HRX215 is a first-in-class MKK4 inhibitor with IC50 of 0.02 μM and shows above 100-fold selectivity against JNK1, BRAF, and MKK7. HRX215 increases liver regeneration after hepatectomy in murine and porcine models.

DB-lipidoid 11-10-8 is a degradable branched (DB) lipidoid. 11-10-8 LNP is more potent than MC3 LNP at delivering mRNA. 11-10-8 LNP enables roughly five-fold higher TTR genome editing efficiency and therapeutic FGF21 protein expression compared to MC3 LNP.

KSQ-4279 is a USP1 and PARP inhibitor. KSQ-4279 showed anti-proliferative effects in a subset of cell lines, often characterized by the presence of homologous recombination deficiencies (HRD), including mutations in BRCA1/2. The combination of KSQ-4279 with olaparib was able to induce strong and durable regressions across a number of ovarian and TNBC PDX models.

PLX5622 is the HCl salt form of PLX-5622, which has better water solubility.PLX-5622 is a highly selective brain-penetrant CSF1R inhibitor (IC50=0.016 µM; Ki=5.9 nM) allowing for extended and specific microglial elimination, preceding and during pathology development.

6-Diazo-5-oxo-L-nor-Leucine (DON) is a glutamine analog that inhibits glutaminases (Ki = 6 µM) and other glutamine-utilizing enzymes, including cytidine triphosphate synthase (CTPS), which uses glutamine in the synthesis of CTP.1,2,3 DON is commonly used in cells or tissues but its use in whole animals is limited by its teratogenicity.

Lipid GVS-18-B6 is a silicon ether ionizable lipid for mRNA delivery. GVS-18-B6 showes particularly good liver specificity, with a liver-to-spleen EGFP signal ratio of 92:1. GVS-18-B6 also showes rapid tissue clearance within 6 hours of dosing.

RMC-7977 is a reversible, tri-complex RAS inhibitor with broad spectrum activity for both mutant and wild-type (WT) KRAS, NRAS, and HRAS variants.RMC-7977 can lead to tumor regressions and was well tolerated in diverse RAS-addicted preclinical cancer models. RMC-7977 also can inhibit the growth of KRASG12C cancer models.

Lipid CAD9 (3-A2-7b is a cationic degradable (CAD) lipid. 3-A2-7b formulated LNP, LNP-CAD9, can deliver FLuc mRNA to the lungs in vivo. LNP-CAD9 co-delivering Cas9 mRNA/VEGFR2 single guide RNA (sgRNA) effectively induces VEGFR2 knock out in lung endothelial cells of female mice.

dCeMM1 is a RBM39 glue degrader. dCeMM1 shows functions by re-directing the activity of the CRL4DCAF15 ligase. dCeMM1 decreases the expression of RBM39 levels in WT KBM7 cells[1].

AAcid-PEG5-C2-Boc is a PEG derivative containing a t-butyl protected carboxyl group with a terminal carboxylic acid. The terminal carboxylic acid can be reacted with primary amine groups in the presence of activators (e.g. EDC, or DCC) to form a stable amide bond. The hydrophilic PEG spacer increases solubility in aqueous media. The t-butyl protected carboxyl group can be deprotected under acidic conditions.

Tri-GalNAc(OAc)3 is a triantenerrary N-acetylgalactosamine (tri-GalNAc) with an amino group, which is useful precursor for synthesis of GalNAc-LYTAC that engage the asialoglycoprotein receptor for targeted protein degradation. Tri-GalNAc(OAc)3 was first reported in Nat Chem Biol. 2021 Sep;17(9):937-946 (compound ). This product has no formal name at the moment.

DSPE-PEG2K-triGalNAc is a polar lipid composed of DSPE and tri-N-acetylgalactosamine that can be used to construct liposomes target to asialoglycoprotein receptor (ASGPR).

RMC-9805 is a first-in-class, mutant-selective, covalent and orally bioavailable KRAS-G12D(ON) inhibitor. RMC-9805 exhibits direct anti-tumor effects and indirectly transformed the TME through inhibition of cancer cell-intrinsic KRAS-G12D oncogenic signaling.

ABBV-303 is a novel c-Met targeted multispecific NK cell engager. ABBV-303 binding to NKG2D and CD16a results in redirection of both innate (NK cells) and adaptive (CD8+ T cells) immune cells to lyse c-Met expressing tumor cells.

ORIC-944 is a potent, selective, allosteric inhibitor of PRC2 that binds the EED (Embryonic Ectoderm Development) subunit within the complex. ORIC-944 demonstrats single agent tumor growth inhibition in a spectrum of in vivo prostate cancer models, including AR-positive, AR-mutant, ARv7, ARPI-responsive and ARPI-resistant models.

BBO-8520 is a first-in-class, direct covalent inhibitor of both KRAS-G12C (ON) and (OFF) states. BBO-8520 displays highly significant binding to KRAS-G12C in a global cysteine proteome analysis and is 100x more selective for KRAS-G12C than for WT-KRAS and other mutant isoforms, with no measurable activity against N- or H-RAS.

NST-628 is a potent pan-RAF-MEK molecular glue that prevents phosphorylation and activation of MEK by RAF. NST-628 demonstrates broad efficacy in cellular and patient-derived, in vivo tumor models harboring KRAS, NRAS, BRAF class II/III, and NF1 mutations.

VVD-214 (RO7589831) is a synthetic lethal allosteric inhibitor of WRN helicase. VD-214 covalently engages cysteine 727 of WRN in a nucleotide cooperative manner and inhibits ATP hydrolysis and helicase activity, resulting in widespread double-stranded DNA breaks, nuclear swelling, and cell death in MSI-high, but not microsatellite stable cells.

RMC-6236 is a first-in-class, potent, oral tri-complex RASMULTI(ON) small molecule inhibitor designed to treat cancers driven by a variety of RAS mutations.

U-101 is an ionizable lipid for mRNA delivery. U-101-LNP/IL-2F mRNA formulation demonstrats effective antitumor activity and safety.LNPs containing lipid U-101 and encapsulating mRNA encoding a fusion protein composed of IL-2, a linker, and CD25 inhibit tumor growth in an MC-38 mouse xenograft model.