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Results for "

splice variant

" in MedChemExpress (MCE) Product Catalog:

11

Inhibitors & Agonists

1

Inhibitory Antibodies

1

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-12248
    Telaglenastat
    60+ Cited Publications

    CB-839

    		 Glutaminase Autophagy Cancer
    Telaglenastat (CB-839) is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat inuduces autophagy and has antitumor activity .
    Telaglenastat
  • HY-117960
    Orismilast

    LEO-32731

    		 Phosphodiesterase (PDE) Inflammation/Immunology
    Orismilast (LEO-32731) is an orally active and selective PDE4 inhibitor used for the research of inflammatory diseases. Orismilast demonstrates potent inhibition of PDE4B and PDE4D subtype splice variants .
    Orismilast
  • HY-N1943
    Ailanthone

    Δ13-Dehydrochaparrinone

    		 Androgen Receptor Inflammation/Immunology Cancer
    Ailanthone (Δ13-Dehydrochaparrinone) is a potent inhibitor of both full-length androgen receptor (AR) (IC50=69 nM) and constitutively active truncated AR splice variants (AR1-651 IC50=309 nM).
    Ailanthone
  • HY-150102
    EPI-7170

    		Androgen Receptor Cancer
    EPI-7170, a ralaniten analogue, is a potent androgen receptor N-terminal structural domain antagonist that blocks the transcriptional activity of full-length AR (FL-AR) and AR splice variants (AR-Vs). EPI-7170 has antitumor effects against enzalutamide resistant castration-resistant prostate cancer (CRPC) .
    EPI-7170
  • HY-145709
    Ar-V7-IN-1

    		Androgen Receptor Cancer
    Ar-V7-IN-1 is a potent inhibitor of Ar-V7. AR-V7 is a hormone-independent splice variant of the androgen receptor. Ar-V7-IN-1 has the potential for the research of various indications, in particular cancers such as prostate cancer (extracted from patent WO2018114781A1, compound 43) .
    Ar-V7-IN-1
  • HY-153341
    CFT1946

    		PROTACs Raf Cancer
    CFT1946 is an orally active, CRBN-based and mutant-selective bifunctional degradation activating compound (BiDAC ™) degrader of BRAF V600E with a DC50 of 14 nM in A375 cells. CFT1946 is capable of degrading BRAF V600E (Class I), G469A (Class II), G466V (Class III) mutations, and the p61-BRAF V600E splice variant. CFT1946 can be used in tumor research .
    CFT1946
  • HY-155812
    Tyrosine kinase-IN-6

    		c-Met/HGFR Cancer
    Tyrosine kinase-IN-6 is a potent and promising RON splice variants inhibitor with anti-cancer and o?antineoplastic effects .
    Tyrosine kinase-IN-6
  • HY-121249
    Capeserod hydrochloride

    SL65.0155

    		 5-HT Receptor Neurological Disease
    Capeserod hydrochloride (SL65.0155) is a 5-HT4(e) receptor partial agonist (Ki=0.6 nM) with potent cognitive enhancing properties. Capeserod hydrochloride acts as a partial agonist in cells expressing 5-HT4(b) and 5-HT4(e) splice variants, stimulating cAMP production with IC50 values ??of 244 and 29 nM, respectively. Capeserod hydrochloride is used in the study of memory impairment and dementia .
    Capeserod hydrochloride
  • HY-12248A
    Telaglenastat hydrochloride

    CB-839 hydrochloride

    		 Glutaminase Autophagy Cancer
    Telaglenastat (CB-839) hydrochloride is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat hydrochloride selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat hydrochloride inudces autophagy and has antitumor activity .
    Telaglenastat hydrochloride
  • HY-P990782
    Efzofitimod

    		Aminoacyl-tRNA Synthetase Inflammation/Immunology
    Efzofitimod is a splice variant of the aminoacyl-tRNA synthetase HARS1, which is fused with the Fc segment of a human antibody. Efzofitimod targets the neuronal phospholipid NRP2 (neuropilin-2) and has anti-inflammatory and immunomodulatory activities. Efzofitimod can downregulate the innate and adaptive immune responses in inflammatory disease states, suppressing indirect lung disease (ILD) .
    Efzofitimod
  • HY-160777
    VNPP433-3β

    Galeterone 3β-imidazole

    		 Androgen Receptor MNK Cancer
    VNPP433-3β is a molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. VNPP433-3β inhibits proliferation of cancer cell LNCaP, C4-2B and CWR22Rv1 with GI50 of 0.2, 0.3 and 0.31 μM. VNPP433-3β exhibits good pharmacokinetic characters in CD-1 mouse and inhibits tumor growth in the CWR22Rv1 xenograft mouse model .
    VNPP433-3β

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