SI-109 (SI 109) is a selective, high-affinity and cell-permeable STAT3 SH2 domain inhibitor with Ki of 9 nM, component of STAT3 degrader SD-36 (PROTAC).

SHP2 PROTAC R1-5C is a potent and highly selective SHP2 PROTAC created by conjugating RMC-4550 with pomalidomide using a PEG linker, with a low nanomolar DC50; SHP2 PROTAC R1-5C is highly selective for SHP2, induces degradation of SHP2 in leukemic cells at submicromolar concentrations. SHP2 PROTAC R1-5C inhibits MAPK signaling, and suppresses cancer cell growth. SHP2 PROTACs serve as an alternative strategy for targeting ERK-dependent cancers and are useful tools alongside allosteric inhibitors for dissecting the mechanisms by which SHP2 exerts its oncogenic activity.

SH045 (SH-045, Larixyl-6-N-methylcarbamate) is a potent, selective TRPC6 antagonist (blocker) with IC50 of 63 nM.SH045 displays 13-fold subtype selectivity over TRPC3 in stably expressing HEK293 cells.Treatment of isolated perfused lung preparations with SH045 led to a decrease in lung ischemia-reperfusion edema (LIRE), a life-threatening condition associated with TRPC6 that may occur after organ transplantation.

SGC-STK17B-1 is a potent, selective, ATP-competitive inhibitor of death-associated protein kinase family member STK17B (DRAK2) with IC50 of 34 nM, >100-fold selectivity over STK17A; SGC-STK17B-1 is also >100-fold selective over all of the other kinases tested, with only STK17A, CAMKK1, and AURKB (IC50s=5-9 uM) in panel of 403 wild type human kinase assays. SGC-STK17B-1 demonstrated the highest cell potency in the NanoBRET target engagement assay (IC50=190 nM). SGC-STK17B-1 is the first truly potent and selective chemical probe of STK17B.

SGC8158 (SGC-8158) is a potent, selective, and SAM-competitive inhibitor of PRMT7 with IC50 of <2.5 nM, the active component of it's cell permeable prodrug SGC3027.

SGC6870N is the negative control of SGC-6870 (R-isomer), which is a potent, selective, cell-active PRMT6 inhibitor.

SGC6870 (SGC-6870 (R-isomer)) is a potent, selective, cell-active PRMT6 inhibitor with IC50 of 77 nM.SGC6870 displays outstanding selectivity for PRMT6 over a broad panel of other methyltransferases and nonepigenetic targets.SGC6870 binds to a unique, induced allosteric pocket of PRMT6.SGC6870 engages PRMT6 and potently inhibits its methyltransferase activity in cells.SGC6870 is a well-characterized PRMT6 chemical probe and a valuable tool for further investigating PRMT6 functions in health and disease.

SGC3027N (SGC-3027N) is a negative control compound for SGC3027, shows markedly less potent (14 uM) against PRMT7 and other protein methyltransferases.

SF-3-030 is a novel ATP-dependent/catalytic site inhibitor of ERK1/2, inhibits A375 cell viability with IC50 of 4.9 uM.SF-3-030 showed selective inhibition of cancer cell lines with activating mutations in the ERK1/2 pathway.SF-3-030 inhibited viability of four melanoma cell lines containing either BRAF or NRas mutations with IC50 of 5-10 uM.SF-3-030 selectively regulates ERK-dependent immediate early gene expression, causes differential changes in AP-1 protein levels characterized by inhibition of Fra-1, FosB, and the alternative splice variant FosB2 but no effect on c-Fos levels, and induces ROS mediates inhibition of A375 cell proliferation.

