variants

Telaglenastat (CB 839) (IC50 of 24 nM), an effective, specific, and oral inhibitor, which is bioavailable glutaminase, for recombinant human GAC.

RMC-6236 is an orally effective and novel triple complex RAS (ON) MULTI inhibitor, which is a potent non covalent inhibitor of multiple RAS variants in GTP binding state. RMC-6236 has anti-tumor activity and can be used in research related to RAS driven tumors. With rich experience in compound synthesis, we can provide fast customized synthesis services for this product according to your research needs.

Vepdegestrant (ARV-471) is an estrogen receptor (ER) α PROTAC molecule that degrades ER in ER-positive breast cancer cell lines with a DC50 of approximately 1 nM. It can reduce the expression of classically regulated ER target genes and inhibit the growth of ER-dependent cell lines (including those expressing ESR1 variants, such as Y537S and D538G) by degrading ER.

4'-Ethynyl-2'-deoxyadenosine (4'-E-dA), a nucleoside reverse transcriptase (RT) inhibitor, demonstrates potent activity against drug-resistant HIV variants, with an EC50 of 98 nM in MT-4 cells for anti-HIV-1 activity.

Grazoprevir sodium salt is a selective Hepatitis C virus NS3/4a protease inhibitor with broad activity across genotypes and resistant variants.

Inarigivir soproxil (SB9200) is an agonist of innate immunity that demonstrates effective antiviral activity against resistant hepatitis C virus (HCV) variants, with EC50s of 2.2 and 1.0 μM for HCV 1a/1b in cells of genotype 1 HCV replicon systems.

RX-3117 (fluorocyclopentenylcytosine) is a novel a cytidine analog. RX-3117 displays anticancer activity in several cancer cell lines, including gemcitabine-resistant variants.

KRAS inhibitor-31 (compound 33), a potent agent targeting KRAS, exhibits K D (SPR) values of 0.019 nM for KRas G12D, 0.019 nM for KRas G12C, and 0.096 nM for KRas G12V, illustrating its efficacy across these variants.

LX1, an anti-prostate cancer compound, specifically targets the androgen receptor (AR), AR variants, and the steroidogenic enzyme AKR1C3. It inhibits AKR1C3's enzymatic function, decreases the conversion of androstenedione to testosterone, and reduces the expression of both AR and AR-V7, subsequently downregulating their target genes. Additionally, LX1 is effective in overcoming tumor cell resistance to Enzalutamide, and when combined with Enzalutamide, it further suppresses tumor growth.

SARS-CoV-2-IN-100 (Compound 172) is a broad-spectrum antiviral agent against various SARS-CoV-2 variants. It works synergistically with Nirmatrelvir to reduce the risk of antiviral resistance.

SARS-CoV-2 Mpro-IN-32 (Compound 1) is a selective inhibitor of SARS-CoV-2 MPro with an IC50 value of 230 nM. In vitro, it also inhibits the replication of various SARS-CoV-2 variants.

SLC6A8 Corrector 1 is an orally active corrector for mutant SLC6A8 variants, capable of crossing the blood-brain barrier. It is utilized in the study of creatine transporter deficiency (CTD).

CACPD2011a-0001278239 is a β2AR hybrid agonist with high affinity binding to both the wild-type and T164I β2AR variants. It exhibits neither cytotoxicity nor mutagenicity, making it suitable for asthma research.

HNC-1664 is an orally active inhibitor of RNA-dependent RNA polymerase (RdRP). It exhibits broad-spectrum antiviral activity against coronaviruses, including SARS-CoV-2 wild type and its variants (XBB.1.18, HK.3.1, BF.7.14, BA.1, HCoV-229E, HCoV-OC43), as well as arenaviruses. HNC-1664 also demonstrates anti-infective efficacy in a mouse model infected with the SARS-CoV-2 Delta variant.

