2810747-89-6
2810747-89-6
Chemical Structure
BLU2864
- CAS No.: 2810747-89-6
- Formula:C24H19F3N4O2
- Molecular Weight:452.43
IUPAC Name: N-((1R,2S)-5-(difluoromethyl)-7-fluoro-2-hydroxy-2,3-dihydro-1H-inden-1-yl)-6-(3-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)nicotinamide
InChIKey: VRPOVDLLZCQZEG-RXVVDRJESA-N
SMILES: FC1=CC(C(F)F)=CC2=C1[C@H]([C@@H](O)C2)NC(C(C=C3)=CN=C3C4=C(C(C)=CN5)C5=NC=C4)=O
Biological Activity: BLU2864 is an orally active, highly selective, ATP-competitive PRKACA inhibitor (IC50=0.3 nM). BLU2864 shows anti-tumor activity. BLU2864 can be used in cancer and polycystic kidney disease research[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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BLU2864 | 99.50% | BLU2864 is an orally active, highly selective, ATP-competitive PRKACA inhibitor (IC50=0.3 nM). BLU2864 shows anti-tumor activity. BLU2864 can be used in cancer and polycystic kidney disease research. | ||||||||||||||||||||
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Porcn-IN-1 | 99.57% | Porcn-IN-1 is potent porcupine inhibitor with an IC50 of 0.5±0.2 nM. | ||||||||||||||||||||
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LY593093 | 98.82% | LY593093 is a selective, orally active, and brain-penetrant muscarinic M1 receptor agonist with an EC50 of 22.8 nM. LY593093 can be utilized in Alzheimer’s disease research. | ||||||||||||||||||||
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VU6004256 | 99.61% | VU6004256 is a potent and selective M1 muscarinic positive allosteric modulator (PAM) with an EC50 value of 155 nM. VU6004256 has the potential for the research of schizophrenia. | ||||||||||||||||||||
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MK-3901 | MK-3901 is a selective P2X3 receptor antagonist with an IC50 of 24 nM. MK-3901 inhibits UGT1A1 (with an IC50 of 1 μM) and CYP2C9 (with an IC50 of 5.7 μM). MK-3901 activates PXR. MK-3901 induces hyperbilirubinemia. MK-3901 can be used for the research of inflammatory pain. | |||||||||||||||||||||
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SGI-7079 | 99.32% | SGI-7079 is a selective, ATP-competitive, orally active inhibitor of the receptor tyrosine kinase Axl. SGI-7079 blocks Axl-mediated signaling pathways such as NF-κB activation and MMP-9 expression, thereby inhibiting tumor cell proliferation, migration and invasion. SGI-7079 is mainly used in the research of malignant tumors such as inflammatory breast cancer and bladder cancer, as well as in combination with immunization (used in combination with PD-1 therapy). | ||||||||||||||||||||
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BTK inhibitor 13 | BTK inhibitor 13 is an orally active Bruton's tyrosine kinase (BTK) inhibitor, with an IC50 value of 1.2 nM against human BTK. BTK inhibitor 13 covalently modifies the Cys481 residue of BTK when binding to the inactive conformation of BTK. BTK inhibitor 13 is used for the research of autoimmune diseases. | |||||||||||||||||||||
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CLK1-IN-3 | 98.54% | CLK1-IN-3 (compound 10ad) is a potent and selective Clk1 inhibitor, with an IC50 of 5 nM and over 300-fold selectivity for Dyrk1A. CLK1-IN-3 also shows a relatively potent inhibition against Clk2 and Clk4, with IC50 values of 42 and 108 nM, respectively. CLK1-IN-3 potently induces autophagy in vitro. CLK1-IN-3 can be used for acute liver injury (ALI) research. | ||||||||||||||||||||
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BTK-IN-15 | BTK-IN-15 (compound 42) is a potent Bruton's tyrosine kinase (BTK) inhibitor with high oral absorption. BTK-IN-15 inhibits BTK with an IC50 value of 0.7 nM. BTK-IN-15 displays excellent kinase selectivity, antitumor activity, and induces apoptosis. | |||||||||||||||||||||
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BLU0588 | 97.63% | BLU0588 is an orally active, potent and selective PRKACA (protein kinase cAMP-activated catalytic subunit alpha) kinase inhibitor, with an IC50 of 1 nM and dissociation constant (Kd) of 4 nM. BLU0588 can be used for fibrolamellar carcinoma (FLC) research. | ||||||||||||||||||||
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VU6052254 | 98.18% | VU6052254, a derivative of VU0467319 (HY-173396), is a selective, potent, orally active and brain-penetrant muscarinic M1 acetylcholine receptor (mAChR1) positive allosteric modulator with an EC50 of 59 nM. VU6052254 has no activity on the M2-5 receptor (EC50 > 30 μM). VU6052254 can improve memory recognition ability and reverse the cognitive impairment induced by Scopolamine (HY-N0296) with minimum effective dose both of 1 mg/kg. VU6052254 can be used for the research of neurological disease, such as Alzheimer's disease. | ||||||||||||||||||||
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References
- [1]. Xiaofang Wang, et al. Protein Kinase A Downregulation Delays the Development and Progression of Polycystic Kidney Disease. J Am Soc Nephrol. 2022 Jun;33(6):1087-1104. [Content Brief]
- [2]. Stefanie S. Schalm, et al. Evaluation of PRKACA as a Therapeutic Target for Fibrolamellar Carcinoma. bioRxiv 2022.01.31.477690.