SEW84 (SEW04784) is a first-in-class, specific inhibitor of the Aha1-stimulated Hsp90 (ASH) ATPase activity (IC50=0.3 uM) without inhibiting basal Hsp90 ATPase; SEW84 binds to the C-terminal domain of Aha1 (Kd=1.7 uM) to weaken its asymmetric binding to Hsp90. SEW84 inhibited the GR- and AR-dependent luciferase expression with IC50 of 1.3 uM and 0.7 uM respectively. SEW84 blocks Aha1-dependent Hsp90 chaperoning activities, including the in vitro and in vivo refolding of firefly luciferase, and the transcriptional activity of the androgen receptor in cell-based models of prostate cancer. SEW84 promotes the clearance of phosphorylated tau in cellular and tissue models of neurodegenerative tauopathy.

sCSF1Rinh is a CNS-penetrant, potent and selective small-molecule CSF1R inhibitor, binds to CSF1R in a DFG-out conformation.is highly selective for CSF1R as compared to other kinases with a selectivity score of S(35)=0.005, sCSF1Rinh exhibited excellent pharmacokinetic properties including good oral bioavailability and CNS penetrance.sCSF1Rinh (500 nM) blocks these phosphorylation events in CSF1 (100 ng/mL) stimulation of BV2 microglia.sCSF1Rinh inhibited murine bone marrow-derived macrophage proliferation with IC50 of 22 nM, sCSF1Rinh significantly depletes microglia in a concentration-dependent manner in murine mixed glial cultures (IC50=188 nM).sCSF1Rinh reduced the number of microglia and infiltrating macrophages in an acute LPS model, with diminished microglial/macrophage proliferation and attenuated inflammatory response.sCSF1Rinh also suppressed a deleterious microglial response in the C57BL/6 EAE (experimental autoimmune encephalomy) model as well as the MOG peptide-induced non-obese diabetic EAE model of progressive MS (NOD-EAE) and improved neurological impairments in both models.

SCR7 is a specific inhibitor of nonhomologous end-joining (NHEJ), blocks Ligase IV-mediated joining by interfering with its DNA binding but not that of T4 DNA Ligase or Ligase I; inhibits NHEJ in a Ligase IV-dependent manner within cells, causes accumulation of double-strand breaks (DSBs), and activates the intrinsic apoptotic pathway; decreases cell proliferation of MCF7, A549, and HeLa with IC50 of 40, 34, and 44 uM, respectively; increases the efficacy of DSB-inducing therapeutic modalities in mouse xenografts; increases the efficiency of precise genome editing with CRISPR-Cas9 in mammalian cell lines and in mice.

SCP1 inhibitor T-65 (T-65) is a specific, small molecule covalent inhibitor of small CTD phosphatase 1 (SCP1), reduces transcription factor REST protein level HEK293 cells with EC50 of 1.5 uM.T-65 showed no detectable inhibition against a panel of eight mammalian cysteine-based phosphatases, including SHP2, TCPTP, CD45, DUSP3 and and lymphoid protein tyrosine phosphatase (LYP) at 25 uM.T-65 promotes REST degradation, increases expression of REST-suppressed genes DYRK1a, ELAVL1, USP37, CELSR3, and SCN2 in HEK293 cells.

SCP1 inhibitor T-62 (T-62) is a specific, small molecule covalent inhibitor of small CTD phosphatase 1 (SCP1), reduces transcription factor REST protein level HEK293 cells.

SC-78080 (SD-2590) is a potent, selective inhibitor of MMP2/9/13 with IC50 of <0.1/0.18/<0.1 nM, respectively.SC-78080 shows weaken inhibitory effect on MMP3/8, and no inhibition on MMP1/7.

SBI-4668 (SBI 4668) is a novel furanylbenzamide molecule as inhibitor of both WT and oncogenic SHP2 with IC50 of 0.73/1.8 uM for Wt SHP2/SHP2-E76K, 13-fold selective over PTP1B and 73-fold selective over STEP; SBI-4668 exhibited cell viability inhibitory effect on cell growth in both Kasumi-1 cells (IC50=8.5 uM) and KYSE-520 cells (IC50=5.4 uM), SBI-4668 on cell viability was also determined in additional AML cell lines, including MOLM-13 (IC50 = 12 μM) and MV4-11 (IC50 = 8.2 μM). SBI-4668 inhibited U-937 cell (harbor a G60R oncogenic mutation in SHP2) growth with IC50 of 6.3 uM, which is comparable to the potency found in AML cells expressing WT SHP2, while RMC4550 showed a very weak effect on this G60R mutation cell.

