CYP1A subfamily, with antitumor activity, induces apoptosis, and inhibits human colon cancer cells by inducing G0 G1 cell cycle arrest.

MBL-IN-5 is an inhibitor of metallo-β-lactamase (MBL). It effectively suppresses three clinically significant B1 subfamily MBLs: NDM-1, VIM-1, and IMP-1 with IC50 values of 0.05 nM, 14 nM, and 21 nM respectively. MBL-IN-5 notably enhances the efficacy of carbapenem antibiotics against MBL-producing clinical strains and, when combined with IPM antibiotics, significantly reduces bacterial load in a thigh infection model.

Selective histone demethylase KDM2/7 subfamily inhibitor

Mesendogen is an inhibitor of TRPM6. Mesendogen alters magnesium homeostasis, promotes mesoderm and definitive endoderm differentiation.

The phospholipases are an extensive family of lipid hydrolases that function in cell signaling, digestion, membrane remodeling, and as venom components. The calcium-independent phospholipases (iPLA2) are a PLA2 subfamily closely associated with the release of arachidonic acid in response to physiologic stimuli. (R)-Bromoenol lactone ((R)-BEL) is an irreversible, chiral, mechanism-based inhibitor of calcium-independent phospholipase γ (iPLA2γ). Unlike (S)-BEL, (R)-BEL does not inhibit iPLA2β except at high doses of 20-30 μM. (R)-BEL inhibits human recombinant iPLA2γ with an IC50 of approximately 0.6 μM.

PDDHV is a resiniferatoxin-type phorboid vanilloid with capsaicin-like selectivity for the cloned rat transient receptor potential cation channel subfamily V member 1 (TRPV1), formerly known as vanilloid receptor 1. It induces Ca2+-uptake by rat dorsal root ganglion neurons with an EC50 value of 70 nM.

2-Methylhexacosane is a saturated hydrocarbon and an insect pheromone. It has been found in the cuticle of M. dasystomus females, but not males, contributing to the mating behavior of males, as well as in D. melanogaster females where it modulates male aggression. 2-Methylhexacosane has also been found in yellow jacket (V. vulgaris) trail extracts.

NR2F6 modulator-1 is a potent modulator of nuclear receptor subfamily 2, group F, member 6 (NR2F6), used to study immune regulation and modulation of tumour stem cell activity.

CCG-273220 is a covalent inhibitor of G protein-coupled receptor (GPCR) kinase 5 (GRK5) (IC50: 220 nM).CCG-273220 covalently binds the GRK5 subfamily-specific residue Cys474 and is more selective for GRK5 than GRK2.

NAZ2329 is the first cell-permeable inhibitor of the R5 subfamily of receptor-type protein tyrosine phosphatases (RPTPs), which is a variant and preferentially inhibits PTPRZ (IC50=7.5 μM for hPTPRZ1) and PTPRG (IC50=4.8 μM for hPTPRG) compared to other PTPs. NAZ2329 inhibited the tumor growth of glioblastoma cells and exhibited stem cell-like properties compared to the whole (D1 + D2) fragment of PTPRZ.

CCG258747 is a novel, selective inhibitor of the GRK2 subfamily.

AZ12099548 is a transient receptor potential cation channel subfamily V member 1 (TRPV1) antagonist.

VRT-043198, the drug metabolite of VX-765 (Belnacasan), is a potent, selective, and blood-brain barrier permeable inhibitor of the interleukin-converting enzyme caspase-1 subfamily caspases, displaying Ki values of 0.8 nM for ICE caspase-1 and 0.6 nM for caspase-4, respectively.

ArgTX-48 is a highly potent and subfamily selective antagonist of the NMDARs and AMPARs.