9-AMN is an inhibitor of the SARS-CoV-2 papain-like protease (SARS-CoV-2 PLpro), effectively reducing its deubiquitinating (DUB) activity and protease activity, with IC50 values of 4.55 µM and 4.15 µM, respectively. Additionally, 9-AMN suppresses the replication of the SARS-CoV variants Delta and Omicron in Calu-3 cells, with IC50 values of 1.04 µM and 2.35 µM, respectively.

Jun13296 is an orally active quinoline SARS-CoV-2 papain-like protease inhibitor (IC50 = 0.13 µM, Ki = 8.8 nM). It demonstrates potent inhibitory effects against SARS-CoV-2 variants and Nirmatrelvir-resistant mutants. Jun13296 reduces lung viral titers and prevents lung tissue damage in SARS-CoV-2 infection models.

AB-343 is a selective covalent inhibitor of SARS-CoV-2 Mpro with an IC50 of 8 nM and a Ki of 2.8 nM. It effectively inhibits the main protease of SARS-CoV-2 and several other coronaviruses and is active against some resistant variants. AB-343 can be utilized in research related to diseases associated with coronavirus infections.

TKB272 is an orally active antiviral agent that selectively targets the main protease (Mpro) of SARS-CoV-2, effectively inhibiting the infection and replication of various strains, including Omicron variants (such as XBB.1.5 and EG.5.1). It exhibits an enzyme inhibitory activity with an IC50 of 0.7 µM against SARS-CoV-2WK-521 Mpro and shows potent antiviral activity at the cellular level with an EC50 as low as 2.6 nM in HeLahACE2-TMPRSS2 cells against the BQ.1.1 strain. TKB272 also has a CC50 of 98 µM, indicating low cytotoxicity. Furthermore, it demonstrates a significant suppression of SARS-CoV-2XBB.1.5 replication in the B6.Cg-Tg(K18-hACE2)2-Prlmn/J transgenic mouse model, suggesting potential use in the research of SARS-CoV-2 infections.

hSTING activator-1 (Compound 68) is a STING agonist capable of effectively activating various human STING variants (R232, H232, HAQ), with EC50 values of 56 nM, 89 nM, and 51 nM, respectively. This compound activates the type I interferon pathway by directly binding to the STING protein and stabilizing its conformation, which leads to downstream IRF3 phosphorylation and cytokine release. hSTING activator-1 also demonstrates potential in cancer research by inhibiting fibrosarcoma tumor growth.

DNJ-20 is an α-glucosidase inhibitor with an IC50 of 55.3 μg/mL. It exhibits broad-spectrum activity against SARS-CoV-2. By interfering with the endoplasmic reticulum-associated glycoprotein folding process (ERQC), DNJ-20 hinders the proper processing of viral glycoproteins, thus blocking the formation and infection of viral particles. It is effective against several SARS-CoV-2 variants, as well as HCoV-229E and HCoV-0C43, with IC50 values reaching up to 1.49 μM. DNJ-20 can be utilized for pan-coronavirus research.

N-0920 is a potent TMPRSS2 inhibitor with an IC50 value of 0.35 nM. It effectively inhibits the entry of SARS-CoV-2 variants [EG.5.1] and [JN.1] into Calu-3 cells, exhibiting EC50 values of 300 pM and 90 pM, respectively.

Grazoprevir, a second generation hepatitis C virus protease inhibitor acting at the NS3/4a protease targets, has good activity against a range of hepatitis C virus genotype variants, including some that are resistant to most currently used antiviral medic

Ensartinib hydrochloride (X-396 dihydrochloride) is a potent new-generation ALK inhibitor with high activity against CNS metastases and a broad range of known crizotinib-resistant ALK mutations. It potently inhibits both wild-type ALK and ALK variants (C1156Y, F1174, G1202R, L1196M, S1206R, and T1151 mutants) with in vitro IC50s of <4 nM.

AG-7404 is a potent protease inhibitor with anti-poliovirus activity. AG-7404 was active against all virus with EC50 values ranging from 0.080 to 0.674 μM. AG-7404 was fully active against V-073-resistant variants with EC50 values ranging from 0.218 to 0.