SBI-2130 (SBI 2130) is a novel furanylbenzamide molecule as inhibitor of both WT and oncogenic SHP2 with IC50 of 0.22/5.0 uM for Wt SHP2/SHP2-E76K.

SBI-0797750 (SBI 0797750) is a potent, fully selective PfGluPho inhibitor with robust nanomolar activity against recombinant PfGluPho, PvG6PD, and P. falciparum blood-stage parasites.SBI-0797750 disturbs the cytosolic glutathione-dependent redox potential, as well as the cytosolic and mitochondrial H2O2 homeostasis of P. falciparum blood stages, at low nanomolar concentrations.SBI-0797750 does not harm red blood cell (RBC) integrity and phagocytosis and thus does not promote anemia.

SBI-0637142 is a potent Smac mimetic that preferentially targets BIRC2, latency-reversing agent (LRA), specifically and potently promote HIV-1 latency reversal activity.SBI-0637142 modestly induced HIV-1 latency ex vivo in CD4+ T cells from ART-suppressed aviremic HIV-infected patients as a single agent, showed robust activity when administered in combination with the HDACi panobinostat.SBI-0637142's latency reversal activity is dependent on the NIK-dependent NF-κB signaling.

S2C3 is a small molecule HIV-1 fusion inhibitor, targets the membrane proximal external region (MPER) of HIV-1 envelope spike.S2C3 interacted with gp41-inter with an affinity of 2.0 uM.S2C3 has been shown to effectively block binding to the intact HIV-1 Env expressed on the cell surface by soluble CD4 but not by CD4 binding the sitedirected NAb VRC01, or the prefusion conformation-specific NAb PG16.S2C3 targets a site in the HIV-1 Env distinct from sites targeted by small-molecule entry inhibitors that have been identified so far.S2C3 could stabilize HIV-1 Env in the prefusion conformation, making it potentially useful in a vaccine preparation to reduce the conformational flexibility of Env.

S1g-2 (Hsp70-Bim inhibitor S1g-2) is a selective inhibitor to block interactions of Hsp70-Bim with IC50 of 0.4 uM in FPA assays, > 40-fold selectivity to target Hsp70-Bim over Bcl-2-Bim. S1g-2 induces cell-type-specific apoptosis in CML cells through selectively disrupting the Hsp70-Bim PPI. S1g-2 progressively enhanced lethality along with the increase in BCR-ABL-independent TKI resistance in the K562 cell lines. S1g-2 is more effective in primary samples from BCR-ABL-independent TKI-resistant patients than those from TKI-sensitive patients.

RTICBM-74 is a potent, selective, brain-penetrant CB1 negative allosteric modulator (NAM) with IC50 of 23 nM in Ca2+ assays.RTICBM-74 displays excellent half-life and low clearance against rat liver microsomes and hepatocytes, and excellent brain penetrance in rats.RTICBM-74 specifically reduces alcohol intake across a range of doses in male or female Wistar or Long-Evans rats, reduces alcohol intake and does not affect locomotion or sucrose self-administration.

RTICBM-229 is a potent, selective, brain-penetrant CB1 negative allosteric modulator (NAM) with IC50 of 169 nM in Ca2+ assay, 40 nM in GTPγS assay.

