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JQ1

Inhibitor of BRD2, BRD4, BRD3, BRDT

Structure

Information

  • BRD2
  • BRD4
  • BRD3
  • BRDT
  • Inhibitor
  • 10 nM - 1 uM

In Vitro Validations

Uniprot ID: P25440
Target Class: Epigenetic
Target SubClass: Bromodomain
Potency: Kd
Potency Value: 128 nM
Potency Assay: ITC assay
PDB ID for probe-target interaction (3D structure): 2OSS,  3MXF
Target aliases:
Bromodomain-containing protein 2, RING3, KIAA9001, ...

DOI Reference: 10.1038/nature09504

Uniprot ID: P25440
Target Class: Epigenetic
Target SubClass: Bromodomain
Potency: IC50
Potency Value: 76.9 BD1, 32.6 BD2 nM
Potency Assay: alpha screen
PDB ID for probe-target interaction (3D structure): 3ONI
Target aliases:
Bromodomain-containing protein 2, RING3, KIAA9001, ...

DOI Reference: 10.1038/nature09504

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Differential scanning fluorimetry; for comparison BRD2/1: 6.47, BRD2/2: 7.97, BRD3/1: 8.27, BRD3/2: 8.39, BRD4/1: 9.35, BRD4/2: 7.44, BRDT/1: 3.93. No activity was detected against: ASH1L, BAZ2B, BRD1, BRD9, BRPF1, CECR2, FALZ, GCN5L2, LOC93349, PB1/1, PB1/2, PB1/5, PB1/6, PCAF, PHIP/2, SP140, TAF1L/3, TIF1, WDR9
Probe Selectivity in Vitro:

In ExpressProfile, negligible activity was detected: H2 [cimetindine]: -27, Neurokinin NK3 [SB 222200]: -23, Somatostatin SST [somatostatin-14]: -22 Benzodiazepine [diazepam]: -20, Prostanoid TP (TXA2/PGH2)[U 44069]: -19, Serotonin 5-HT transporter [imipramine]: -19, Serotonin 5-HT1A [8-OH-DPAT]: : -14, Muscarinic M1 [pirenzepine]: -14, GABA [GABA]: -12, Serotonin 5-HT7 [serotonin]: -12, Norepinephrine transporter [protriptyline]: -10, Adenosine A1 [DPCPX]: -10, Adenosine A2A [NECA]: -9, VPAC1 [VIP]: -9, Dopamine transporter [BTCP]: -7, Alpha-2 Adrenergic (nonselective) [yohimbine]:-7, Serotonin 5-HT5a [serotonin]: -7, Opioid Delta 2 (DOP) [DPDPE]: -6, Serotonin 5-HT3 [MDL 7222]: -6, Chemokine CXCR2 (IL-8B) [IL-8]: -5 Alpha-1 Adrenergic (nonselective) [prazosin]: -5, Histamine H1 [pyrilamine]: -5, Vasopressin V1a [[d(CH2)51Tyr(Me)2]-AVP]: -5, Ca2+ channel [D 600]: -5 Chemokine CCR1 [MIP-1alpha]: -4, Opioid Mu (MOP) [DAMGO]: -4, K+ (KV) channel [alpha-dendrotoxin]: -4, Serotonin 5-HT1B [serotonin]: -4,, Muscarinic M3 [4-DAMP]: -4, Neurotensin NTS1 (NT1) [neurotensin]: -4, Bradykinin B2 [NPC 567]: -3, Opioid-like NOP (ORL1) [nociception]: -2, Dopamine D1 [SCH 23390]: -2, Dopamine D2S [(+)-butaclamol]:-2, Neuropeptide Y1 [NPY]: -2, Serotonin 5-HT2B [DOI]: -2, Angiotensin-II AT1 [saralasin]: 0, Cannabinoid CB1 [CP 55940]: 0, Melanocortin MC4 [NDP-alpha-MSH]: 0, Beta-1 Adrenergic [atenolol]: +1, Muscarinic M2 [methoctramine]: +2, Serotonin 5-HT6 [serotonin]: +2, Cl- channel (GABA gated) [picrotoxinin]: +3, K+ Channel SKCa [apamin]: +3, Opioid Kappa (KOP) [U 50488]: +3 Beta-2 Adrenergic [ICI 118551]: +4, Galanin GAL2 [galanin]: +5, Cholecystokinin CCK1 (CCKA) [CCK-8s]: +9, Neuropeptide Y2 [NPY]: +10, Endothelin ETA [endothelin-1]: +16, Na+ channel [veratridine]: +18, Serotonin 5-HT2A [ketanserin]: +24, Melatonin MT1( ML1A) [melatonin]: +29, Neurokinin NK2 [[Nleu10]-NKA (4010)]: +56, Adenosine A3 [IB-MECA]: +61

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SERP ratings and comments

SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 18 May 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

JQ1 is very potent probe for the BET family of proteins that can be used in cells.

(last updated: 24 May 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

This is an excellent selective cellular probe for the BET family of bromodomains, binding potently to all eight (BD1 and BD2 of BRD2/3/4/T). It has been extensively used in cells as a positive control. Its drawback is its suboptimal in vivo pharmacokinetics (IV t1/2 0.9 hours: source http://dx.doi.org/10.1038%2Fnature09504), so for in vivo studies, I would recommend using other BET-family bromodomain inhibitors.

(last updated: 30 May 2016 )

Portal Comments

In a 2023 study, Hu et al. evaluated JQ1 in live-cell assays for Phospholipidosis induction, cautioning about adverse effects at concentrations near 1 uM. (DOI: 10.1016/j.chembiol.2023.09.003)

(last updated: 7 Nov 2023)