RS-1748 is a highly potent, selective, orallu active CCR4 antagonist, inhibits [125I]CCL17 binding to human CCR4 with IC50 of 59.9 nM.RS-1748 displays no competitive displacement in the binding of [125I]CCL3 (MIP-1α) to CCR1 and [125I]CCL2 (MCP-1) to CCR2b. dose-dependently inhibited 50 nM CCL22-induced [Ca2+]i mobilization with IC50 of 28.3 nM, inhibited the binding of [35S]GTPgS to human CCR4-expressing CHO cells with IC50 of 18.4 nM.Orally administered RS-1748 (30 mg/kg) significantly lowered the total cell numbers and the eosinophils numbers in ovalbumin-sensitized guinea pigs.

RS-1269 is a highly potent, selective CCR4 antagonist, inhibits [125I]CCL17 binding to human CCR4 with IC50 of 27.7 nM.RS-1269 also has strong affinity to displace the CCL17 binding with IC50 of 27.0 nM in CCR4-expressing CHO cells.RS-1269 displays no competitive displacement in the binding of [125I]CCL3 (MIP-1α) to CCR1 and [125I]CCL2 (MCP-1) to CCR2b.RS-1269 dose-dependently inhibited CCL17-induced migration of Th2 cells with IC50 of 5.5 nM.Orally administered RS-1269 (30 mg/kg) ameliorates ovalbumin-induced ear swelling in mice.RS-1269 also inhibited LPS-induced TNF-α production in vivo.

RP12146 (RP12146) is a novel, selective, and potent small molecule inhibitor of PARP1/2 with IC50 of 0.6/0.5 nM, with several fold selectivity over other isoforms.RP12146 inhibited cell growth in both BRCA mutant and non-BRCA mutant cancer cell lines with a GI50 range of 0.043 to 19.83 µM in a dose dependent manner.RP12146 demonstrated anti-tumor activities in both tumor size and tumor weight in OVCAR3 xenograft model.

Rohinitib is a potent and specific inhibitor of eIF4A1, inhibits growth and survival of AML cells especially cells with FLT3-ITD.

RO 5459072 (RG-7625) is a potent, highly selective of cathepsin S with IC50 of 0.1 nM and 0.3 nM for human and murine Cathepsin S, respectively; shows no sub-micro molar inhibition against others cathepsins (Cat L, B, K, and F) with the exception of Cat V (IC50=700  nM); dose-dependently reverses aberrant systemic autoimmunity, e.g. plasma cytokines, activation of myeloid cells and hypergammaglobulinemia, especially suppresses IgG autoantibody production.

RJR-2403 (Rivanicline, Metanicotine) is a potent, selective neuronal nicotinic ACh (nAChR) agonist with high affinity to rat brain cortex (Ki=26 nM), does not significantly activate muscle type nAChRs or muscarinic receptors; RJR-2403 is comparable to nicotine in activating rat thalamic synaptosomes with EC50 of 732 nM; significantly improves passive avoidance retention after scopolamine-induced amnesia and enhanced both working and reference memory in rats, also demonstrates greatly reduced cardiovascular effects; exerts its antinociceptive effect via nicotinic rather than either opioid or muscarinic mechanisms.

RGM8-51 is a β-lactam derivative, potent, selective TRPM8 antagonist with IC50 of 1.06 and 1.74 uM for rat and human TRPM8, respectively.RGM8-51 does not have any ability to activate TRPM8 channels, but produces a concentration-dependent inhibition of menthol activation.RGM8-51 is selective for cold-activated TRPM8 channels, displays no agonist or antagonist profile in cool-activated TRPA1 channels and has negligible activity as TRPV3 and ASIC3 channel antagonists.RGM8-51 (1 µM) inhibited menthol-activated currents in rTRPM8-expressing HEK293 cells.RGM8-51 exhibits in vivo antinociceptive activity in response to cold, in a mouse model of oxaliplatin-induced peripheral neuropathy.RGM8-51 reduces cold, mechanical and heat hypersensitivity in a rat model of neuropathic pain arising after chronic constriction of the sciatic nerve.RGM8-51 exhibits mechanical hypersensitivity-relieving activity, in a mouse model of NTG-induced hyperesthesia.